Azepexole dihydrochloride  (Synonyms: B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride)

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^[1]. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC₅₀= 78.72 nM)^[2].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

254.16

C₉H₁₇Cl₂N₃O

36067-72-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]