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α2 adrenoceptors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (6) Adrenergic Receptor (73) Apoptosis (5) Autophagy (4) Dopamine Receptor (7) Endogenous Metabolite (2) Histamine Receptor (3) Histone Methyltransferase (5) Imidazoline Receptor (7) mAChR (1) Monoamine Oxidase (1) Parasite (2) Prostaglandin Receptor (1)
By Research Areas:	Cancer (23) Cardiovascular Disease (26) Endocrinology (32) Inflammation/Immunology (5) Metabolic Disease (6) Neurological Disease (42)

Inhibitors & Agonists

Peptides

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-17034A

Dexmedetomidine hydrochloride Maximum Cited Publications 10 Publications Verification (+)-Medetomidine hydrochloride; (S)-Medetomidine hydrochloride	Adrenergic Receptor	Neurological Disease Endocrinology Cancer
Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of *α2-adrenoceptor, with a K_i* of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects .

HY-12719

Dexmedetomidine Maximum Cited Publications 10 Publications Verification (+)-Medetomidine; (S)-Medetomidine	Adrenergic Receptor	Neurological Disease Cancer
Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of *α2-adrenoceptor, with a K_i* of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects .

HY-B0409A

Clonidine hydrochloride 5 Publications Verification	Adrenergic Receptor	Cardiovascular Disease Endocrinology Cancer
Clonidine hydrochloride is an agonist of *α2-adrenoceptor* and potent antihypertensive agent.

HY-155879

(±)-N-Methylcoclaurine	Adrenergic Receptor	Others
(±)-N-Methylcoclaurine is a selective α2-adrenoceptor antagonist .

HY-17034

Medetomidine	Adrenergic Receptor	Neurological Disease Endocrinology
Medetomidine is an orally active *α2-adrenoceptor* agonist (K_i: 1.08 nM). Medetomidine has sedative and analgesic effects. Medetomidine can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels .

HY-17034B

Medetomidine hydrochloride MPV785	Adrenergic Receptor	Neurological Disease Endocrinology
Medetomidine hydrochloride is an orally active *α2-adrenoceptor* agonist (K_i: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels .

HY-121312

Flutonidine ST-600	Adrenergic Receptor	Cardiovascular Disease
Flutonidine (ST-600) is a Clonidine (HY-12721) analogue that shows antihypertensive and sympatholytic effects. The initial hypertension produced by Flutonidine is due to stimulation of the peripheral α1, α2 adrenoceptors and the subsequent fall in blood pressure is due to the stimulation of central α2 adrenoceptors. Flutonidine reduces the arrhythmogenic and lethal effects of ouabain. Flutonidine is promising for research of ventricular arrhythmias caused by cardiac glycosides .

HY-12719R

Dexmedetomidine (Standard)	Adrenergic Receptor	Neurological Disease Cancer
Dexmedetomidine (Standard) is the analytical standard of Dexmedetomidine. This product is intended for research and analytical applications. Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of *α2-adrenoceptor, with a K_i* of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects .

HY-101683

Deriglidole SL 86-0715	Adrenergic Receptor	Metabolic Disease Endocrinology
Deriglidole is a peripheral *adrenoceptor* antagonist with a high affinity for α₂-adrenoceptors.

HY-136935

Alloyohimbine	Adrenergic Receptor	Endocrinology
Alloyohimbine, an alkaloid, is a selective *α2-adrenoceptor* antagonist with K_Dα1, K_Dα2 of 0.28 μM and 0.006 μM, respectively .

HY-12380A

Atipamezole 5+ Cited Publications MPV 1248	Adrenergic Receptor	Neurological Disease Endocrinology
Atipamezole (MPV 1248) is a potent α₂-adrenoceptor antagonist with a K_i of 1.6 nM .

HY-106874B

rel-Delequamine rel-RS-15385-197	Adrenergic Receptor Prostaglandin Receptor	Neurological Disease
rel-Delequamine (rel-RS-15385-197) is an orally active, brain-penetrant, potent and selective *M₂-adrenoceptor* antagonist and *α₂-adrenoceptor* antagonist. rel-Delequamine has a pK_i of 9.45 for α₂-adrenoceptors in the rat cortex. rel-Delequamine augments K ⁺-evoked release of noradrenaline with an EC₅₀ of 1 nM .

