Search Result
Results for "
alpha 2 adrenergic receptor
" in MedChemExpress (MCE) Product Catalog:
15
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B0659
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- HY-B0659A
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- HY-W702712
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- HY-17034BS
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- HY-116222
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Fluorescent Dye
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Endocrinology
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A 53693 is a rigid catecholamine with selective adrenergic agonist activity. A 53693 has affinity for certain rat alpha-2 receptor subtypes. A 53693 shows high selectivity for alpha-2 receptors and, in contrast, has low affinity for alpha-1 receptors. A 53693 is used as a probe in biological studies to explore the molecular interactions of alpha agonist compounds .
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- HY-103208
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Adrenergic Receptor
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Metabolic Disease
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Benalfocin is a novel selective alpha-2 adrenergic receptor antagonist. Benalfocin reduces blood pressure and heart rate. Benalfocin can be used in the study of cardiovascular effects .
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- HY-W042920A
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Adrenergic Receptor
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Neurological Disease
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TDIQ hydrochloride is an analog of Amphetamine with high affinity for α2-adrenergic receptor. TDIQ hydrochloride is a selective α2-adrenoceptor ligand with the Ki values of 75 nM, 95 nM, and 65 nM for α2A-, α2B-, and α2C-adrenergic receptors, respectively .
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- HY-19057
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MK-467; L-659066
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Adrenergic Receptor
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Cardiovascular Disease
Neurological Disease
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Vatinoxan (MK-467) is an alpha 2-adrenergic receptor antagonist. The peripheral selectivity of Vatinoxan determines that it has limited penetration across the blood-brain barrier and therefore has low concentrations in the central nervous system. Vatinoxan antagonizes alpha 2-adrenergic receptor receptors by binding to them, thereby reducing or preventing cardiovascular effects caused by α2-adrenergic agonists. Vatinoxan can be used in studies of cardiovascular effects, sedation and analgesia .
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- HY-B0659S
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- HY-107358A
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WHR-1142A
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Adrenergic Receptor
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Others
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Lidamidine hydrochloride (WHR-1142A) is an α2-adrenergic receptor agonist and antidiarrheal agent .
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- HY-B0194A
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- HY-U00402
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- HY-101610
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- HY-105960
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- HY-105960A
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- HY-103212B
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B-HT 933
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Adrenergic Receptor
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Neurological Disease
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Azepexole (B-HT 933) is a selective α2 adrenergic inducer with over 300-fold selectivity for α2 adrenergic receptors over α1 adrenergic receptors. Azepexole can be used to study the biological functions of α2 adrenergic receptors and inhibition of related diseases. Azepexole may also play a role in regulating mood and improving cognitive function .
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- HY-B0659R
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UK 14304 (Standard); AGN190342 (Standard)
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Reference Standards
Adrenergic Receptor
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Endocrinology
Cancer
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Brimonidine (Standard) is the analytical standard of Brimonidine. This product is intended for research and analytical applications. Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
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- HY-107358
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- HY-U00371
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- HY-106444A
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MPV-1730 hydrochloride; JP-1730 hydrochloride
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Adrenergic Receptor
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Neurological Disease
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Fipamezole hydrochloride is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole hydrochloride is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease .
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- HY-B0225B
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L-(-)-α-Methyldopa hydrate; MK-351 hydrate
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Adrenergic Receptor
Endogenous Metabolite
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Cardiovascular Disease
Endocrinology
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Methyldopa hydrate (L-(-)-α-Methyldopa hydrate), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrate is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system .
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- HY-B0225A
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L-(-)-α-Methyldopa hydrochloride; MK-351 hydrochloride
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Adrenergic Receptor
Endogenous Metabolite
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Cardiovascular Disease
Endocrinology
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Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system .
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- HY-B0225
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- HY-106617A
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5-HT Receptor
Adrenergic Receptor
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Neurological Disease
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Etoperidone hydrochloride, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone hydrochloride shows Kd values of 36 nM, 38 nM, 85 nM, and 570 nM for 5-HT2 receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively .
