Search Result
Results for "
H1 receptor antagonist
" in MedChemExpress (MCE) Product Catalog:
55
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B0781
-
|
Histamine Receptor
mAChR
Adrenergic Receptor
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Neurological Disease
Endocrinology
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Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
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- HY-119832B
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(S)-EGIS-2062 free acid; (S)-EGYT-2062 free acid
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Histamine Receptor
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Inflammation/Immunology
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(S)-Setastine ((S)-EGIS-2062 free acid) is a non-sedating, highly potent antagonist of H1 receptor-mediated responses. (S)-Setastine has a long-lasting antihistamine effect and good oral efficacy. (S)-Setastine can be used in the research of allergic diseases .
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- HY-B1067A
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Phenazoline
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Histamine Receptor
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Neurological Disease
Endocrinology
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Antazoline (Phenazoline) is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline has anti-arrhythmic effect in acute myocardial infarctions. Antazoline can be studied in research for cardiovascular diseases, and HBV .
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- HY-B1281
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Pyrilamine maleate
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Histamine Receptor
|
Neurological Disease
Endocrinology
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Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with Kds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pKd of 9.4 for H1 receptor.
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- HY-B1589A
-
-
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- HY-B0781R
-
|
Reference Standards
Histamine Receptor
mAChR
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Promethazine (hydrochloride) (Standard) is the analytical standard of Promethazine (hydrochloride). This product is intended for research and analytical applications. Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
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-
-
- HY-B1067B
-
Phenazoline phosphate
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Antazoline phosphate is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect .
Antazoline phosphate is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline phosphate can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline phosphate can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline phosphate can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline phosphate also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline phosphate has anti-arrhythmic effect in acute myocardial infarctions. Antazoline phosphate can be studied in research for cardiovascular diseases, and HBV .
|
-
-
- HY-B1067AR
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Phenazoline (Standard)
|
Reference Standards
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Antazoline (Phenazoline) (Standard) is the analytical standard of Antazoline. This product is intended for research and analytical applications. Antazoline is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline has anti-arrhythmic effect in acute myocardial infarctions. Antazoline can be studied in research for cardiovascular diseases, and HBV .
|
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- HY-B1067BR
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Phenazoline phosphate (Standard)
|
Reference Standards
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Antazoline (phosphate) (Standard) is the analytical standard of Antazoline (phosphate). This product is intended for research and analytical applications. Antazoline phosphate is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline phosphate can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline phosphate can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline phosphate can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline phosphate also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline phosphate has anti-arrhythmic effect in acute myocardial infarctions. Antazoline phosphate can be studied in research for cardiovascular diseases, and HBV .
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- HY-100280
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- HY-B1589
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- HY-B1303A
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- HY-129783
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- HY-B1281R
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Pyrilamine maleate (Standard)
|
Reference Standards
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Mepyramine maleate (Standard) is the analytical standard of Mepyramine maleate. This product is intended for research and analytical applications. Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with Kds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pKd of 9.4 for H1 receptor.
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- HY-B1303
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- HY-402545
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- HY-U00018
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- HY-B0548S1
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-
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- HY-W010841
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(R)-Cetirizine dihydrochloride
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Histamine Receptor
|
Inflammation/Immunology
Endocrinology
Cancer
|
Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
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- HY-B0814
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(R)-Cetirizine
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
Cancer
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Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
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- HY-101830
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- HY-B0286A
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- HY-B0298A
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HS-592 fumarate; Meclastine fumarate
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Histamine Receptor
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Neurological Disease
Endocrinology
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Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist. Clemastine fumarate is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .
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- HY-B0539S3
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- HY-B0539S1
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- HY-B0539S
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- HY-B0298
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HS-592; Meclastine
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Histamine Receptor
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Neurological Disease
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Clemastine (HS-592) is a potent and orally active histamine receptor H1 antagonist. Clemastine is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .
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- HY-B1589AS
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- HY-B0539R
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- HY-105542
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Histamine Receptor
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Neurological Disease
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Niaprazine is a histamine H1-receptor antagonist. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research .
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- HY-101724
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NNC-05-1869 hydrochloride
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Histamine Receptor
|
Inflammation/Immunology
Endocrinology
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ReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guinea pig brain) with Ki of 0.19±0.04 μM and the non-selective σ site (guinea pig brain) with Ki of 0.45 μM.
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- HY-W701635
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- HY-A0178A
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- HY-U00084
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- HY-B0539S4
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- HY-B0814S
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(R)-Cetirizine-d4(dihydrochloride)
|
Isotope-Labeled Compounds
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Levocetirizine-d4 (dihydrochloride) is the deuterium labeled Levocetirizine. Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].
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- HY-123829
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- HY-B0539S2
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- HY-B0814R
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
Cancer
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Levocetirizine (Standard) is the analytical standard of Levocetirizine. This product is intended for research and analytical applications. Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
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- HY-W010841R
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(R)-Cetirizine dihydrochloride (Standard)
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Reference Standards
Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Levocetirizine (dihydrochloride) (Standard) is the analytical standard of Levocetirizine (dihydrochloride). This product is intended for research and analytical applications. Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
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- HY-B0303A
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- HY-B0548AS
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- HY-A0178
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- HY-19489S
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- HY-W653762
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- HY-B1589AR
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- HY-B1305
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- HY-17042B
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(S)-P071
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Histamine Receptor
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Inflammation/Immunology
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(S)-Cetirizine dihydrochloride ((S)-P071) is an orally active antagonist of the histamine H1 receptor with a Ki value of 39.1 nM. (S)-Cetirizine dihydrochloride exerts anti-allergic activity by binding to the histamine H1 receptor and blocking the action of histamine. (S)-Cetirizine dihydrochloride is promising for research of allergic diseases such as allergic rhinitis .
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- HY-B0303
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- HY-B0298AR
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HS-592 fumarate (Standard); Meclastine fumarate (Standard)
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Reference Standards
Histamine Receptor
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Neurological Disease
Endocrinology
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Clemastine (fumarate) (Standard) is the analytical standard of Clemastine (fumarate). This product is intended for research and analytical applications. Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist. Clemastine fumarate is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .
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- HY-B1303AR
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- HY-105014
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Norastemizole
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Histamine Receptor
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Inflammation/Immunology
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Tecastemizole (Norastemizole), a major metabolite of Astemizole, is a potent and selective H1 receptor antagonist. Tecastemizole shows anti-inflammatory activities .
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- HY-B0781S1
-
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Isotope-Labeled Compounds
mAChR
Adrenergic Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Promethazine-d3 (hydrochloride) is deuterium labeled Promethazine (hydrochloride). Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
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- HY-B0524A
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- HY-B0524
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- HY-D0237
-
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Histamine Receptor
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Inflammation/Immunology
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Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist . Betahistine mesylate is used for the study of rheumatoid arthritis (RA) .
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- HY-B1296S1
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- HY-B0814S1
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(R)-Cetirizine-d4
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Isotope-Labeled Compounds
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Inflammation/Immunology
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Levocetirizine-d4 ((R)-Cetirizine-d4) is the deuterium-labeled Levocetirizine (HY-B0814) . Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
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- HY-B0895
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- HY-131256A
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Cetirizine Impurity C dihydrochloride is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist [1] [2] .
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- HY-131256
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Cetirizine Impurity C is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist [1] [2] .