HY-12380

Atipamezole hydrochloride 5+ Cited Publications MPV-1248 hydrochloride	Adrenergic Receptor	Neurological Disease Endocrinology
Atipamezole (MPV-1248) hydrochloride is a potent α₂-adrenoceptor antagonist with a K_i of 1.6 nM .

HY-12710

Rauwolscine α-Yohimbine; Corynanthidine; Isoyohimbine	Adrenergic Receptor	Cancer
Rauwolscine is a selective *α2-adrenoceptor* antagonist that inhibits tumor growth and induces apoptosis .

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-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-100850

Piperoxan hydrochloride Benodaine hydrochloride	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Piperoxan (Benodaine) hydrochloride is an α₂ adrenoceptor antagonist. Piperoxan hydrochloride is the first-generation antihistamine.

HY-W263279

(E)-Guanabenz (E)-Wy-8678	Adrenergic Receptor	Cardiovascular Disease Neurological Disease
(E)-Guanabenz ((E)-Wy-8678) is an orally active central *α2-adrenoceptor* agonist. (E)-Guanabenz has antihypertensive activity, acts via stimulating central α2-adrenoceptors, and reducing net sympathetic outflow into the periphery. (E)-Guanabenz also directly binds to and inhibits GADD34, and has neuroprotective activity. (E)-Guanabenz can be used for researching hypertension and Parkinson disease .

HY-B0409AR

Clonidine hydrochloride (Standard)	Adrenergic Receptor	Cardiovascular Disease Endocrinology Cancer
Clonidine (hydrochloride) (Standard) is the analytical standard of Clonidine (hydrochloride). This product is intended for research and analytical applications. Clonidine hydrochloride is an agonist of α2-adrenoceptor and potent antihypertensive agent.

HY-U00123

Guanoxabenz Hydroxyguanabenz	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Guanoxabenz 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-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-A0008

Talipexole dihydrochloride B-HT 920 dihydrochloride	Adrenergic Receptor Dopamine Receptor 5-HT Receptor	Neurological Disease Endocrinology
Talipexole dihydrochloride (B-HT 920 dihydrochloride) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.

HY-U00165

Midaglizole hydrochloride (±)-DG5128; DG5128	Adrenergic Receptor	Cardiovascular Disease Metabolic Disease Endocrinology
Midaglizole hydrochloride ((±)-DG5128, DG5128) is a potent *α2-adrenoceptor* antagonist. Midaglizole hydrochloride is a hypoglycemic agent. Midaglizole hydrochloride increases blood pressure and reduces blood glucose levels in vivo .

HY-103203

ST91	Adrenergic Receptor	Neurological Disease
ST91 is a **α₂-adrenoceptor (α₂AR)** agonist. ST91 activates both α_2AAR and non-α_2AAR subtypes to produce spinal antinociception .

HY-101061

2-MPMDQ	Adrenergic Receptor	Cardiovascular Disease
2-MPMDQ is a potent and selective *α1-adrenoceptor* (K_i=0.37 nM) antagonist over α2-adrenoceptor (K_i=1740 nM). 2-MPMDQ is potent anti-hypertensive agent and has the potential for hypertension research .

HY-B1416A

Efaroxan hydrochloride	Adrenergic Receptor Imidazoline Receptor	Cardiovascular Disease Metabolic Disease
Efaroxan hydrochloride is a potent, selective and orally active *α2-adrenoceptor* antagonist, with antidiabetic activity. Efaroxan hydrochloride is a selective I1-Imidazoline receptor antagonist. Efaroxan hydrochloride can be used for the research of cardiovascular disease .

HY-148529

Midaglizole (±)-DG5128 free base; DG5128 free base	Adrenergic Receptor	Cardiovascular Disease Metabolic Disease
Midaglizole ((±)-DG5128 free base; DG5128 free base) is a potent *α2-adrenoceptor* antagonist. Midaglizole is a hypoglycemic agent. Midaglizole increases blood pressure and reduces blood glucose levels in vivo .

HY-B0354A

Urapidil hydrochloride	5-HT Receptor Adrenergic Receptor	Cardiovascular Disease Endocrinology
Urapidil hydrochloride is an orally active *α1-adrenoceptor* antagonist and 5-HT_1A receptor agonist with a pIC₅₀ of 6.13 and 4.38 against α1- and α2-adrenoceptor, respectively. Urapidil hydrochloride shows antihypertensive effect .