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- HY-106617
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5-HT Receptor
Adrenergic Receptor
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Neurological Disease
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Etoperidone, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone shows Kd values of 36 nM, 38 nM, 85 nM, and 570 nM for 5-HT2 receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively .
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- HY-106444
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MPV 1730; JP-1730
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Adrenergic Receptor
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Neurological Disease
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Fipamezole (MPV 1730; JP-1730) is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease .
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- HY-B0659AR
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UK 14304 tartrate (Standard); AGN190342 tartrate (Standard)
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Reference Standards
Adrenergic Receptor
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Endocrinology
Cancer
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Brimonidine (tartrate) (Standard) is the analytical standard of Brimonidine (tartrate). This product is intended for research and analytical applications. Brimonidine tartrate (UK 14304 tartrate) is a full α2-adrenergic receptor (α2-AR) agonist.
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- HY-129697
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3-OH Medetomidine; Medetomidine metabolite MIII
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Drug Metabolite
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Metabolic Disease
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3-Hydroxy Medetomidine (3-OH Medetomidine; Medetomidine metabolite MIII) is a metabolite of the α2-adrenergic receptor agonist medetomidine.
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- HY-B1696
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Adrenergic Receptor
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Cardiovascular Disease
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Methyldopate is an ethyl ester proagent of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate has the potential for severe hypertension research .
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- HY-B1696A
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Adrenergic Receptor
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Cardiovascular Disease
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Methyldopate hydrochloride is an ethyl ester hydrochloride proagent of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate hydrochloride has the potential for severe hypertension research .
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- HY-103413
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Dopamine Receptor
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Neurological Disease
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Eticlopride hydrochloride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1‐adrenergic, α2‐adrenergic, 5HT1, 5HT2 receptors with Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. Eticlopride hydrochloride is an antipsychotic agent .
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- HY-121129
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FLB-131
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Dopamine Receptor
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Neurological Disease
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Eticlopride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1‐adrenergic, α2‐adrenergic, 5HT1, 5HT2 receptors with Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. Eticlopride is an antipsychotic agent .
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- HY-112074
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HOE 440
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Adrenergic Receptor
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Cardiovascular Disease
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Tiamenidine (HOE 440) is an orally active α2-adrenergic receptor agonist with antihypertensive effect. Tiamenidine is used as an antihypertensive agent for hypertension research .
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- HY-B0225AS
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L-(-)-α-Methyldopa-d3 hydrochloride; MK-351-d3 hydrochloride
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Isotope-Labeled Compounds
Adrenergic Receptor
Endogenous Metabolite
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Cardiovascular Disease
Endocrinology
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Methyldopa-d3 (hydrochloride) is deuterium labeled Methyldopa (hydrochloride). Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system .
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- HY-U00117
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- HY-B0225BR
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L-(-)-α-Methyldopa hydrate (Standard); MK-351 hydrate (Standard)
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Reference Standards
Adrenergic Receptor
Endogenous Metabolite
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Cardiovascular Disease
Endocrinology
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Methyldopa (hydrate) (Standard) is the analytical standard of Methyldopa (hydrate). This product is intended for research and analytical applications. Methyldopa hydrate (L-(-)-α-Methyldopa hydrate), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrate is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system .
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- HY-B0225R
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Adrenergic Receptor
Endogenous Metabolite
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Cardiovascular Disease
Endocrinology
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Methyldopa (Standard) is the analytical standard of Methyldopa. This product is intended for research and analytical applications. Methyldopa (L-(-)-α-Methyldopa), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system .
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- HY-B0194S
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- HY-106874A
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RS-15385-197 hydrochloride
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Adrenergic Receptor
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Neurological Disease
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Delequamine (RS-15385-197) hydrochloride is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine hydrochloride shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine hydrochloride can be used for the study of erectile dysfunction .
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- HY-106874
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RS-15385-197
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Adrenergic Receptor
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Neurological Disease
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Delequamine (RS-15385-197) is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine can be used for the study of erectile dysfunction .
