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Isoforms Recommended:	α adrenergic receptor

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α2-adrenergic receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (21) Adenosine Receptor (1) Adenylate Cyclase (1) Adrenergic Receptor (97) Cytochrome P450 (4) Dopamine Receptor (11) Drug Derivative (1) Drug Metabolite (3) Endogenous Metabolite (5) GABA Receptor (3) GnRH Receptor (2) Histamine Receptor (3) Imidazoline Receptor (9) Isotope-Labeled Compounds (9) mAChR (2) Monoamine Oxidase (3) Monoamine Transporter (1) nAChR (3) Opioid Receptor (3) Potassium Channel (1) Reference Standards (14) Sigma Receptor (2) Vasopressin Receptor (1)
By Research Areas:	Cancer (7) Cardiovascular Disease (31) Endocrinology (32) Infection (1) Inflammation/Immunology (4) Metabolic Disease (11) Neurological Disease (62)

By Targets:

5-HT Receptor (21)

Adenosine Receptor (1)

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Adrenergic Receptor (97)

Cytochrome P450 (4)

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Drug Derivative (1)

Drug Metabolite (3)

Endogenous Metabolite (5)

GABA Receptor (3)

GnRH Receptor (2)

Histamine Receptor (3)

Imidazoline Receptor (9)

Isotope-Labeled Compounds (9)

mAChR (2)

Monoamine Oxidase (3)

Monoamine Transporter (1)

nAChR (3)

Opioid Receptor (3)

Potassium Channel (1)

Reference Standards (14)

Sigma Receptor (2)

Vasopressin Receptor (1)

By Research Areas:

Cancer (7)

Cardiovascular Disease (31)

Endocrinology (32)

Infection (1)

Inflammation/Immunology (4)

Metabolic Disease (11)

Neurological Disease (62)

107

Inhibitors & Agonists

Peptides

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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0225

Methyldopa 2 Publications Verification L-(-)-α-Methyldopa; MK-351	Adrenergic Receptor Endogenous Metabolite	Cardiovascular Disease Endocrinology
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 .

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-A0019

Paliperidone 3 Publications Verification 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-32329

Setiptiline 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-19057A

Vatinoxan hydrochloride 2 Publications Verification MK-467 hydrochloride; L-659066 hydrochloride	Adrenergic Receptor	Neurological Disease Endocrinology
Vatinoxan hydrochloride (MK-467 hydrochloride;L-659066 hydrochloride) is a peripheral **α2 adrenergic receptor** antagonist.

HY-B0225B

Methyldopa hydrate 2 Publications Verification L-(-)-α-Methyldopa hydrate; MK-351 hydrate	Adrenergic Receptor Endogenous Metabolite	Cardiovascular Disease Endocrinology
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 .

HY-B0362A

Phentolamine mesylate 5+ Cited Publications 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-B0659

Brimonidine Maximum Cited Publications 7 Publications Verification UK 14304; AGN190342	Adrenergic Receptor	Cardiovascular Disease Endocrinology Cancer
Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.

HY-B0659A

Brimonidine tartrate Maximum Cited Publications 7 Publications Verification UK 14304 tartrate; AGN190342 tartrate	Adrenergic Receptor	Cardiovascular Disease Endocrinology Cancer
Brimonidine tartrate (UK 14304 tartrate) is a full α2-adrenergic receptor (α2-AR) agonist.

HY-103413

Eticlopride hydrochloride	Dopamine Receptor	Neurological Disease
Eticlopride hydrochloride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1-adrenergic, α2-adrenergic, 5HT1, 5HT2 receptors with K_is of 0.09, 112, 699, 6220, and 830 nM, respectively. Eticlopride hydrochloride is an antipsychotic agent .

HY-B2169

Melperone	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 K_ds 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 K_d 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-B1052

Lofexidine hydrochloride Baq-168; MDL-14042	Adrenergic Receptor Imidazoline Receptor	Neurological Disease Metabolic Disease
Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α₂-adrenergic receptor (α2-adrenergic *receptor). Lofexidine hydrochloride binds to the α₂A-adrenergic* receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal .

HY-A0066A

Tolazoline hydrochloride Imidaline hydrochloride; NSC35110 hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
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-A0066

Tolazoline Imidaline; NSC35110	Adrenergic Receptor	Cardiovascular Disease Endocrinology
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 .

HY-B1052A

Lofexidine Baq-168 free base; MDL-14042 free base	Imidazoline Receptor Adrenergic Receptor	Neurological Disease Metabolic Disease
Lofexidine (Baq-168 free base) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α₂-adrenergic receptor (α2-adrenergic *receptor). Lofexidine binds to the α₂A-adrenergic* receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine is applicable to research on opioid addiction and withdrawal .