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- HY-12966
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- HY-30234S
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Histamine Receptor
HCV
TRP Channel
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Cancer
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Clemizole-d4 is a deuterium labeled Clemizole. Clemizole is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication .
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- HY-B0298AS
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- HY-B0895R
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- HY-17039
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R89674
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Alcaftadine (R89674) is a histamine H1 receptor antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis. Alcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. Alcaftadine also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects .
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- HY-122508
-
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Drug Metabolite
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Neurological Disease
|
Hydroxyebastine is an Ebastine (HY-B0674) (a histamine H1-receptor antagonist) metabolite. Hydroxyebastine is metabolized to Carebastine (HY-121356) by CYP2J2 and CYP3A4 .
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- HY-B1303R
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Mebhydroline 1,5-naphthalenedisulfonate salt (Standard)
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Reference Standards
Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Mebhydrolin (napadisylate) (Standard) is the analytical standard of Mebhydrolin (napadisylate). This product is intended for research and analytical applications. Mebhydrolin napadisylate is a specific histamine H1 receptor antagonist.
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- HY-B1397C
-
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Histamine Receptor
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Neurological Disease
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Cyclizine hydrochloride, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine hydrochloride can be used for the research of nausea, vomiting, and dizziness .
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- HY-B1397A
-
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Histamine Receptor
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Neurological Disease
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Cyclizine dihydrochloride, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine dihydrochloride can be used for the research of nausea, vomiting, and dizziness .
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- HY-B1397
-
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Histamine Receptor
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Neurological Disease
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Cyclizine, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine can be used for the research of nausea, vomiting, and dizziness .
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- HY-A0069A
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- HY-A0069
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- HY-B0286AR
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- HY-117501
-
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Histamine Receptor
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Inflammation/Immunology
Cancer
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Dexchlorpheniramine is an potent and blood-brain barrier (BBB) penetrant histamine 1 (H1) receptor antagonist with anticholinergic properties. Dexchlorpheniramine can be used for researching allergies .
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- HY-14447S
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- HY-17428
-
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Histamine Receptor
Endogenous Metabolite
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Inflammation/Immunology
Endocrinology
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Tripelennamine hydrochloride, an ethylenediamine derivative, is a potent histamine H1-receptor antagonist. Tripelennamine hydrochloride lessens the allergic response of the organism caused by histamine. Tripelennamine hydrochloride can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions .
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- HY-105542R
-
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Reference Standards
Histamine Receptor
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Neurological Disease
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Niaprazine (Standard) is the analytical standard of Niaprazine. This product is intended for research and analytical applications. Niaprazine is a histamine H1-receptor antagonist. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research .
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- HY-B0303AS1
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- HY-14447
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Bilastine is an oral histamine H1-receptor antagonist. Bilastine can be used for allergic rhinitis and urticaria studies, and it also improves diabetic nephropathy in mice, showing safety for the central nervous system .
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- HY-B0303AS
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- HY-17428A
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- HY-101690
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- HY-101633
-
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Histamine Receptor
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Others
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GSK-1004723 is a novel H1/H3 receptor antagonist with limited activity for the suppression of seasonal allergic rhinitis. GSK-1004723 is available as a suspension or solution for intranasal administration.
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- HY-A0191
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(+)-Brompheniramine; (S)-Brompheniramine
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Endogenous Metabolite
Histamine Receptor
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Inflammation/Immunology
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Dexbrompheniramine is an orally active H1 receptor antagonist. Dexbrompheniramine is an antihistamine that reduces the effects of natural chemical histamine. Dexbrompheniramine can be used for the research of hay fever and urticaria .
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- HY-B1397B
-
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Histamine Receptor
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Neurological Disease
|
Cyclizine lactate, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine lactate can be used for the research of nausea, vomiting, and dizziness .
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- HY-A0191A
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(+)-Brompheniramine maleate; (S)-Brompheniramine maleate
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Endogenous Metabolite
Histamine Receptor
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Inflammation/Immunology
|
Dexbrompheniramine maleate is an orally active H1 receptor antagonist. Dexbrompheniramine maleate is an antihistamine that reduces the effects of natural chemical histamine. Dexbrompheniramine maleate can be used for the research of hay fever and urticaria .
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- HY-14447R
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- HY-B0548
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Hydroxyzine, a benzodiazepine antihistamine agent, acts as an orally active histamine H1-receptor and serotonin antagonist.
Hydroxyzine has anxiolytic effect and can be used for the research of generalised anxiety disorder .
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- HY-B0801A
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MDL-16455 hydrochloride; Terfenadine carboxylate hydrochloride
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Histamine Receptor
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Inflammation/Immunology
Cancer
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Fexofenadine (MDL-16455) hydrochloride is an orally active and nonsedative H1 receptor antagonist. Fexofenadine hydrochloride can be used in allergic rhinitis and chronic idiopathic urticarial research .
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- HY-131579
-
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Drug Metabolite
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Inflammation/Immunology
|
Deschloro Cetirizine Dihydrochloride is a Cetirizine impurity. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist.
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- HY-B0801
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MDL-16455; Terfenadine carboxylate
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Histamine Receptor
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Inflammation/Immunology
Cancer
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Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research .
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- HY-17042A
-
P071
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
Cancer
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Cetirizine dihydrochloride, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine dihydrochloride marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
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- HY-17042
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
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- HY-B0349B
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Meclozine dihydrochloride monohydrate
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Histamine Receptor
Apoptosis
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Neurological Disease
Inflammation/Immunology
|
Meclizine (Meclozine) dihydrochloride monohydrate, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride monohydrate is an effective anti-motion sickness agent. Meclizine dihydrochloride monohydrate crosses the blood-brain barrier. Meclizine dihydrochloride monohydrate is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine dihydrochloride monohydrate can be used for the research of polyQ toxicity disorders, such as Huntington's disease .
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- HY-B0349
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Meclozine dihydrochloride
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Histamine Receptor
Apoptosis
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Neurological Disease
Endocrinology
Cancer
|
Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .
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- HY-B0349A
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Meclozine
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Histamine Receptor
Apoptosis
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Neurological Disease
Inflammation/Immunology
|
Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease .
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- HY-17039R
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R89674 (Standard)
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Alcaftadine (Standard) is the analytical standard of Alcaftadine. This product is intended for research and analytical applications. Alcaftadine (R89674) is a histamine H1 receptor antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis. Alcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. Alcaftadine also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects .
|
-
- HY-B0524AS
-
-
- HY-14277A
-
R 50547 hydrochloride
|
Histamine Receptor
Neurotensin Receptor
Integrin
|
Inflammation/Immunology
|
Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) .
|
-
- HY-14277
-
R 50547
|
Histamine Receptor
Neurotensin Receptor
Integrin
|
Inflammation/Immunology
|
Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) .
|
-
- HY-17428B
-
|
Histamine Receptor
Endogenous Metabolite
|
Inflammation/Immunology
Endocrinology
|
Tripelennamine citrate, an ethylenediamine derivative, is a potent histamine H1-receptor antagonist. Tripelennamine citrate lessens the allergic response of the organism caused by histamine. Tripelennamine citrate can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions .