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- HY-136693
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Adrenergic Receptor
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Neurological Disease
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L-654284 is an α2-adrenergic receptor antagonist with significant selectivity. L-654284 competes with the binding of 3H-clonidine and 3H-rauwolscine in vitro and shows Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 can block the protrusion effect of clonidine in isolated vas deferens in rats, with a pA2 value of 9.1. L-654284 exhibits remarkable selectivity for α2 and α1 adrenergic receptors, and exhibits a Ki of 110 nM in inhibiting 3H-prazosin binding. L-654284 can significantly increase the turnover rate of norepinephrine in rat cerebral cortex in vivo, showing α2-adrenergic receptor blocking activity in the central nervous system .
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- HY-12710A
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- HY-U00123
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- HY-U00244
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- HY-100300
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- HY-162620
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Adrenergic Receptor
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Cancer
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α2A-AR agonist 1 (Compound B9) is a selective agonist for α2-adrenergic receptor (α2A-AR) with EC50 of 0.23 nM. α2A-AR agonist 1 exhibits a hypnotic effect, with ED50 of 0.138 mg/kg in the loss of righting reflex (LORR) experiment. α2A-AR agonist 1 exhibits metabolic stability in mouse liver microsomes .
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- HY-U00123A
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Hydroxyguanabenz hydrochloride
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Adrenergic Receptor
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Neurological Disease
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Guanoxabenz (Hydroxyguanabenz) hydrochloride is an α2 adrenergic receptor agonist, with a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor .
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- HY-12717
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Adrenergic Receptor
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Endocrinology
Cancer
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Phentolamine is a potent, selective and orally active α1 adrenergic and α2 adrenergic receptor antagonist. Phentolamine can be used for the research of erectile dysfunction .
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- HY-14607
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HP 749
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Potassium Channel
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Neurological Disease
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Besipirdine (hydrochloride) is a potassium channel blocker with cholinergic and adrenergic activity. The cholinergic activity of Besipirdine (hydrochloride) involves stimulating phosphatidylinositol turnover and reducing potassium currents. The adrenergic activity of Besipirdine (hydrochloride) involves stimulating norepinephrine release, which is attributed to the inhibition of presynaptic α2-adrenergic receptors and the inhibition of norepinephrine uptake. Besipirdine (hydrochloride) may be used in research for Alzheimer's disease .
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- HY-159639
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- HY-112658
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Adrenergic Receptor
Adenosine Receptor
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Endocrinology
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p-Iodoclonidine hydrochloride is a partial agonist of α2-adrenergic receptor. p-Iodoclonidine hydrochloride also has minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, and potentiates ADP induced platelet aggregation with an EC50 of 1.5 μM .
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- HY-A0066A
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Imidaline hydrochloride; NSC35110 hydrochloride
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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Tolazoline hydrochloride (Imidaline hydrochloride) is an α-adrenergic receptor antagonist. Tolazoline hydrochloride inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline hydrochloride can be used to study erectile dysfunction, α2-adrenergic receptor agonist-related poisoning, and skin vascular disease research .
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- HY-A0066
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Imidaline; NSC35110
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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Tolazoline (Imidaline) is an α-adrenergic receptor antagonist. Tolazoline inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline can be used to study erectile dysfunction, α2-adrenergic receptor agonist-related poisoning, and skin vascular disease research .
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- HY-105412A
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Adrenergic Receptor
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Neurological Disease
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RU 52583 is an oral bioactive antagonist of alpha 2-adrenergic receptor. RU 52583 possesses cognition-enhancing properties in rats with damage to the septohippocampal system .
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- HY-19057A
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- HY-119456A
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- HY-119456
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- HY-12709
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- HY-176078
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Adrenergic Receptor
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Others
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4-Hydroxy xylazine O-glucuronide (lithium) is a metabolite of the α2-adrenergic receptor agonist xylazine. 4-Hydroxy xylazine O-glucuronide (lithium) can be synthesized from xylazine via the intermediate metabolite 4-hydroxy xylazine .
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- HY-14561
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RX 781094
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Adrenergic Receptor
Imidazoline Receptor
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Neurological Disease
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Idazoxan (RX 781094) is a potent antagonist of α2 adrenergic receptor (α2AR) and potential I2 imidazoline receptor agonist. Idazoxan can be used in the research of antidepression and schizophrenia. Idazoxan has oral bioactivity .
