2. Signaling Pathways
  3. GPCR/G Protein
    Immunology/Inflammation
    Neuronal Signaling
  4. Histamine Receptor

Histamine Receptor

Histamine Receptor

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Histamine Receptors are a class of G protein-coupled receptors with histamine as their endogenous ligand. There are four known histamine receptors: H1 receptor, H2 receptor, H3 receptor, H4 receptor. The H1 receptor is a histamine receptor belonging to the family of Rhodopsin-like G-protein-coupled receptors. This receptor, which is activated by the biogenic amine histamine, is expressed throughout the body, to be specific, in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of Protein Kinase A. Histamine H3 receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act asautoreceptors in presynaptic histaminergic neurons, and also control histamine turnover by feedback inhibition of histamine synthesis and release. The Histamine H4 receptor has been shown to be involved in mediating eosinophil shape change and mast cell chemotaxis.

Histamine Receptor Isoform Specific Products:

Histamine Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-135495
    AM-0466
    		Inhibitor
    AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing.
    AM-0466
  • HY-138110R
    Toladryl (Standard)
    		Antagonist
    Toladryl (Standard) is the analytical standard of Toladryl. This product is intended for research and analytical applications. Toladryl is a derivative of Diphenhydramine (HY-B0303), capable of penetrating the blood-brain barrier and possessing oral activity, as well as antihistamine and anticholinergic activities. The anticholinergic activity of Toladryl is approximately one-tenth that of Diphenhydramine (HY-B0303), and its protective effect against lethal doses of histamine in guinea pigs is 2 to 4 times that of Diphenhydramine (HY-B0303). The side effects of Toladryl are fewer and milder than those of Diphenhydramine (HY-B0303), but at higher doses, it may cause central nervous system symptoms such as insomnia, agitation, and disorientation. Toladryl can be used for research in allergic diseases.
    Toladryl (Standard)
  • HY-155297
    Nebidrazine
    Nebidrazine is a centrally-acting hypotensive agent compared to clonidine, demonstrating weaker cardiovascular effects in rats. It induces dose-dependent hypotension and bradycardia when administered intracerebroventricularly (i.c.v.), with significantly lower sedative potential than clonidine in conscious rats. Yohimbine attenuates the cardiovascular effects of both Nebidrazine and clonidine, suggesting involvement of central alpha-autoreceptors sensitive to yohimbine. Unlike clonidine, Nebidrazine does not affect peripheral alpha-adrenoceptors in pithed rats, indicating a selective central mechanism. Chemical sympathectomy reduces Nebidrazine's cardiovascular effects more than clonidine's, and metiamide diminishes responses to both drugs, implicating central histamine receptors. These findings highlight Nebidrazine's distinct pharmacological profile and potential therapeutic application in managing hypertension through central alpha-autoreceptor stimulation.
    Nebidrazine
  • HY-121406
    (Z)-Lafutidine
    		Antagonist
    (Z)-Lafutidine ((Z)-FRG-8813) is a potent histamine H2 receptor antagonist. (Z)-Lafutidine shows anti-secretory and gastroprotective activities.
    (Z)-Lafutidine
  • HY-116120
    N-Acetyldesloratadine
    		Antagonist 99.93%
    N-Acetyldesloratadine (SCH-37370) is a potent, orally active dual antagonist of platelet-activating factor (PAF) and histamine. N-Acetyldesloratadine inhibits PAF-induced aggregation of human platelets, with an IC50 of 0.6 µM. N-Acetyldesloratadine can be used for the study of allergic diseases, such as asthma.
    N-Acetyldesloratadine
  • HY-107495
    Betahistine EP Impurity C
    		Modulator 98.38%
    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).
    Betahistine EP Impurity C
  • HY-B0801AS
    Fexofenadine-d10 hydrochloride
    		Inhibitor
    Fexofenadine-d10 (hydrochloride) is deuterium labeled Fexofenadine (hydrochloride). Fexofenadine hydrochloride (MDL-16455 hydrochloride), a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial (person aged ≥16 years).
    Fexofenadine-d<sub>10</sub> hydrochloride
  • HY-108977
    VUF 8430
    		Agonist
    VUF 8430 is a potent and selective histamine H4 receptor agonist with a Ki of 31.6 nM and an EC50 of 50 nM.
    VUF 8430
  • HY-B0349S
    Meclizine-d8
    		Antagonist
    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.
    Meclizine-d<sub>8</sub>
  • HY-A0015S
    Bepotastine-d6 besylate
    		Antagonist
    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.
    Bepotastine-d<sub>6</sub> besylate
  • HY-17042B
    (S)-Cetirizine dihydrochloride
    		Antagonist
    (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.
    (S)-Cetirizine dihydrochloride
  • HY-B0801S3
    Fexofenadine-d10
    Fexofenadine-d10 is deuterium labeled Fexofenadine.
    Fexofenadine-d<sub>10</sub>
  • HY-W062109
    Olopatadine
    		Antagonist 98.94%
    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.
    Olopatadine
  • HY-W580721
    4-Methylhistamine
    		Agonist
    4-Methylhistamine is a potent agonist of histamine 4 receptor (H4R). 4-Methylhistamine has the potential for the research of immune-related diseases such as cancer and autoimmune disorders.
    4-Methylhistamine
  • HY-A0129R
    Histamine phosphate (Standard)
    		Agonist
    Histamine phosphate (Standard) is the analytical standard of Histamine phosphate (HY-A0129). This product is intended for research and analytical applications. Histamine phosphate is the agonist for histamine receptor and a vasodilator. Histamine phosphate is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine phosphate affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine phosphate can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.
    Histamine phosphate (Standard)
  • HY-B1067R
    Antazoline hydrochloride (Standard)
    		Inhibitor
    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.
    Antazoline hydrochloride (Standard)
  • HY-B1589AS
    Carbinoxamine-d6 maleate
    		Antagonist
    Carbinoxamine-d6 (maleate) is the deuterium labeled Carbinoxamine maleate salt. Carbinoxamine maleate salt is a histamine H1 receptor antagonist.
    Carbinoxamine-d<sub>6</sub> maleate
  • HY-B0426AS1
    (Z)-Olopatadine-d3 hydrochloride
    		Inhibitor
    (Z)-Olopatadine-d3 (hydrochloride) is deuterium labeled Olopatadine (hydrochloride).
    (Z)-Olopatadine-d<sub>3</sub> hydrochloride
  • HY-121364
    Bodilisant
    Bodilisant is a fluorescent histamine H3 receptor ligand. Bodilisant can be used at low concentrations (1-10 nM) to detect the performance of hH3R in cells overexpressing hH3R, and at about 1 μM concentration for tissues rich in hH3R. Bodilisant is a useful pharmacological tool for receptor imaging.
    Bodilisant
  • HY-14939A
    Vapitadine hydrochloride
    		Antagonist
    Vapitadine hydrochloride (Compound 3a) is a selective, orally active and nonsedating antihistamine agent, which exhibits a good binding affinity with human cloned histamine H1 receptor with a Ki of 19 nM. Vapitadine hydrochloride decreases the histamine-induced lethality (ED50 is 0.056-1.2 mg/kg), antagonizes the cutaneous reactions to histamine (ED50 is 0.51-1.4 mg/kg) in rats.
    Vapitadine hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

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