|
-
- HY-B0303AR
-
-
- HY-B0970
-
4-Diphenylmethoxy-1-methylpiperidine hydrochloride
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Diphenylpyraline hydrochloride is a potent histamine H1?receptor antagonist. Diphenylpyraline hydrochloride acts as an orally active antihistamine agent?with antimuscarinic and antiallergic effects. Diphenylpyraline hydrochloride can be used for the relief of allergic conditions including rhinitis and hay fever, and in pruritic skin disorders in vivo.
|
-
- HY-B0674
-
LAS-W 090; RP64305
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research .
|
-
- HY-W750960R
-
|
Reference Standards
Antibiotic
|
Others
|
Isothipendyl (hydrochloride) (Standard) is the analytical standard of Isothipendyl (hydrochloride). This product is intended for research and analytical applications. Isothipendyl hydrochloride (), an azaphenothiazine derivative, is a potent histamine 1 (H1) receptor antagonist.othipendyl is a primary metabolite .
|
-
- HY-A0178AR
-
NSC 169186 (Standard)
|
Reference Standards
Endogenous Metabolite
Histamine Receptor
|
Inflammation/Immunology
|
Isothipendyl (hydrochloride) (Standard) is the analytical standard of Isothipendyl (hydrochloride). This product is intended for research and analytical applications. Isothipendyl hydrochloride (), an azaphenothiazine derivative, is a potent histamine 1 (H1) receptor antagonist.othipendyl is a primary metabolite .
|
-
- HY-B0548A
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
|
-
- HY-100660A
-
|
Drug Metabolite
|
Others
|
Cetirizine Impurity B dihydrochloride is an impurity of Cetirizine dihydrochloride. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
|
-
- HY-135740
-
-
- HY-100661
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Cetirizine Impurity D is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
|
-
- HY-B0303R
-
-
- HY-Z9101
-
|
Histamine Receptor
|
Neurological Disease
|
Promethazine sulfoxide is a metabolite of the histamine H1 receptor antagonist Promethazine (HY-B1296). It is formed from promethazine by the cytochrome P450 (CYP) isoform CYP2D6.
|
-
- HY-A0019
-
9-Hydroxyrisperidone
|
Drug Metabolite
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .
|
-
- HY-B1305R
-
|
Reference Standards
FAK
Histamine Receptor
VEGFR
|
Endocrinology
Cancer
|
Chloropyramine hydrochloride (Standard) is the analytical standard of Chloropyramine hydrochloride. This product is intended for research and analytical applications. Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.
|
-
- HY-119995
-
|
Apoptosis
Histamine Receptor
|
Cardiovascular Disease
Cancer
|
Chloropyramine is competitive reversible H1 receptor antagonist. Chloropyramine also has anti-tumour activity in breast cancer. Chloropyramine can be used for the research of allergic conditions, such as conjunctivitis and bronchial asthma .
|
-
- HY-12752
-
Trimeprazine
|
Histamine Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .
|
-
- HY-D0237R
-
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
|
Betahistine (mesylate) (Standard) is the analytical standard of Betahistine (mesylate). This product is intended for research and analytical applications. Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist . Betahistine mesylate is used for the study of rheumatoid arthritis (RA) .
|
-
- HY-B0524AR
-
-
- HY-B1794
-
-
- HY-B1317
-
Neohetramine
|
Histamine Receptor
|
Inflammation/Immunology
|
Thonzylamine is an orally active H1 histamine receptor antagonist with good antihistaminic and antianaphylactic properties. Thonzylamine can be used for the research of hypersensitivity diseases, nasal congestion, allergic conjunctivitis and other allergic diseases .
|
-
- HY-B1317A
-
Neohetramine hydrochloride
|
Histamine Receptor
|
Inflammation/Immunology
|
Thonzylamine hydrochloride is an orally active H1 histamine receptor antagonist with good antihistaminic and antianaphylactic properties. Thonzylamine hydrochloride can be used for the research of hypersensitivity diseases, nasal congestion, allergic conjunctivitis and other allergic diseases .
|
-
- HY-105014R
-
Norastemizole (Standard)
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
|
Tecastemizole (Standard) is the analytical standard of Tecastemizole. This product is intended for research and analytical applications. Tecastemizole (Norastemizole), a major metabolite of Astemizole, is a potent and selective H1 receptor antagonist. Tecastemizole shows anti-inflammatory activities .
|
-
- HY-N6772R
-
|
Reference Standards
Autophagy
|
Cancer
|
Antazoline (phosphate) (Standard) is the analytical standard of Antazoline (phosphate). This product is intended for research and analytical applications. Antazoline phosphate is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect .
|
-
- HY-107495
-
NSC19005
|
Histamine Receptor
|
Inflammation/Immunology
|
Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine . Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3 receptor antagonist used for the study of rheumatoid arthritis (RA) .
|
-
- HY-B0349R
-
Meclozine dihydrochloride (Standard)
|
Reference Standards
Histamine Receptor
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
Meclizine (dihydrochloride) (Standard) is the analytical standard of Meclizine (dihydrochloride). This product is intended for research and analytical applications. Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .
|
-
- HY-124626
-
|
Histamine Receptor
|
Inflammation/Immunology
|
(R)-(+)-Mequitazine is a histamine H1 receptor antagonist that mainly undergoes bio-transformation via human liver microsomes, resulting in hydroxylated and S-oxidized metabolites. (R)-(+)-Mequitazine competitively binds to the H1 receptors in gastrointestinal, vascular, and respiratory effect cells, thus blocking the endogenous activity of histamine. (R)-(+)-Mequitazine has an inhibitory effect on CYP3A-catalyzed midazolam 1’-hydroxylase. (R)-(+)-Mequitazine can be used in the study of various allergic diseases .
|
-
- HY-14447S1
-
-
- HY-B1397S
-
-
- HY-162231
-
|
Histamine Receptor
mAChR
|
Inflammation/Immunology
|
HY-078020 (compound III-4) is a selective, orally active antagonist for histamine H1 receptor with an IC50 of 24.12 nM. HY-078020 exhibits an anti-inflammatory effect in allergic diseases .
|
-
- HY-107559
-
|
Histamine Receptor
|
Neurological Disease
|
GT-2016 is a potent, selective, and brain penetrant histamine H3 receptor antagonist with a Ki of 43.8 nM. GT-2016 displays selectivity against H1 and H2 receptors, and has non-active against histamine methyltransferase .
|
-
- HY-164430
-
BU-E-50
|
Histamine Receptor
|
Cardiovascular Disease
|
Arpromidine (BU-E-50) is the agonist for histamine H2 receptor and the antagonist for histamine H1 receptor. Arpromidine exhibits positive inotropic effect with less risks in causing arrhythmias. Arpromidine can be used in research of congestive heart failure .
|
-
- HY-B0524AS1
-
-
- HY-17042AS
-
|
Isotope-Labeled Compounds
Histamine Receptor
|
Inflammation/Immunology
|
Cetirizine-d4 (dihydrochloride) is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
|
-
- HY-17042S1
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Cetirizine-d8 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
|
-
- HY-17042AS1
-
|
Isotope-Labeled Compounds
Histamine Receptor
|
Inflammation/Immunology
|
Cetirizine-d8 (dihydrochloride) is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
|
-
- HY-123205
-
-
- HY-101232
-
ICI 125211
|
Histamine Receptor
|
Cardiovascular Disease
|
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors .
|
-
- HY-B1794A
-
|
Dopamine Receptor
Histamine Receptor
Bacterial
Amyloid-β
|
Infection
Neurological Disease
|
Thiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects .
|
-
- HY-17042S
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Cetirizine-d4 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
|
-
- HY-12532
-
R 43512
|
Histamine Receptor
Potassium Channel
|
Inflammation/Immunology
Endocrinology
|
Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K + channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects .
|
-
- HY-17428R
-
|
Reference Standards
Histamine Receptor
Endogenous Metabolite
|
Inflammation/Immunology
Endocrinology
|
Tripelennamine (hydrochloride) (Standard) is the analytical standard of Tripelennamine (hydrochloride). This product is intended for research and analytical applications. Tripelennamine hydrochloride, an ethylenediamine derivative, is a potent histamine H1-receptor antagonist. Tripelennamine hydrochloride lessens the allergic response of the organism caused by histamine. Tripelennamine hydrochloride can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions .
|
-
- HY-B0640A
-
WAL801 hydrochloride
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action .
|
-
- HY-B0349S
-
-
- HY-B0478
-
AF-1161
|
5-HT Receptor
Serotonin Transporter
Histamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
Trazodone hydrochloride (AF-1161) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone hydrochloride has anti-depressant and anti-insomnious activity. Trazodone hydrochloride exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects .
|
-
- HY-14277AR
-
R 50547 hydrochloride (Standard)
|
Reference Standards
Histamine Receptor
Neurotensin Receptor
Integrin
|
Inflammation/Immunology
|
Levocabastine (hydrochloride) (Standard) is the analytical standard of Levocabastine (hydrochloride). This product is intended for research and analytical applications. Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) .
|
-
- HY-B0801S2
-
MDL-16455-d3; Terfenadine carboxylate-d3
|
Histamine Receptor
|
Inflammation/Immunology
|
Fexofenadine-d3 is the deuterium labeled Fexofenadine . Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research .
|
-
- HY-108411
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
|
-
- HY-121356
-
-
- HY-30234A
-
-
- HY-B0640
-
WAL801
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action .
|
-
- HY-B0548AS2
-
|
Isotope-Labeled Compounds
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Hydroxyzine-d8 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
|
-
- HY-B0548AS1
-
Vistaril-d4' dihydrochloride; Atarax-dd4' dihydrochloride
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Hydroxyzine-d4 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
|
-
- HY-17042R
-
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
Cancer
|
Cetirizine (Standard) is the analytical standard of Cetirizine. This product is intended for research and analytical applications. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
|
-
- HY-17042AR
-
P071 (Standard)
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
Cancer
|
Cetirizine (dihydrochloride) (Standard) is the analytical standard of Cetirizine (dihydrochloride). This product is intended for research and analytical applications. Cetirizine dihydrochloride, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine dihydrochloride marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
|
-
- HY-A0019S
-
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
Paliperidone-d4 is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .
|
-
- HY-B0478A
-
AF-1161 free base
|
5-HT Receptor
Serotonin Transporter
Histamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
Trazodone (AF-1161 free base) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone has anti-depressant and anti-insomnious activity. Trazodone exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects .
|
-
- HY-B0781S
-
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Promethazine-d4 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.
|
-
- HY-B0548R
-
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Hydroxyzine (Standard) is the analytical standard of Hydroxyzine. This product is intended for research and analytical applications. Hydroxyzine, a benzodiazepine antihistamine agent, acts as an orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine has anxiolytic effect and can be used for the research of generalised anxiety disorder .
|
-
- HY-30234
-
-
- HY-I0021
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Bepotastine is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
|
-
- HY-B0674S
-
-
- HY-107431
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Diphenylpyraline is a potent histamine H1 receptor antagonist. Diphenylpyraline acts as an orally active antihistamine agent with antimuscarinic and antiallergic effects. Diphenylpyraline can be used for the research of allergic diseases, including rhinitis and hay fever, and pruritic skin disorders et.al .
|
-
- HY-A0019R
-
9-Hydroxyrisperidone (Standard)
|
Drug Metabolite
Reference Standards
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
Paliperidone (Standard) is the analytical standard of Paliperidone. This product is intended for research and analytical applications. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .
|
-
- HY-107431R
-
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
|
Diphenylpyraline (Standard) is the analytical standard of Diphenylpyraline. This product is intended for research and analytical applications. Diphenylpyraline is a potent histamine H1?receptor antagonist. Diphenylpyraline acts as an orally active antihistamine agent?with antimuscarinic and antiallergic effects. Diphenylpyraline can be used for the research of allergic diseases, including rhinitis and hay fever, and pruritic skin disorders et.al .
|
-
- HY-167633
-
|
mGluR
Histamine Receptor
|
Neurological Disease
|
Oxomemazine hydrochloride is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine hydrochloride is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki= 84 nM, M1 receptor) and low (Ki= 1.65 μM, M2 receptor) affinity sites [1]. Oxomemazine hydrochloride an antihistamine and anticholinergic agent used for the study of cough treatment .
|
-
- HY-N1514R
-
|
Reference Standards
P-glycoprotein
|
Cancer
|
Doxylamine (succinate) (Standard) is the analytical standard of Doxylamine (succinate). This product is intended for research and analytical applications. Doxylamine (succinate), a first generation antihistamine, is a histamine (H1) receptor antagonist. Doxylamine is also a local analgesic agent and effective hypnotic agent .
|
-
- HY-B0801R
-
|
Histamine Receptor
|
Inflammation/Immunology
Cancer
|
Fexofenadine (Standard) is the analytical standard of Fexofenadine. This product is intended for research and analytical applications. Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research .
|
-
- HY-I0021A
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Bepotastine tosylate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine tosylate can suppress the expression of nerve growth factor (NGF). Bepotastine tosylate can be used in studies of allergic rhinitis, allergic conjunctivitis and urticaria/pruritus .
|
-
- HY-B2178
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
|
-
- HY-A0069R
-
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Doxylamine (succinate) (Standard) is the analytical standard of Doxylamine (succinate). This product is intended for research and analytical applications. Doxylamine (succinate), a first generation antihistamine, is a histamine (H1) receptor antagonist. Doxylamine is also a local analgesic agent and effective hypnotic agent .
|
-
- HY-B0801AR
-
MDL-16455 hydrochloride (Standard); Terfenadine carboxylate hydrochloride (Standard)
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
|
Fexofenadine (hydrochloride) (Standard) is the analytical standard of Fexofenadine (hydrochloride). This product is intended for research and analytical applications. Fexofenadine (MDL-16455) hydrochloride is an orally active and nonsedative H1 receptor antagonist. Fexofenadine hydrochloride can be used in allergic rhinitis and chronic idiopathic urticarial research .
|
-
- HY-B0548AR
-
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Hydroxyzine (dihydrochloride) (Standard) is the analytical standard of Hydroxyzine (dihydrochloride). This product is intended for research and analytical applications. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
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-
- HY-B1794R
-
|
Dopamine Receptor
Histamine Receptor
Bacterial
Amyloid-β
|
Infection
Neurological Disease
|
Thiethylperazine (Standard) is the analytical standard of Thiethylperazine. This product is intended for research and analytical applications. Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects .