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- HY-13715
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- HY-101690
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- HY-13715A
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- HY-160210
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Adrenergic Receptor
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Cardiovascular Disease
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BAY-6096 is a potent, selective, and highly water-soluble adrenergic receptor α2B antagonist with an IC50 of 14 nM. BAY-6096 can effectively reduceα 2B receptor agonist-induced rat vascular contraction .
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- HY-W741575
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- HY-13715B
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- HY-A0066R
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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Tolazoline (Standard) is the analytical standard of Tolazoline. This product is intended for research and analytical applications. Tolazoline (Imidaline) is an α-adrenergic receptor antagonist. Tolazoline inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline can be used to study erectile dysfunction, α2-adrenergic receptor agonist-related poisoning, and skin vascular disease research .
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- HY-12716
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Adrenergic Receptor
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Endocrinology
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BRL-44408 is a selective adrenergic receptor antagonist of α2A/α2B AR. BRL-44408 can effectively antagonize the inhibitory effects of norepinephrine or adrenergic receptor agonist Clonidine (HY-12721) on K +-induced [3H]norepinephrine and [3H]5-hydroxytryptamine release. BRL-44408 has a higher affinity for human platelet membranes containing α2A-adrenoceptors than BRL-41992 and Imiloxan (HY-101337). BRL-44408 may affect the release of norepinephrine and 5-hydroxytryptamine through a mechanism mediated by α2A-adrenoceptors, and has a potential role in the regulation of neurotransmitter release .
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- HY-U00244A
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P2647 hydrochloride; BZQ hydrochloride; Benzoquinamide hydrochloride
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Adrenergic Receptor
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Cancer
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Benzquinamide (P2647) is an antiemetic which can bind to the α2A, α2B, and α2C adrenergic receptors (α2-AR) with Ki values of 1,365, 691, and 545 nM, respectively. Benzquinamide also inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells .
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- HY-119883
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Adrenergic Receptor
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Neurological Disease
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A-61603 free base is a potent adrenergic receptor agonist. A-61603 free base reduces carotid artery conductance in anesthetized pigs mediated by α1 and α2 adrenergic receptors (pEC50=7.25). A-61603 free base can be used as a probe to study adrenergic function .
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- HY-13715C
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- HY-114814
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Adrenergic Receptor
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Neurological Disease
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ORM-10921 free base is a selective α-2C adrenergic receptor antagonist with a Ki of 1.4 nM. ORM-10921 free base displays potent antidepressant and antipsychotic-like effects .
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- HY-106838A
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Adrenergic Receptor
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Neurological Disease
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Org 6906 is a monoamine reuptake inhibitor that promotes monoaminergic neurotransmission by inhibiting the reuptake of noradrenaline, dopamine, and serotonin. Org 6906 is also an α2 Adrenergic Receptor antagonist, with a pKi value of 6.3 (using the selective α2 adrenergic receptor ligand [ 3H]rauwolscine as a ligand). Org 6906 exhibits antidepressant activity and can be used in research related to neurological disorders .
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- HY-10791
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- HY-12715S
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- HY-12717R
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Reference Standards
Adrenergic Receptor
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Endocrinology
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Phentolamine (Standard) is the analytical standard of Phentolamine. This product is intended for research and analytical applications. Phentolamine is a potent, selective and orally active α1 adrenergic and α2 adrenergic receptor antagonist. Phentolamine can be used for the research of erectile dysfunction .
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- HY-A0066AR
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Imidaline hydrochloride (Standard); NSC35110 hydrochloride (Standard)
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Reference Standards
Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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Tolazoline (hydrochloride) (Standard) is the analytical standard of Tolazoline hydrochloride (HY-A0066A). This product is intended for research and analytical applications. Tolazoline hydrochloride (Imidaline hydrochloride) is an α-adrenergic receptor antagonist. Tolazoline hydrochloride inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline hydrochloride can be used to study erectile dysfunction, α2-adrenergic receptor agonist-related poisoning, and skin vascular disease research .
