CAS 36067-72-8|Azepexole dihydrochloride
| 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 | / |
| MSDS | ChineseUSA | Flash Point | 153.9ºC |
Names
| Name | B-HT 933 dihydrochloride |
|---|
Azepexole dihydrochloride BiologicalActivity
| 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 DiseaseResearch Areas >>EndocrinologySignaling 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 |
| InChIKey | HBLPYIOKPJVFQW-UHFFFAOYSA-N |
| SMILES | CCN1CCc2nc(N)oc2CC1.Cl.Cl |
Toxicological Information
CHEMICAL IDENTIFICATION |
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
More 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... |