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-
- HY-W062109
-
|
Endogenous Metabolite
Histamine Receptor
|
Inflammation/Immunology
|
Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis .
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-
- HY-A0015
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
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- HY-B0674R
-
LAS-W 090 (Standard); RP64305 (Standard)
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Ebastine (Standard) is the analytical standard of Ebastine. This product is intended for research and analytical applications. Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research .
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- HY-12532S
-
-
- HY-10791
-
-
- HY-B0801S4
-
MDL-16455-d3-1; Terfenadine carboxylate-d3-1
|
Histamine Receptor
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
Fexofenadine-d3-1 fumarate is deuterated labeled Fexofenadine (HY-B0801). Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research .
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-
- HY-B0674S1
-
-
- HY-123676
-
PNU-101387G mesylate; U-101387G mesylate
|
Dopamine Receptor
|
Neurological Disease
|
Sonepiprazole mesylate is a selective D4 dopamine antagonist with Kis of 3.6, 10.1, 5147, and 7430 nM for rD4-Dopamine, hD4.2-Dopamine, rD2-Dopamine, and Histamine-H1 receptors, respectively .
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-
- HY-12394
-
Dosulepin; Dothep
|
Histamine Receptor
5-HT Receptor
|
Neurological Disease
|
Dothiepin (Dosulepin; Dothep) is an antidepressant agent with sedative/anxiolytic activity. Dothiepin is an inhibitor preferring of noradrenaline uptake than serotonin uptake. Dothiepin facilitates noradrenergic neurotransmission via inhibiting the neuronal uptake. Dothiepin is also an antagonist of histamine H1-receptor without cardiotoxicity. Dothiepin exhibits significant analgesic activity in psychogenic facial pain,idiopathic fibromyalgia syndrome or rheumatoid arthritis .
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-
- HY-100661R
-
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Cetirizine Impurity D (Standard) is the analytical standard of Cetirizine Impurity D. This product is intended for research and analytical applications. Cetirizine Impurity D is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
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-
- HY-101232R
-
ICI 125211 (Standard)
|
Reference Standards
Histamine Receptor
|
Cardiovascular Disease
|
Tiotidine (Standard) is the analytical standard of Tiotidine. This product is intended for research and analytical applications. Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors .
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-
- HY-B0725S
-
|
Histamine Receptor
Cytochrome P450
|
Neurological Disease
|
Doxepin-d3 (hydrochloride) is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2 .
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-
- HY-136587
-
|
Histamine Receptor
mGluR
|
Inflammation/Immunology
|
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites. Oxomemazine is an antihistamine and anticholinergic agent used for the study of cough treatment. Oxomemazine is protective against anaphylactic microshock in guinea pigs .
|
-
- HY-12752BS
-
Trimeprazine-d6 hydrochloride
|
Histamine Receptor
Isotope-Labeled Compounds
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Alimemazine-d6 hydrochloride (Trimeprazine-d6 hydrochloride) is the deuterium labeled Alimemazine (HY-12752). Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .
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-
- HY-12532R
-
R 43512 (Standard)
|
Reference Standards
Histamine Receptor
Potassium Channel
|
Inflammation/Immunology
Endocrinology
|
Astemizole (Standard) is the analytical standard of Astemizole. This product is intended for research and analytical applications. Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K + channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects .
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-
- HY-B1317R
-
Neohetramine (Standard)
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
|
Thonzylamine (Standard) is the analytical standard of Thonzylamine. This product is intended for research and analytical applications. Thonzylamine is an orally active H1 histamine receptor antagonist, exhibits good antihistaminic and antianaphylactic properties. Thonzylamine can be used for the research of hypersensitivity diseases, nasal congestion, allergic conjunctivitis and other allergic diseases .
|
-
- HY-121356S
-
|
Isotope-Labeled Compounds
Histamine Receptor
|
Endocrinology
Cancer
|
Carebastine-d5 is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner . Carebastine suppresses the expression of macrophage migration inhibitory factor .
|
-
- HY-124517
-
|
Histamine Receptor
Adrenergic Receptor
|
Neurological Disease
Inflammation/Immunology
|
Burimamide is a blocker of histamine H2-receptor. Burimamide inhibits gastric acid secretion evoked by Pentagastrin (HY-A0261) or Gastrin. Burimamide also has alpha-adrenoceptor blocking activity. Burimamide in combination with the H1-receptor antagonist Mepyramine (HY-B1281) shows anti-inflammatory activity in a rat paw edema model induced by Compound 48/80 (HY-115768) .
|
-
- HY-B1794AR
-
|
Dopamine Receptor
Histamine Receptor
Bacterial
Amyloid-β
|
Infection
Neurological Disease
|
Thiethylperazine (dimaleate) (Standard) is the analytical standard of Thiethylperazine (dimaleate). This product is intended for research and analytical applications. Thiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects .
|
-
- HY-B0164A
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Mizolastine dihydrochloride is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine dihydrochloride effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine dihydrochloride can be used in studies of allergic rhinitis and chronic idiopathic urticarial .
|
-
- HY-121356S1
-
|
Isotope-Labeled Compounds
Histamine Receptor
|
Endocrinology
Cancer
|
Carebastine-d5 Methyl Ester is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner . Carebastine suppresses the expression of macrophage migration inhibitory factor .
|
-
- HY-B0164
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Mizolastine is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine can be used in studies of allergic rhinitis and chronic idiopathic urticarial .
|
-
- HY-147336
-
|
Drug Metabolite
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2 .
|
-
- HY-32329
-
Org-8282
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
|
-
- HY-B0478AR
-
AF-1161 free base (Standard)
|
Reference Standards
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
Serotonin Transporter
|
Neurological Disease
|
Trazodone (AF-1161 free base) (Standard) is the analytical standard of Trazodone. This product is intended for research and analytical applications. Trazodone is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone has anti-depressant and anti-insomnious activity. Trazodone exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects .
|
-
- HY-B1067
-
Phenazoline hydrochloride
|
Histamine Receptor
HBV
|
Neurological Disease
Endocrinology
|
Antazoline hydrochloride is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline hydrochloride can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline hydrochloride can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline hydrochloride has anti-arrhythmic effect in acute myocardial infarctions. Antazoline hydrochloride can be studied in research for cardiovascular diseases, and HBV .
|
-
- HY-B1193
-
-
- HY-B0640AR
-
WAL801 hydrochloride (Standard)
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Epinastine (hydrochloride) (Standard) is the analytical standard of Epinastine (hydrochloride). This product is intended for research and analytical applications. Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action .
|
-
- HY-108411R
-
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
|
Emedastine (Standard) is the analytical standard of Emedastine. This product is intended for research and analytical applications. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
|
-
- HY-14328
-
PNU-101387G; U-101387G
|
Dopamine Receptor
|
Neurological Disease
|
Sonepiprazole (PNU-101387G) is a selective D4 dopamine antagonist with Kis of 3.6, 10.1, 5147, and 7430 nM for rD4-Dopamine, hD4.2-Dopamine, rD2-Dopamine, and Histamine-H1 receptors, respectively .
|
-
- HY-14328A
-
PNU-101387G hydrochloride; U-101387G hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
Sonepiprazole (PNU-101387G) hydrochloride is a selective D4 dopamine antagonist with Kis of 3.6, 10.1, 5147, and 7430 nM for rD4-Dopamine, hD4.2-Dopamine, rD2-Dopamine, and Histamine-H1 receptors, respectively .