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- HY-12709R
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Adrenergic Receptor
5-HT Receptor
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Neurological Disease
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ARC 239 (Standard) is the analytical standard of ARC 239. This product is intended for research and analytical applications. ARC 239 is an α2B/C-adrenergic receptor antagonist with pKi of 7.06 and 6.95 for rat kidney α2B and human α2C, respectively. ARC 239 also inhibits 5-HT1A receptor with a Ki of 63.1 nM .
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- HY-A0007
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N-0923 Hydrochloride
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Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
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Neurological Disease
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Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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- HY-32329
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Org-8282
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5-HT Receptor
Adrenergic Receptor
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Neurological Disease
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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-15394
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N-0437 hydrochloride
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Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
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Neurological Disease
Endocrinology
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(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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- HY-103109
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5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
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Neurological Disease
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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-B2169
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5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
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Neurological Disease
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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 .
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- HY-32329A
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MO-8282
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5-HT Receptor
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Neurological Disease
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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 .
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- HY-15394A
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N-0437
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Adrenergic Receptor
5-HT Receptor
Dopamine Receptor
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Neurological Disease
Endocrinology
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(Rac)-Rotigotine (N-0437) is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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- HY-13715AR
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- HY-P3641
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GnRH Receptor
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Neurological Disease
Metabolic Disease
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Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
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- HY-13715S
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- HY-176060
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Histamine Receptor
Adrenergic Receptor
5-HT Receptor
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Cardiovascular Disease
Cancer
|
Platelet aggregation-IN-3 (Compound 5) is a ligand for H2 histamine receptors, α2(A,C)-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. Platelet aggregation-IN-3 can inhibit platelet aggregation induced by ADP and collagen and can also modulate tumour cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 is promising for research of antiplatelet therapy in cardiovascular diseases and the prevention of cancer-related thrombosis and tumour metastasis .
|
-
- 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-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-13715R
-
-
- HY-105699
-
|
Adrenergic Receptor
|
Neurological Disease
|
Napamezole is an α2A adrenergic receptor antagonist and a serotonin/norepinephrine uptake inhibitor. Napamezole increases the levels of monoamines in the brain by blocking monoamine uptake, which gives it antidepressant activity .
|
-
- HY-122221
-
-
- HY-75502
-
N-0923; (-)-N 0437
|
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
Endocrinology
|
Rotigotine is a potent dopamine receptor agonist with Ki values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research .
|
-
- HY-A0007R
-
N-0923 Hydrochloride (Standard)
|
Reference Standards
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
Rotigotine (Hydrochloride) (Standard) is the analytical standard of Rotigotine (Hydrochloride). This product is intended for research and analytical applications. Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
|
-
- 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-13715BR
-
Levarterenol bitartrate monohydrate (Standard); L-Noradrenaline bitartrate monohydrate (Standard)
|
Reference Standards
Adrenergic Receptor
Autophagy
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
Cancer
|
Norepinephrine (bitartrate monohydrate) (Standard) is the analytical standard of Norepinephrine (bitartrate monohydrate). This product is intended for research and analytical applications. Norepinephrine (Levarterenol; L-Noradrenaline) bitartrate monohydrate is a potent adrenergic receptor (AR) agonist. Norepinephrine activates α1, α2, β1 receptors .
|
-
- HY-15394S1
-
N-0437-d3 hydrochloride
|
Isotope-Labeled Compounds
Adrenergic Receptor
Dopamine Receptor
5-HT Receptor
|
Endocrinology
|
(Rac)-Rotigotine-d3 hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
|
-
- HY-15394R
-
|
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
Endocrinology
|
(Rac)-Rotigotine (hydrochloride) (Standard) is the analytical standard of (Rac)-Rotigotine (hydrochloride). This product is intended for research and analytical applications. (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
|
-
- 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-75502R
-
N-0923 (Standard); (-)-N 0437 (Standard)
|
Reference Standards
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
Endocrinology
|
Rotigotine (Standard) is the analytical standard of Rotigotine. This product is intended for research and analytical applications. Rotigotine is a potent dopamine receptor agonist with Ki values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research .
|
-
- 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-B0362A
-
Phentolamine methanesulfonate
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction .
|
-
- HY-P3641A
-
|
GnRH Receptor
|
Neurological Disease
Metabolic Disease
|
Kisspeptin 13 TFA is the TFA salt form of Kisspeptin 13 (HY-P3641). Kisspeptin-13 TFA inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 TFA activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 TFA interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 TFA is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
|
-
- HY-101392
-
Harmane
1 Publications Verification
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
- HY-101392A
-
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
- HY-12717AS
-
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
Phentolamine-d4 (hydrochloride) is the deuterium labeled Phentolamine hydrochloride. Phentolamine hydrochloride is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine hydrochloride can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction .
|
-
- 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-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-W700834
-
|
Isotope-Labeled Compounds
|
Neurological Disease
Inflammation/Immunology
|
Harman-d3 is deuterium labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
- 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-103110
-
ST1936
1 Publications Verification
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
|
-
- HY-B0362AR
-
Phentolamine methanesulfonate (Standard)
|
Reference Standards
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
Phentolamine (mesylate) (Standard) is the analytical standard of Phentolamine (mesylate). This product is intended for research and analytical applications. Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction .
|
-
- HY-A0139
-
NSC 108165; Navan; Navane
|
Sigma Receptor
mAChR
Histamine Receptor
Dopamine Receptor
Adrenergic Receptor
|
Others
|
Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
|
-
- HY-103110A
-
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
|
-
- HY-15394S
-
N-0437-d7 hydrochloride
|
Isotope-Labeled Compounds
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
Endocrinology
|
(Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
|
-
- HY-B2195
-
|
Adrenergic Receptor
|
Metabolic Disease
|
Aidioxa has the ability to improve delayed gastric emptying in rats. It can partially improve delayed gastric emptying caused by clonidine or restraint stress. The allyltoin part of Aidioxa restores gastric emptying activity by antagonizing α-2 adrenergic receptors. Its aluminum hydroxide part is involved in restoring gastric compliance. Aidioxa can improve both delayed gastric emptying and impaired gastric compliance, both of which play an important role in functional dyspepsia (FD). Aidioxa is a candidate agent for inhibiting FD.
|
-
- HY-W777360
-
|
Isotope-Labeled Compounds
Adrenergic Receptor
Monoamine Oxidase
nAChR
Opioid Receptor
Imidazoline Receptor
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
Harman- 13C2, 15N is 13C and 15N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
|
-
- HY-W748758
-
NSC 108165-d8; Navan-d8; Navane-d8
|
Isotope-Labeled Compounds
Dopamine Receptor
Histamine Receptor
mAChR
Adrenergic Receptor
Sigma Receptor
|
Others
|
(Z)-Thiothixene-d8 (NSC 108165-d8; Navan-d8; Navane-d8) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
|
-
- HY-120179A
-
|
AAK1
|
Neurological Disease
|
LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors .
|
-
- HY-120179
-
|
AAK1
|
Neurological Disease
|
LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors .
|
-
- HY-103117
-
|
5-HT Receptor
|
Neurological Disease
|
S 32212 hydrochloride is an inverse agonist of 5-HT receptors 5-HT2(CINI) and 5-HT2(CVSV) (Kis=6.6, 8.9 nM) and an antagonist of 5-HT2A and α2β-adrenergic receptors (Ki=5.8, 5.8 nM). S 32212 hydrochloride can reduce the binding of GTPγS to Gαq, and reduce the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2(CINI) receptor and CHO cells expressing 5-HT2(CVSV) receptor (EC50=38 and 18.6 nM, respectively). S 32212 hydrochloride (2.5 mg/kg) reduces 5-HT receptor agonist-induced head twitches and penile erections in mice and rats. S 32212 hydrochloride (10, 40 mg/kg) reduces immobility time in the forced swim test and marble burying behavior in mice and rats, exerting antidepressant and anxiolytic activities.
|
-
- HY-103216A
-
|
Adrenergic Receptor
|
Neurological Disease
|
RWJ-52353 hydrochloride is an orally potent, highly selective α2D adrenergic receptor agonist (Ki: 1.5 nM) with potential analgesic effects. RWJ-52353 hydrochloride demonstrated analgesic activity in abdominal tests in rats and mice, and improved agitation in mice in the hot plate test and tail flick test. RWJ-52353 hydrochloride also regulates the organic cation transporter (OCT) subtype, inhibiting rOCT1 and rOCT2 with IC50s of 100 μM and 20 μM respectively; it also activates rOCT3, affecting [3H]-1- in cells. Methyl-4-phenylpyridinium ([3H]MPP) transport .
