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α2A-adrenoceptor agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (14) Apoptosis (6) Autophagy (5) Drug Metabolite (1) Histamine Receptor (1) Imidazoline Receptor (5) Isotope-Labeled Compounds (2)
By Research Areas:	Cancer (7) Cardiovascular Disease (9) Endocrinology (4) Infection (1) Neurological Disease (4)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-109075A

Tasipimidine sulfate	Adrenergic Receptor	Neurological Disease
Tasipimidine sulfate is an orally active and selective *α2A-adrenoceptor* agonist with a pEC₅₀ of 7.57 against human α2A-adrenoceptor. Tasipimidine sulfate can be used for situational anxiety and fear research .

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-100490B

Rilmenidine phosphate	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cardiovascular Disease Cancer
Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an *alpha 2-adrenoceptor* agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na ⁺/H ⁺ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

HY-100490

Rilmenidine	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cardiovascular Disease Cancer
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an *alpha 2-adrenoceptor* agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na ⁺/H ⁺ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

HY-109075

Tasipimidine	Adrenergic Receptor	Neurological Disease
Tasipimidine is an orally active and selective *α_2A-adrenoceptor* agonist with a pEC₅₀ of 7.57 for human α_2A-adrenoceptors. Tasipimidine can be utilized in research related to situational anxiety and fear .

HY-17416S

Guanfacine-d2 hydrochloride	Isotope-Labeled Compounds Adrenergic Receptor	Cardiovascular Disease Endocrinology
Guanfacine-d₂ (hydrochloride) is the deuterium labeled Guanfacine hydrochloride. Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors .

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-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-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-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 .

HY-100490A

Rilmenidine hemifumarate	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cardiovascular Disease Cancer
Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an *alpha 2-adrenoceptor* agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na ⁺/H ⁺ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

HY-100490S

Rilmenidine-d4	Isotope-Labeled Compounds Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cardiovascular Disease Cancer
Rilmenidine-d₄ is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].

HY-12716

BRL-44408	Adrenergic Receptor	Endocrinology
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 .

HY-136498AR

T-705RMP (ammonium) (Standard)	Drug Metabolite	Infection
Rilmenidine (phosphate) (Standard) is the analytical standard of Rilmenidine (phosphate). This product is intended for research and analytical applications. Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

HY-100490BR

Rilmenidine (phosphate) (Standard)	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cardiovascular Disease Cancer
Rilmenidine (phosphate) (Standard) is the analytical standard of Rilmenidine (phosphate). This product is intended for research and analytical applications. Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

HY-101198

Clobenpropit dihydrobromide	Histamine Receptor Apoptosis	Neurological Disease Cancer
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC₅₀ of 8.07 for histamine H3LR . Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (K_i 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (K_i 7.4 nM) and α2A/α2C adrenoceptors (K_i 17.4/7.8 nM) . Clobenpropit dihydrobromide increases apoptosis .

Cat. No.	Product Name	Chemical Structure

HY-17416S

Guanfacine-d2 hydrochloride
Guanfacine-d₂ (hydrochloride) is the deuterium labeled Guanfacine hydrochloride. Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors .

HY-100490S

Rilmenidine-d4
Rilmenidine-d₄ is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].

Rilmenidine-d4

Rilmenidine-d₄ is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].

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