|
-
- HY-A0027A
-
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases .
|
-
- HY-A0027
-
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
Endocrinology
|
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases .
|
-
- HY-123205R
-
KW-4354 (Standard)
|
Reference Standards
Histamine Receptor
P2X Receptor
5-HT Receptor
Apoptosis
PERK
p38 MAPK
COX
|
Inflammation/Immunology
|
Oxatomide (Standard) (KW-4354 (Standard)) is the analytical standard of Oxatomide (HY-123205). This product is intended for research and analytical applications. Oxatomide (KW-4354) is an orally active dual antagonist of the H1-histamine receptor and the P2X7 receptor, as well as an inhibitor of serotonin. Oxatomide possesses antihistaminic, antiallergic and anti-inflammatory activities. Oxatomide can be used in the research of allergic diseases .
|
-
- HY-B0971
-
Prophenpyridamine maleate; Tripoton maleate; Pheniramine maleate
|
Histamine Receptor
Apoptosis
|
Inflammation/Immunology
Endocrinology
|
Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
|
-
- HY-W062109S
-
|
Histamine Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
Olopatadine-d6 is the deuterium labeled Olopatadine . Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis .
|
-
- HY-B0971A
-
Prophenpyridamine; Tripoton; Pheniramine solution
|
Histamine Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
|
-
- HY-108411S
-
|
Isotope-Labeled Compounds
Histamine Receptor
|
Inflammation/Immunology
|
Emedastine- 13C,d3 fumarate is the 13C- and deuterium labeled Emedastine. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
|
-
- HY-I0021R
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Bepotastine (Standard) is the analytical standard of Bepotastine. This product is intended for research and analytical applications. Bepotastine is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
|
-
- HY-32329A
-
MO-8282
|
5-HT Receptor
|
Neurological Disease
|
Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
|
-
- HY-165378
-
(E)-Dosulepin hydrochloride; (E)-Dothep hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
(E)-Dothiepin ((E)-Dosulepin;(E)-Dothep) hydrochloride is an antidepressant agent with sedative/anxiolytic activity. (E)-Dothiepin hydrochloride is an inhibitor preferring of noradrenaline uptake than serotonin uptake. (E)-Dothiepin hydrochloride facilitates noradrenergic neurotransmission via inhibiting the neuronal uptake. (E)-Dothiepin hydrochloride is also an antagonist of histamine H1-receptor without cardiotoxicity. (E)-Dothiepin hydrochloride exhibits significant analgesic activity in psychogenic facial pain,idiopathic fibromyalgia syndrome or rheumatoid arthritis .
|
-
- HY-10791R
-
|
5-HT Receptor
Histamine Receptor
Dopamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
Ritanserin (Standard) is the analytical standard of Ritanserin. This product is intended for research and analytical applications. Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors .
|
-
- HY-A0015S
-
|
Isotope-Labeled Compounds
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Bepotastine-d6(besylate) is deuterium labeled Bepotastine (besilate). Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
|
-
- HY-B2178R
-
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
|
Emedastine (difumarate) (Standard) is the analytical standard of Emedastine (difumarate). This product is intended for research and analytical applications. Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
|
-
- HY-B0640S
-
WAL801-13C,d3 hydrobromide
|
Isotope-Labeled Compounds
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Epinastine- 13C,d3 (hydrobromide) is the 13C- and deuterium labeled Epinastine. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action .
|
-
- HY-136587R
-
|
Reference Standards
Histamine Receptor
mGluR
|
Inflammation/Immunology
|
Oxomemazine (Standard) is the analytical standard of Oxomemazine (HY-136587). This product is intended for research and analytical applications. Oxomemazine is a phenothiazine-based histamine H1-receptor blocker. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites. Oxomemazine is an antihistamine and anticholinergic agent used for the study of cough treatment. Oxomemazine is protective against anaphylactic microshock in guinea pigs .
|
-
- HY-A0015R
-
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Bepotastine (besilate) (Standard) is the analytical standard of Bepotastine (besilate). This product is intended for research and analytical applications. Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
|
-
- HY-A0027AS
-
|
Isotope-Labeled Compounds
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Fenspiride-d5 is the deuterium labeled Fenspiride. Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases .
|
-
- HY-A0027R
-
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
Endocrinology
|
Fenspiride (hydrochloride) (Standard) is the analytical standard of Fenspiride (hydrochloride). This product is intended for research and analytical applications. Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases .
|
-
- HY-107647
-
|
mAChR
Histamine Receptor
|
Inflammation/Immunology
|
(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48) .
|
-
- HY-B1067R
-
Phenazoline hydrochloride (Standard)
|
Reference Standards
Histamine Receptor
HBV
|
Neurological Disease
Endocrinology
|
Antazoline (hydrochloride) (Standard) is the analytical standard of Antazoline (hydrochloride). This product is intended for research and analytical applications. Antazoline hydrochloride is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline hydrochloride can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline hydrochloride can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline hydrochloride has anti-arrhythmic effect in acute myocardial infarctions. Antazoline hydrochloride can be studied in research for cardiovascular diseases, and HBV .
|
-
- HY-32329S
-
|
Isotope-Labeled Compounds
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
Setiptiline-d3 is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
|
-
- HY-32329R
-
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
Setiptiline (Standard) is the analytical standard of Setiptiline. This product is intended for research and analytical applications. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
|
-
- HY-A0015A
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
(Rac)-Bepotastine (besilate) is the isomer of Bepotastine (besilate) (HY-A0015), and can be used as an experimental control. Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
|
-
- HY-B0164R
-
|
Reference Standards
Histamine Receptor
|
Inflammation/Immunology
|
Mizolastine (Standard) is the analytical standard of Mizolastine. This product is intended for research and analytical applications. Mizolastine is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine can be used in studies of allergic rhinitis and chronic idiopathic urticarial .
|
-
- HY-B0352
-
-
- HY-B1193S
-
-
- HY-B1193R
-
-
- HY-103093
-
|
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
Dopamine Receptor
|
Neurological Disease
|
Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo .
|
-
- HY-32329AR
-
|
5-HT Receptor
|
Neurological Disease
|
Setiptiline (maleate) (Standard) is the analytical standard of Setiptiline (maleate). This product is intended for research and analytical applications. Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
|
-
- HY-B0480A
-
-
- HY-B0971R
-
Prophenpyridamine maleate (Standard); Tripoton maleate (Standard); Pheniramine maleate (Standard)
|
Reference Standards
Histamine Receptor
Apoptosis
|
Inflammation/Immunology
Endocrinology
|
Pheniramine (maleate) (Standard) is the analytical standard of Pheniramine (maleate). This product is intended for research and analytical applications. Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
|
-
- HY-N7814R
-
|
Reference Standards
Endogenous Metabolite
|
Others
|
Pheniramine (maleate) (Standard) is the analytical standard of Pheniramine (maleate). This product is intended for research and analytical applications. Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
|
-
- HY-B0971AR
-
Prophenpyridamine (Standard); Tripoton (Standard); Pheniramine solution (Standard)
|
Reference Standards
Histamine Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
Pheniramine (Standard) is the analytical standard of Pheniramine. This product is intended for research and analytical applications. Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
|
-
- HY-19443
-
|
Histamine Receptor
Lipoxygenase
|
Inflammation/Immunology
|
UCB-35440 is an orally active histamine H1 receptor antagonist and 5-lipoxygenase inhibitor. UCB-35440 inhibits LTB4 formation in human whole blood and reduces polymorphonuclear cell infiltration in mouse models. UCB-35440 inhibits histamine-stimulated bronchoconstriction and reduces skin inflammation in guinea pigs. UCB-35440 can be used for research on asthma and skin inflammation .