HY-B1696

Methyldopate	Adrenergic Receptor	Cardiovascular Disease
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 .

HY-101392A

Harmane hydrochloride 1 Publications Verification	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-12710A

Rauwolscine hydrochloride α-Yohimbine hydrochloride; Corynanthidine hydrochloride; Isoyohimbine hydrochloride	Adrenergic Receptor	Neurological Disease Endocrinology
Rauwolscine hydrochloride is a potent and specific *α2 adrenergic* receptor antagonist with a K_i of 12 nM.

HY-P3641A

Kisspeptin 13 TFA	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-W702712

3-Hydroxy xylazine	Adrenergic Receptor	Neurological Disease
3-Hydroxy xylazine is a metabolite of the α2-adrenergic receptor agonist Xylazine.

HY-101610

OPC-28326	Adrenergic Receptor	Cardiovascular Disease Endocrinology
OPC-28326 is a selective peripheral vasodilator and an angatonist of **α2-adrenergic receptor, with K_i** of 2040, 285, and 55 nM for α2A-, α2B- and α2C-adrenoceptors, respectively.

HY-32329A

Setiptiline maleate 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-HT_2A, 5-HT_2C, and/or 5-HT₃ subtypes, as well as an H1 receptor inverse agonist/antihistamine .

HY-103110

ST1936 1 Publications Verification	5-HT Receptor Adrenergic Receptor	Neurological Disease
ST1936 is a selective, nanomolar affinity 5-HT₆ receptor agonist with K_i values of 13 nM, 168 nM and 245 nM for human 5-HT₆, 5-HT₇ and 5-HT_2B receptors, respectively. ST1936 also shows moderate affinity (K_i of 300 nM) for human and rat **α2 adrenergic receptor** .

HY-B0659S

Brimonidine-d4	Adrenergic Receptor	Endocrinology
Brimonidine-d₄ is the deuterium labeled Brimonidine. Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.

HY-B1052S

Lofexidine-d4 hydrochloride Baq-168-d₄; MDL-14042-d₄	Isotope-Labeled Compounds Imidazoline Receptor Adrenergic Receptor	Neurological Disease Metabolic Disease
Lofexidine-d₄ hydrochloride (Baq-168-d₄) is the deuterium labeled Lofexidine hydrochloride (HY-B1052). Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α₂-adrenergic receptor (α2-adrenergic *receptor). Lofexidine hydrochloride binds to the α₂A-adrenergic* receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal .

HY-B0225A

Methyldopa hydrochloride L-(-)-α-Methyldopa hydrochloride; MK-351 hydrochloride	Adrenergic Receptor Endogenous Metabolite	Cardiovascular Disease Endocrinology
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 .

HY-19057

Vatinoxan 2 Publications Verification MK-467; L-659066	Adrenergic Receptor	Cardiovascular Disease Neurological Disease
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 .

HY-B0659AR

Brimonidine tartrate (Standard) UK 14304 tartrate (Standard); AGN190342 tartrate (Standard)	Reference Standards Adrenergic Receptor	Endocrinology Cancer
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.

HY-B1696A

Methyldopate hydrochloride	Adrenergic Receptor	Cardiovascular Disease
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 .

HY-P3641

Kisspeptin 13	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 .

HY-119456A

Romifidine hydrochloride	Adrenergic Receptor	Neurological Disease
Romifidine hydrochloride is an **α₂ adrenergic receptor** agonist. Romifidine hydrochloride shows sedation effects in vivo .

HY-U00123A

Guanoxabenz hydrochloride Hydroxyguanabenz hydrochloride	Adrenergic Receptor	Neurological Disease
Guanoxabenz (Hydroxyguanabenz) hydrochloride is an **α2 adrenergic receptor** agonist, with a K_i of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor .

HY-A0019S

Paliperidone-d4	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-103109

Melperone hydrochloride	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 K_ds 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 K_d 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-129697

3-Hydroxy Medetomidine 3-OH Medetomidine; Medetomidine metabolite MIII	Drug Metabolite	Metabolic Disease
3-Hydroxy Medetomidine (3-OH Medetomidine; Medetomidine metabolite MIII) is a metabolite of the α2-adrenergic receptor agonist medetomidine.

HY-121129

Eticlopride FLB-131	Dopamine Receptor	Neurological Disease
Eticlopride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1‐adrenergic, α2‐adrenergic, 5HT1, 5HT2 receptors with K_is of 0.09, 112, 699, 6220, and 830 nM, respectively. Eticlopride is an antipsychotic agent .