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-101690

QF0301B	Adrenergic Receptor	Cardiovascular Disease Endocrinology
QF0301B is an α1 adrenergic receptor antagonist and a low α2 adrenoceptor, 5-HT2A, and histamine H1 receptor blocker.

HY-17034AR

Dexmedetomidine hydrochloride (Standard) (+)-Medetomidine hydrochloride (Standard); (S)-Medetomidine hydrochloride (Standard)	Adrenergic Receptor	Neurological Disease Endocrinology Cancer
Dexmedetomidine (hydrochloride) (Standard) is the analytical standard of Dexmedetomidine (hydrochloride). This product is intended for research and analytical applications. Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of *α2-adrenoceptor, with a K_i* of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects .

HY-B0354AR

Urapidil hydrochloride (Standard)	5-HT Receptor Adrenergic Receptor	Cardiovascular Disease Endocrinology
Urapidil (hydrochloride) (Standard) is the analytical standard of Urapidil (hydrochloride). This product is intended for research and analytical applications. Urapidil hydrochloride is an orally active *α1-adrenoceptor* antagonist and 5-HT_1A receptor agonist with a pIC₅₀ of 6.13 and 4.38 against α1- and α2-adrenoceptor, respectively. Urapidil hydrochloride shows antihypertensive effect .

HY-14561A

Idazoxan hydrochloride RX 781094 hydrochloride	Adrenergic Receptor Imidazoline Receptor	Neurological Disease Endocrinology
Idazoxan hydrochloride (RX 781094 hydrochloride) is an *α₂-adrenoceptor* antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like agents (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism .

HY-169791

ECPLA	5-HT Receptor	Neurological Disease
ECPLA, a lysergamide lysergic acid diethylamidean (LSD) analog, is a potent 5-HT2A agonist (EC₅₀ of 14.6 nM) for Gq-mediated calcium flux. ECPLA has high affinity for most serotonin receptors, α2-adrenoceptors, and D2-like dopamine receptors .

HY-12707

Piribedil 1 Publications Verification	Dopamine Receptor Adrenergic Receptor Histone Methyltransferase	Neurological Disease Endocrinology Cancer
Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a *α2-adrenoceptors* antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC₅₀: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers .

HY-12707A

Piribedil dihydrochloride	Adrenergic Receptor Dopamine Receptor Histone Methyltransferase	Neurological Disease Endocrinology Cancer
Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a *α2-adrenoceptors* antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC₅₀: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers .

HY-12707C

Piribedil hydrochloride	Dopamine Receptor Adrenergic Receptor Histone Methyltransferase	Neurological Disease Endocrinology Cancer
Piribedil hydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil hydrochloride is also a *α2-adrenoceptors* antagonist. Piribedil hydrochloride can inhibit MLL1 methyltransferase activity (EC₅₀: 0.18 μM). Piribedil hydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers .

HY-12707B

Piribedil maleate	Dopamine Receptor Adrenergic Receptor Histone Methyltransferase	Neurological Disease Endocrinology Cancer
Piribedil maleate is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil maleate is also a *α2-adrenoceptors* antagonist. Piribedil maleate can inhibit MLL1 methyltransferase activity (EC₅₀: 0.18 μM). Piribedil maleate has the potential for the research of parkinson's disease, circulatory disorders, cancers .

HY-160932

RS-15385-198	Others	Endocrinology
RS-15385-198 is the enantiomer of Delequamine (RS-15385-197) (HY-106874). RS-15385-198 exhibits a pK_i of 6.32 for α₂-adrenoceptors in the rat cortex. RS-15385-198 is an antagonist for UK-14304 (HY-B0659) in the rat vas deferens and in the guinea-pig ileum .

HY-106973A

Nolomirole hydrochloride CHF 1035	Dopamine Receptor Adrenergic Receptor	Cardiovascular Disease
Nolomirole (CHF 1035) hydrochloride is an orally active and selective DA2 dopaminergic receptor/α2-adrenoceptor agonist. Nolomirole attenuates the heart failure signs in the Monocrotaline (HY-N0750)-induced congestive heart failure model. Nolomirole increases cardiac output .