|
-
- HY-121311
-
|
Serotonin Transporter
Adrenergic Receptor
|
Cardiovascular Disease
|
Metrenperone is an inhibitor for 5-HT2 receptor. Metrenperone exhibits α1 and α2 antagonist activity as well as anti-H1 and anti-dopaminergic efficacy. Metrenperone can lower the blood pressure, enhances bradycardia in peripheral ischemia, inhibits serotonin-induced platelet aggregation, and antagonizes serotonin-mediated vasoconstriction. Metrenperone promotes the repair of acutely damaged collagen tissue .
|
-
- HY-B0480
-
(±)-Brompheniramine maleate
|
Histamine Receptor
mAChR
Potassium Channel
Sodium Channel
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research .
|
-
- HY-B0352S2
-
-
- HY-B0352S3
-
-
- HY-B0352R
-
-
- HY-103093R
-
|
Reference Standards
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
Dopamine Receptor
|
Neurological Disease
|
Zotepine (Standard) is the analytical standard of Zotepine. This product is intended for research and analytical applications. Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo .
|
-
- HY-B0539
-
Desloratadine
Maximum Cited Publications
10 Publications Verification
Sch34117
|
Histamine Receptor
TNF Receptor
Leukotriene Receptor
|
Inflammation/Immunology
|
Desloratadine (Sch34117) is an orally active and selective H1 receptor antagonist (Ki=0.9 nM) with anti-inflammatory and anti-allergic activities. Desloratadine inhibits the release of histamine and LTC4 from human basophils and targets the regulatory signals of IL-4 and IL-13 production in basophils. Desloratadine significantly alleviates SAR symptoms in patients with concurrent asthma and can be used in the study of seasonal allergic rhinitis and chronic idiopathic urticaria .
|
-
- HY-W744038
-
|
Isotope-Labeled Compounds
Dopamine Receptor
Histamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
Zotepine-d6 is the deuterium labeled Zotepine (HY-103093). Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo .
|
-
- HY-B0480AR
-
(±)-Brompheniramine (Standard)
|
Reference Standards
Histamine Receptor
mAChR
Potassium Channel
Sodium Channel
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
Brompheniramine (Standard) is the analytical standard of Brompheniramine. This product is intended for research and analytical applications. Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research [4].
|
-
- HY-B0480R
-
(±)-Brompheniramine maleate (Standard)
|
Reference Standards
Histamine Receptor
mAChR
Potassium Channel
Sodium Channel
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
Brompheniramine (maleate) (Standard) is the analytical standard of Brompheniramine (maleate). This product is intended for research and analytical applications. Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research .
|
-
- HY-101094
-
R79598
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.
|
-
- HY-B0725
-
|
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Cancer
|
Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2 . Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant .. Doxepin has therapeutic effects in atopic dermatitis,chronic urticarial,can improve cognitive processes, protect central nervous system .. Doxepin has also been proposed as a protective factor against oxidative stress ..
|
-
- HY-148825
-
-
- HY-14541A
-
LY170053 hydrochloride
|
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
Olanzapine hydrochloride is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine hydrochloride is an atypical antipsychotic .
|
-
- HY-14541
-
LY170053
|
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
- HY-163101
-
|
Platelet-activating Factor Receptor (PAFR)
Leukotriene Receptor
|
Inflammation/Immunology
|
CP-96021 is a potent and orally available leukotriene D4 (LTD4 Ki=34 μM) / platelet activating factor (PAF Ki=37 μM) receptor antagonist. CP-96021 has antagonist capable of simultaneously targeting two different inflammatory mediators, LTD4 and PAF. CP-96021 shows high specificity for α1, α2, β, dopamine-2, adenosine 1, 5-HT1, H1, muscarine, μ opioid, and GABA receptors, all expressing IC50 values greater than 10 μM. CP-96021 can be used to study the pathogenesis of many inflammatory diseases such as asthma .
|
-
- HY-14541S
-
LY170053-d3
|
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
- HY-B1101
-
Pimetixene
|
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
|
-
- HY-B1101A
-
Pimetixene maleate
|
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
|
-
- HY-14541R
-
LY170053 (Standard)
|
Reference Standards
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
- HY-B0725R
-
|
Reference Standards
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Cancer
|
Doxepin (Hydrochloride) (Standard) is the analytical standard of Doxepin (Hydrochloride). This product is intended for research and analytical applications. Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2 . Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant .. Doxepin has therapeutic effects in atopic dermatitis,chronic urticarial,can improve cognitive processes, protect central nervous system .. Doxepin has also been proposed as a protective factor against oxidative stress ..
|
-
- HY-14541S2
-
LY170053-d8
|
Isotope-Labeled Compounds
Apoptosis
Dopamine Receptor
Autophagy
mAChR
Mitophagy
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
- HY-103109
-
|
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
|
Neurological Disease
|
Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .
|
-
- HY-10564
-
MCI-9042
|
5-HT Receptor
|
Cardiovascular Disease
|
Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
|
-
- HY-B2169
-
|
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
|
Neurological Disease
|
Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly .
|
-
- HY-117046
-
|
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
AVN-101 is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis .
|
-
- HY-117046A
-
|
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis .
|
-
- HY-B1101AR
-
Pimetixene maleate (Standard)
|
Reference Standards
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Pimethixene maleate (Standard) is the analytical standard of Pimethixene maleate. This product is intended for research and analytical applications. Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
|
-
- HY-10564R
-
MCI-9042 (Standard)
|
Reference Standards
5-HT Receptor
|
Cardiovascular Disease
|
Sarpogrelate (hydrochloride) (Standard) is the analytical standard of Sarpogrelate (hydrochloride). This product is intended for research and analytical applications. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
|
-
- HY-B2169R
-
|
5-HT Receptor
Reference Standards
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
|
Neurological Disease
|
Melperone (Standard) is the analytical standard of Melperone (HY-B2169). This product is intended for research and analytical applications. Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.
|
-
- HY-B2169S2
-
|
Isotope-Labeled Compounds
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
|
Neurological Disease
|
Melperone-d4 hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109) . Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .
|
-
- HY-10564S
-
MCI-9042-d3
|
Isotope-Labeled Compounds
5-HT Receptor
|
Cardiovascular Disease
|
Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
|
-
- HY-10564S1
-
MCI-9042-d4
|
Isotope-Labeled Compounds
5-HT Receptor
|
Cardiovascular Disease
|
Sarpogrelate-d4 (MCI-9042-d4) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
|
-
- HY-101179
-
-
- HY-111501
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R .
|
-
- HY-101179R
-
-
- HY-167886
-
|
Angiotensin Receptor
|
Cardiovascular Disease
|
GA 0113 is a potent and orally active angiotensin II (Ang II) AT1-receptor antagonist. GA 0113 inhibits the Ang II (HY-13948)-induced pressor response with ID50 of 0.032 mg/kg and dose-dependently increases plasma renin activity for 48 h .