HY-105960A

Fenmetozole hydrochloride	Adrenergic Receptor	Neurological Disease
Fenmetozole hydrochloride is an antagonist of ethanol, and also antagonizes α2-adrenergic receptor, which has antidepressant effect .

HY-16525

XEN-2174	Monoamine Transporter Adrenergic Receptor	Neurological Disease
XEN-2174 is a noradrenaline transporter (NET) inhibitor. XEN-2174 inhibits the reuptake of noradrenaline through non-competitive inhibition, increasing the concentration of noradrenaline in the synaptic cleft, thereby activating **α2-adrenergic receptor** at the spinal level and exerting analgesic effects. XEN-2174 exhibits long-lasting analgesic effects in models of neuropathic pain and postoperative pain in rats. XEN-2174 can be used in pain research .

HY-112074

Tiamenidine HOE 440	Adrenergic Receptor	Cardiovascular Disease
Tiamenidine (HOE 440) is an orally active **α2-adrenergic receptor** agonist with antihypertensive effect. Tiamenidine is used as an antihypertensive agent for hypertension research .

HY-B2169S2

Melperone-d4 hydrochloride	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 K_ds 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 K_d 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-A0139

Thiothixene 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-106617

Etoperidone	5-HT Receptor Adrenergic Receptor	Neurological Disease
Etoperidone, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone shows K_d 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 .

HY-106617A

Etoperidone hydrochloride	5-HT Receptor Adrenergic Receptor	Neurological Disease
Etoperidone hydrochloride, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone hydrochloride shows K_d 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 .

HY-106444

Fipamezole MPV 1730; JP-1730	Adrenergic Receptor	Neurological Disease
Fipamezole (MPV 1730; JP-1730) is a potent and orally active **α2-adrenergic receptor antagonist with K_i** 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 .

HY-119456

Romifidine	Adrenergic Receptor	Neurological Disease
Romifidine is an **α₂ adrenergic receptor** agonist. Romifidine shows sedation effects in vivo .

HY-106874A

Delequamine hydrochloride RS-15385-197 hydrochloride	Adrenergic Receptor	Neurological Disease
Delequamine (RS-15385-197) hydrochloride is an orally active and selective **α2-adrenergic receptor antagonist with a pK_i** 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 .

HY-106874

Delequamine RS-15385-197	Adrenergic Receptor	Neurological Disease
Delequamine (RS-15385-197) is an orally active and selective **α2-adrenergic receptor antagonist with a pK_i** 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 .

HY-U00117

Lusaperidone R107474	Adrenergic Receptor	Neurological Disease Endocrinology
Lusaperidone (R107474) is an α2 adrenergic *receptor* antagonist with K_is of 0.13 and 0.15 nM for α2A and α2C, respectively.

HY-14561

Idazoxan RX 781094	Adrenergic Receptor Imidazoline Receptor	Neurological Disease
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 .

HY-W982195

Napamezole hydrochloride	Adrenergic Receptor 5-HT Receptor	Neurological Disease
Napamezole hydrochloride is an orally active **α-2 adrenergic receptor** antagonist and serotonin (5-HT Receptor) reuptake inhibitor, with K_i values of 28 nM and 93 nM for rat α-2 and α-1 adrenergic receptors, respectively. Napamezole hydrochloride can be used for the research of depression .

Cat. No.	Product Name	Target	Research Area

HY-P3641A

Kisspeptin 13 TFA	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

Kisspeptin 13	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 .

HY-16525

XEN-2174	Monoamine Transporter Adrenergic Receptor	Neurological Disease
XEN-2174 is a noradrenaline transporter (NET) inhibitor. XEN-2174 inhibits the reuptake of noradrenaline through non-competitive inhibition, increasing the concentration of noradrenaline in the synaptic cleft, thereby activating **α2-adrenergic receptor** at the spinal level and exerting analgesic effects. XEN-2174 exhibits long-lasting analgesic effects in models of neuropathic pain and postoperative pain in rats. XEN-2174 can be used in pain research .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B0225

Methyldopa 2 Publications Verification L-(-)-α-Methyldopa; MK-351	Classification of Application Fields Ketones, Aldehydes, Acids Hippocastanaceae Aesculus hippocastanum Plants Disease Research Fields Endocrinology Source Classification	Adrenergic Receptor Endogenous Metabolite
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 .

