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α2-adrenergic receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (27) 5-HT Receptor (8) Adenylate Cyclase (1) Dopamine Receptor (5) Drug Metabolite (2) Imidazoline Receptor (1) Isotope-Labeled Compounds (1)
By Research Areas:	Cancer (1) Cardiovascular Disease (3) Endocrinology (7) Metabolic Disease (1) Neurological Disease (25)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Adrenergic Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-106444A

Fipamezole hydrochloride MPV-1730 hydrochloride; JP-1730 hydrochloride	Adrenergic Receptor	Neurological Disease
Fipamezole hydrochloride 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 hydrochloride is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease .

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-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-U00402

Fenmetozole Tosylate	Adrenergic Receptor	Neurological Disease Endocrinology
Fenmetozole Tosylate is an antagonist of the actions of ethanol, also antagonizes **α2-adrenergic receptor**, and acts as an antidepressant agent.

HY-105960

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

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-19057

Vatinoxan 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-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-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-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-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-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-136693

L-654284	Adrenergic Receptor	Neurological Disease
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 K_i 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 K_i 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 .

HY-32329S

Setiptiline-d3	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[1][2].

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-19057A

Vatinoxan hydrochloride 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-105412A

RU 52583	Adrenergic Receptor	Neurological Disease
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 .

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-106838A

Org 6906	Adrenergic Receptor	Neurological Disease
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 .

HY-122221

KUM 32	Adrenergic Receptor Adenylate Cyclase	Cardiovascular Disease
KUM 32 is a potent antagonists of epinephrine-induced platelet aggregation. KUM 32 is an adenylate cyclase activity inhibitor. KUM 32 binds to the **alpha 2 adrenergic receptor** of human platelets .

HY-103208

Benalfocin hydrochloride	Adrenergic Receptor	Metabolic Disease
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 .

HY-12717

Phentolamine 4 Publications Verification	Adrenergic Receptor	Endocrinology Cancer
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 .

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-12715S

Yohimbine-13C,d3	Adrenergic Receptor	Neurological Disease Endocrinology
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-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-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[1].

HY-12717R

Phentolamine (Standard)	Adrenergic Receptor	Endocrinology
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 .

HY-A0019R

Paliperidone (Standard)	Drug Metabolite 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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-A0019

Paliperidone 3 Publications Verification 9-Hydroxyrisperidone	Structural Classification Natural Products Source classification Endogenous metabolite	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-12710A

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

HY-A0019R

Paliperidone (Standard)	Structural Classification Natural Products Source classification Endogenous metabolite	Drug Metabolite 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 .

Cat. No.	Product Name	Chemical Structure

HY-12715S

Yohimbine-13C,d3
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-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[1][2].

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[1][2].

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[1].

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α2-adrenergic receptor antagonist

Inhibitors & Agonists

NaturalProducts

Isotope-Labeled Compounds

Natural
Products