|
-
- HY-103149
-
SB-216641 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
SB-216641A (SB-216641 hydrochloride) is a selective antagonist of 5-HT1B/D receptor. SB-216641A shows high affinity and selectivity for h5-HT1B receptors over h5-HT1D receptors. SB-216641A inhibits the function of SKF-99101H .
|
-
- HY-12882
-
NP-120; RC-61-91
|
iGluR
Adrenergic Receptor
Potassium Channel
Calcium Channel
Influenza Virus
|
Infection
Neurological Disease
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Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
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- HY-12882A
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NP-120 tartrate; RC-61-91 tartrate
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iGluR
Adrenergic Receptor
Potassium Channel
Calcium Channel
Influenza Virus
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Infection
Neurological Disease
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Ifenprodil (NP-120) tartrate, a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate is an α1 adrenergic receptor antagonist. Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil tartrate has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil tartrate can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0548S1
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Hydroxyzine-d8 is deuterium labeled Hydroxyzine. Hydroxyzine is a histamine H1-receptor antagonist .
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- HY-19489S
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(±)-Levomepromazine-d6 is the deuterium labeled Methotrimeprazine, which is a D3 dopamine and Histamine H1 receptor antagonist.
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- HY-B0539S3
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Desloratadine-d5 is deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities .
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- HY-B0539S1
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Desloratadine-d9 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities .
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- HY-B0539S
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Desloratadine-d4 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
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- HY-B1589AS
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Carbinoxamine-d6 (maleate) is the deuterium labeled Carbinoxamine maleate salt. Carbinoxamine maleate salt is a histamine H1 receptor antagonist.
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- HY-B0539S4
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Desloratadine-d4 hydrobromide is deuterated labeled Desloratadine (HY-B0539). Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities .
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- HY-B0814S
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Levocetirizine-d4 (dihydrochloride) is the deuterium labeled Levocetirizine. Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].
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- HY-B0539S2
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Desloratadine-3,3,5,5-d4 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
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- HY-B0548AS
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Hydroxyzine-d4 (dihydrochloride) is deuterium labeled Hydroxyzine. Hydroxyzine is a heterocyclic histamine H1-receptor antagonist. Hydroxyzine has anticholinergic, anxiolytic and analgesic properties .
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- HY-B0781S1
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Promethazine-d3 (hydrochloride) is deuterium labeled Promethazine (hydrochloride). Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
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- HY-B1296S1
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Promethazine-d4 is a deuterated-labeled promethazine (HY-B0781). Promethazine is an orally active H1 receptor and mAChR antagonist with antihistamine (H1), sedative, antiemetic, anticholinergic, and anti-motion sickness properties .
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- HY-B0814S1
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Levocetirizine-d4 ((R)-Cetirizine-d4) is the deuterium-labeled Levocetirizine (HY-B0814) . Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
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- HY-30234S
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Clemizole-d4 is a deuterium labeled Clemizole. Clemizole is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication .
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- HY-B0298AS
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1 Publications Verification
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Clemastine-d5 (fumarate) is the deuterium labeled Clemastine fumarate. Clemastine fumarate (HS-592 fumarate) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
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- HY-14447S
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Bilastine-d6 is the deuterium labeled Bilastine. Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria .
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- HY-B0303AS1
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Diphenhydramine-d5 (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
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- HY-B0303AS
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Diphenhydramine-d6 (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
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- HY-B0524AS
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Betahistine-d3 (dihydrochloride) is the deuterium labeled Betahistine dihydrochloride. Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist . Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA) .
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- HY-14447S1
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Bilastine-d4 is deuterium labeled Bilastine. Bilastine is an oral histamine H1-receptor antagonist. Bilastine can be used for allergic rhinitis and urticaria studies, and it also improves diabetic nephropathy in mice, showing safety for the central nervous system .
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- HY-B1397S
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Cyclizine-d3 is deuterium labeled Cyclizine. Cyclizine, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine can be used for the research of nausea, vomiting, and dizziness .
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- HY-B0524AS1
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Betahistine- 13C,d3 (dihydrochloride) is the 13C- and deuterium labeled Betahistine (dihydrochloride). Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist . Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA) .
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- HY-17042AS
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Cetirizine-d4 (dihydrochloride) is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
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- HY-17042S1
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Cetirizine-d8 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
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- HY-17042AS1
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Cetirizine-d8 (dihydrochloride) is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
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- HY-17042S
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Cetirizine-d4 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
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- HY-B0349S
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Meclizine-d8 is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .
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- HY-B0801S2
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Fexofenadine-d3 is the deuterium labeled Fexofenadine . Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research .
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- HY-B0548AS2
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Hydroxyzine-d8 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
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- HY-B0548AS1
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Hydroxyzine-d4 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
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- HY-A0019S
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Paliperidone-d4 is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .
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- HY-B0781S
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Promethazine-d4 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.
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- HY-B0674S
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Ebastine-d5 is the deuterium labeled Ebastine. Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research .
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- HY-12532S
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Astemizole-d3 is the deuterium labeled Astemizole. Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects .
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- HY-B0801S4
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Fexofenadine-d3-1 fumarate is deuterated labeled Fexofenadine (HY-B0801). Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research .
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- HY-B0674S1
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Ebastine-d6 is deuterated labeled Ebastine (HY-B0674). Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research .
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- HY-B0725S
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Doxepin-d3 (hydrochloride) is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2 .
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- HY-12752BS
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Alimemazine-d6 hydrochloride (Trimeprazine-d6 hydrochloride) is the deuterium labeled Alimemazine (HY-12752). Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .
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- HY-121356S
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Carebastine-d5 is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner . Carebastine suppresses the expression of macrophage migration inhibitory factor .
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- HY-121356S1
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Carebastine-d5 Methyl Ester is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner . Carebastine suppresses the expression of macrophage migration inhibitory factor .
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- HY-W062109S
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Olopatadine-d6 is the deuterium labeled Olopatadine . Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis .
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- HY-108411S
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Emedastine- 13C,d3 fumarate is the 13C- and deuterium labeled Emedastine. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
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- HY-A0015S
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Bepotastine-d6(besylate) is deuterium labeled Bepotastine (besilate). Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
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- HY-B0640S
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Epinastine- 13C,d3 (hydrobromide) is the 13C- and deuterium labeled Epinastine. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action .
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- HY-A0027AS
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Fenspiride-d5 is the deuterium labeled Fenspiride. Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases .
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- HY-32329S
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Setiptiline-d3 is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
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- HY-B1193S
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Terfenadine-d3 ((±)-Terfenadine-d3) is the deuterium labeled Terfenadine. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM . Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].
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- HY-B0352S2
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Mirtazapine-d4 is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively .
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- HY-B0352S3
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Mirtazapine-d4 hydrochloride is deuterated labeled Mirtazapine (HY-B0352). Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively .
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- HY-W744038
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Zotepine-d6 is the deuterium labeled Zotepine (HY-103093). Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo .
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- HY-14541S
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Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic .
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- HY-14541S2
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Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
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- HY-B2169S2
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Melperone-d4 hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109) . Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .
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- HY-10564S
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Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
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- HY-10564S1
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Sarpogrelate-d4 (MCI-9042-d4) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
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