|
-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3641A
-
|
GnRH Receptor
|
Neurological Disease
Metabolic Disease
|
Kisspeptin 13 TFA is the TFA salt form of Kisspeptin 13 (HY-P3641). Kisspeptin-13 TFA inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 TFA activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 TFA interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 TFA is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
|
-
- HY-P3641
-
|
GnRH Receptor
|
Neurological Disease
Metabolic Disease
|
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-B0225B
-
-
-
- HY-B0225
-
-
-
- HY-A0066A
-
-
-
- HY-13715
-
-
-
- HY-13715A
-
-
-
- HY-13715B
-
-
-
- HY-B0225A
-
-
-
- HY-B0225BR
-
-
-
- HY-B0225R
-
-
-
- HY-12710A
-
-
-
- HY-13715C
-
-
-
- HY-A0066AR
-
Imidaline hydrochloride (Standard); NSC35110 hydrochloride (Standard)
|
Alkaloids
Other Alkaloids
Source classification
Alpinia officinarum Hance
Plants
Zingiberaceae
|
Reference Standards
Adrenergic Receptor
|
Tolazoline (hydrochloride) (Standard) is the analytical standard of Tolazoline hydrochloride (HY-A0066A). This product is intended for research and analytical applications. Tolazoline hydrochloride (Imidaline hydrochloride) is an α-adrenergic receptor antagonist. Tolazoline hydrochloride inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline hydrochloride can be used to study erectile dysfunction, α2-adrenergic receptor agonist-related poisoning, and skin vascular disease research .
|
-
-
- HY-13715AR
-
-
-
- HY-13715R
-
-
-
- HY-13715BR
-
-
-
- HY-A0019
-
-
-
- HY-101392
-
Harmane
1 Publications Verification
|
Alkaloids
Structural Classification
other families
Source classification
Pyridine Alkaloids
Plants
Indole Alkaloids
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Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
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Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
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- HY-101392A
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Apocynaceae
Structural Classification
Alkaloids
Other Alkaloids
Source classification
Plants
Rauwolfia canescens
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Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
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Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
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- HY-A0019R
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* This product has been "discontinued".
Optimized version of product available:
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Product Name |
Chemical Structure |
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- HY-B0194S
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Tizanidine-d4 is the deuterium labeled Tizanidine. Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons .
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- HY-12715S
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Yohimbine- 13C,d3 is the 13C- and deuterium labeled Yohimbine. Yohimbine is a potent and relatively nonselective alpha 2-adrenergic receptor (AR) antagonist, with IC50 of 0.6 μM.
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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-15394S1
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(Rac)-Rotigotine-d3 hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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- HY-12717AS
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Phentolamine-d4 (hydrochloride) is the deuterium labeled Phentolamine hydrochloride. Phentolamine hydrochloride is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine hydrochloride can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction .
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- HY-17034BS
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Medetomidine-d3 (hydrochloride) is the deuterium labeled Medetomidine hydrochloride. Medetomidine hydrochloride is an agonist of adrenergic alpha-2 receptor .
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- HY-B0659S
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Brimonidine-d4 is the deuterium labeled Brimonidine. Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
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- HY-B0225AS
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Methyldopa-d3 (hydrochloride) is deuterium labeled Methyldopa (hydrochloride). Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system .
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- HY-13715S
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(Rac)-Norepinephrine-d3 (formate) is deuterium labeled Norepinephrine. Norepinephrine (Levarterenol; L-Noradrenaline) is a potent adrenergic receptor (AR) agonist. Norepinephrine activates α1, α2, β1 receptors .
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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-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-W700834
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Harman-d3 is deuterium labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
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- HY-15394S
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(Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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- HY-W777360
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Harman- 13C2, 15N is 13C and 15N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF) .
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- HY-W748758
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(Z)-Thiothixene-d8 (NSC 108165-d8; Navan-d8; Navane-d8) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
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