HY-101392

Harmane 1 Publications Verification	Alkaloids other families Pyridine Alkaloids Plants Indole Alkaloids Source Classification	Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor nAChR GABA Receptor Opioid Receptor
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-A0019

Paliperidone 3 Publications Verification 9-Hydroxyrisperidone	Natural Products Endogenous metabolite Source Classification	Drug Metabolite Dopamine Receptor 5-HT Receptor Adrenergic Receptor
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-B0225B

Methyldopa hydrate 2 Publications Verification L-(-)-α-Methyldopa hydrate; MK-351 hydrate	Cardiovascular Disease Alkaloids Classification of Application Fields Other Alkaloids Phenols Polyphenols Endogenous metabolite Disease Research Fields Endocrinology Source Classification	Adrenergic Receptor Endogenous Metabolite
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 .

HY-A0066A

Tolazoline hydrochloride Imidaline hydrochloride; NSC35110 hydrochloride	Alkaloids Classification of Application Fields Other Alkaloids Alpinia officinarum Hance Plants Disease Research Fields Endocrinology Source Classification Zingiberaceae	Adrenergic Receptor
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-101392A

Harmane hydrochloride 1 Publications Verification	Apocynaceae Alkaloids Other Alkaloids Plants Rauwolfia canescens Source Classification	Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor nAChR GABA Receptor Opioid Receptor
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-12710A

Rauwolscine hydrochloride α-Yohimbine hydrochloride; Corynanthidine hydrochloride; Isoyohimbine hydrochloride	Alkaloids other families Classification of Application Fields Neurological Disease Plants Disease Research Fields Endocrinology Indole Alkaloids Source Classification	Adrenergic Receptor
Rauwolscine hydrochloride is a potent and specific *α2 adrenergic* receptor antagonist with a K_i of 12 nM.

HY-B0225A

Methyldopa hydrochloride L-(-)-α-Methyldopa hydrochloride; MK-351 hydrochloride	Cardiovascular Disease Alkaloids Classification of Application Fields Other Alkaloids Phenols Polyphenols Endogenous metabolite Disease Research Fields Endocrinology Source Classification	Adrenergic Receptor Endogenous Metabolite
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 .

HY-B0225BR

Methyldopa hydrate (Standard) L-(-)-α-Methyldopa hydrate (Standard); MK-351 hydrate (Standard)	Structural Classification Alkaloids Other Alkaloids Phenols Polyphenols Endogenous metabolite Source Classification	Reference Standards Adrenergic Receptor Endogenous Metabolite
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 .

HY-A0066AR

Tolazoline hydrochloride (Standard) Imidaline hydrochloride (Standard); NSC35110 hydrochloride (Standard)	Alkaloids Other Alkaloids Alpinia officinarum Hance Plants Source Classification 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-A0019R

Paliperidone (Standard) 9-Hydroxyrisperidone (Standard)	Structural Classification Natural Products Endogenous metabolite Source Classification	Drug Metabolite Reference Standards Dopamine Receptor 5-HT Receptor Adrenergic Receptor
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 .

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HY-P702203

	ADRA2A-VLPs Protein, Human (HEK293, His) Alpha-2A adrenergic receptor; Alpha-2 adrenergic receptor subtype C10; Alpha-2A adrenoreceptor; Alpha-2A adrenoceptor; Alpha-2AAR	Human	HEK293
	ADRA2A-VLPs Protein, Human (HEK293, His) is recommended for animal immunization, ELISA. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays. If VLP control is required, it is recommended HY-P701236. Tags can only be detected under denaturing conditions.

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Cat. No.	Product Name	Chemical Structure

HY-B0659S

Brimonidine-d4
Brimonidine-d₄ is the deuterium labeled Brimonidine. Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.

HY-B1052S

Lofexidine-d4 hydrochloride

Lofexidine-d₄ hydrochloride (Baq-168-d₄) is the deuterium labeled Lofexidine hydrochloride (HY-B1052). Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α₂-adrenergic receptor (α2-adrenergic receptor). Lofexidine hydrochloride binds to the α₂A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal .

HY-A0019S

Paliperidone-d4
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-B2169S2

Melperone-d4 hydrochloride

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 K_ds 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 K_d 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-12717AS

Phentolamine-d4 hydrochloride

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-B1052S1

Lofexidine-d4

Lofexidine-d₄ (Baq-168 free base-d₄) is deuterium labeled Lofexidine (HY-B1052A). Lofexidine (Baq-168 free base) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α₂-adrenergic receptor (α2-adrenergic receptor). Lofexidine binds to the α₂A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine is applicable to research on opioid addiction and withdrawal .

HY-B0225AS

Methyldopa-d3 hydrochloride
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 .

HY-32329S

Setiptiline-d3

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-W777360

Harman-13C2,15N

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

(Z)-Thiothixene-d8

(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-12715S

Yohimbine-13C,d3 1 Publications Verification
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.

HY-W700834

Harman-d3

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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