Azepexole dihydrochloride

Modify Date: 2024-01-16 18:20:30

Azepexole dihydrochloride Structure
Azepexole dihydrochloride structure
Common Name Azepexole dihydrochloride
CAS Number 36067-72-8 Molecular Weight 254.16
Density 1.126g/cm3 Boiling Point 330.9ºC at 760mmHg
Molecular Formula C9H17Cl2N3O Melting Point N/A
MSDS Chinese USA Flash Point 153.9ºC

 Use of Azepexole dihydrochloride


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].

 Names

Name B-HT 933 dihydrochloride

 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
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

 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

 Articles27

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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...