HY-101338

RS-79948-197	Adrenergic Receptor	Neurological Disease
RS-79948-197 is a non-imidazoline *α2-adrenoceptor* antagonist. RS-79948-197 shows K_d values of 0.42 nM, 0.18 nM, 0.19 nM, 0.60 nM, 0.46 nM, and 0.77 nM for rat α2A, rat α2B, rat α2C, human α2A, human α2B, and human α2C, respectively .

HY-161836

α2AR agonist 1	Adrenergic Receptor	Cardiovascular Disease
α2AR agonist 1 (compound S6a), a new morpholine-containing pyrimidinone, acts as an agonist of *α2-adrenoceptor*. α2AR agonist 1 induces a concentration-dependent relaxation on aortic ring pre-contracted with Phenylephrine (HY-B0769; pEC₅₀=6.81). α2AR agonist 1 increases NOx and NO levels in HUVECs .

HY-B0352

Mirtazapine 1 Publications Verification Org3770; 6-Azamianserin	5-HT Receptor Histamine Receptor Adrenergic Receptor	Neurological Disease Inflammation/Immunology Cancer
Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT₂, 5-HT₃, histamine H1 receptor and *α2-adrenoceptor* antagonist with pK_i values of 8.05, 8.1, 9.3 and 6.95, respectively .

HY-12707R

Piribedil (Standard)	Dopamine Receptor Adrenergic Receptor Histone Methyltransferase	Neurological Disease Endocrinology Cancer
Piribedil (Standard) is the analytical standard of Piribedil. This product is intended for research and analytical applications. Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a *α2-adrenoceptors* antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC₅₀: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers .

HY-B0352R

Mirtazapine (Standard) 1 Publications Verification Org3770 (Standard); 6-Azamianserin (Standard)	5-HT Receptor Histamine Receptor Adrenergic Receptor	Neurological Disease Inflammation/Immunology Cancer
Mirtazapine (Standard) is the analytical standard of Mirtazapine. This product is intended for research and analytical applications. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT₂, 5-HT₃, histamine H1 receptor and *α2-adrenoceptor* antagonist with pK_i values of 8.05, 8.1, 9.3 and 6.95, respectively .

HY-101392R

Harmane (Standard)	Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor	Neurological Disease Cancer
Harmane (Standard) is the analytical standard of Harmane. This product is intended for research and analytical applications. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC₅₀=30 nM) over *α2-adrenoceptor* (IC₅₀=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC₅₀s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect .

HY-103197

2-Methoxyidazoxan monohydrochloride RX821002 hydrochloride	Adrenergic Receptor	Neurological Disease
2-Methoxyidazoxan monohydrochloride (RX821002 hydrochloride) is a highly selective *alpha 2-adrenoceptor* antagonist with little or no imidazoline antagonist effect. RX 821002 has markedly higher affinity for (guinea-pig) alpha 2D-adrenoceptors (pK_d 9.7) than for (rabbit) alpha 2A-adrenoceptors (pK_d 8.2) .

HY-103212

Azepexole dihydrochloride B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Azepexole (B-HT 933) dihydrochloride is a potent and selective *alpha 2-adrenoceptor* agonist with pK_is of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively . Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC₅₀= 78.72 nM) .

HY-158194

*α2C adrenoceptor* agonist 1**	Adrenergic Receptor	Cancer
α2C adrenoceptor agonist 1 (Compound A) is an orally active, highly selective, and non-central nervous system penetrating agonist for the *α2C-adrenoceptor, with EC₅₀* and K_i values of 108 nM and 12 nM, respectively. α2C adrenoceptor agonist 1 can be used in the study of nasal congestion .

HY-103212A

Azepexole hydrochloride B-HT 933 hydrochloride; Oxazoloazepin hydrochloride	Adrenergic Receptor	Cardiovascular Disease
Azepexole hydrochloride (B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride) is a selective agonist for *α 2-adrenoceptor, with pK_i* of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions with IC₅₀ of 78.72 nM. Azepexole hydrochloride exhibits antitussive and analgesic efficacy .

Cat. No.	Product Name	Target	Research Area

HY-P5846

Muscarinic toxin 3 MT3	mAChR Adrenergic Receptor	Neurological Disease
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and *adrenoceptors* antagonist with pIC₅₀s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M₁, M₄, α_1A, α_1B, α_1D,α_2A,α_2B and α_2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .

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α2 adrenoceptors

Inhibitors & Agonists

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