36067-72-8

36067-72-8 structure

Name: Azepexole dihydrochloride
Chemical Name: B-HT 933 dihydrochloride
CAS Number: 36067-72-8
Molecular Formula: C₉H₁₇Cl₂N₃O
Molecular Weight: 254.16
Catalog: Signaling Pathways GPCR/G Protein Adrenergic Receptor
Create Date: 2018-12-26 17:04:41
Modify Date: 2024-01-16 18:20:30
Azepexole (B-HT 933) dihydrochloride is a potent and selective alpha 2-adrenoceptor agonist with pKis of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively[1]. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC50= 78.72 nM)[2].

Name	B-HT 933 dihydrochloride

Description	Azepexole (B-HT 933) dihydrochloride is a potent and selective alpha 2-adrenoceptor agonist with pKis of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively[1]. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC50= 78.72 nM)[2].
Related Catalog	Research Areas >> Cardiovascular Disease Research Areas >> Endocrinology Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
In Vitro	In normoglycemic rats, the sympathetically-induced vasopressor responses are dose-dependently inhibited by 1 and 3 μg/kg.min (i.v.) Azepexole dihydrochloride, with 10 and 30 μg/kg.min Azepexole dihydrochloride producing no further inhibition. In diabetic rats, the electrically-induced vasopressor responses are: (i) unchanged by 1 and 3 μg/kg.min Azepexole dihydrochloride; (ii) significantly inhibited at all frequencies of stimulation by 10 μg/kg.min B-HT 933 dihydrochloride; and (iii) similarly inhibited (i.e. supramaximal inhibition) by 30 μg/kg.min Azepexole dihydrochloride[1].
References	[1]. Altamirano-Espinoza AH, et al. Specific role of α2A - and α2B -, but not α2C -, adrenoceptor subtypes in the inhibition of the vasopressor sympathetic out-flow in diabetic pithed rats. Basic Clin Pharmacol Toxicol. 2015;117(1):31-38.

CHEMICAL NAME :: 4H-Oxazolo(4,5-d)azepin-2-amine, 5,6,7,8-tetrahydro-6-ethyl-, dihydrochloride

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4259342

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