Azepexole dihydrochloride

Names

[ Name ]:
Azepexole dihydrochloride

Biological Activity

[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 & Physical Properties

[ Density]:
1.126g/cm3

[ Boiling Point ]:
330.9ºC at 760mmHg

[ Molecular Formula ]:
C₉H₁₇Cl₂N₃O

[ Molecular Weight ]:
254.16

[ Flash Point ]:
153.9ºC

[ Exact Mass ]:
253.07500

[ PSA ]:
55.29000

[ LogP ]:
2.80040

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RQ5831345

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

CAS REGISTRY NUMBER :: 36067-72-8

LAST UPDATED :: 199712

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C9-H15-N3-O.2Cl-H

MOLECULAR WEIGHT :: 254.19

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2210 mg/kg

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

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
2

[ RTECS ]:
RQ5831345

Articles

The role of several alpha(1)- and alpha(2)-adrenoceptor subtypes mediating vasoconstriction in the canine external carotid circulation.

Br. J. Pharmacol. 132 , 1292-1298, (2001)

1. It has recently been shown that both alpha(1)- and alpha(2)-adrenoceptors mediate vasoconstriction in the canine external carotid circulation. The present study set out to identify the specific sub...

Pharmacological evidence that alpha2A- and alpha2C-adrenoceptors mediate the inhibition of cardioaccelerator sympathetic outflow in pithed rats.

Eur. J. Pharmacol. 554(2-3) , 205-11, (2007)

It has been suggested that the alpha(2)-adrenoceptors mediating cardiac sympatho-inhibition in pithed rats closely resemble the pharmacological profile of the alpha(2A)-adrenoceptor subtype. However, ...

Evidence that some imidazoline derivatives inhibit peripherally the vasopressor sympathetic outflow in pithed rats.

Auton. Neurosci. 143(1-2) , 40-5, (2008)

Imidazoline derivatives (e.g. clonidine and moxonidine) and alpha(2)-adrenoceptor agonists (e.g. B-HT 933) have been shown to inhibit sympathetically-induced [(3)H]noradrenaline release in several iso...

Related Compounds

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