B-HT 933 DIHYDROCHLORIDE
B-HT 933 DIHYDROCHLORIDE Basic information
- Product Name:
- B-HT 933 DIHYDROCHLORIDE
- Synonyms:
-
- 2-amino-6-ethyl-4,5,7,8-tetrahydro-6h-oxazolo(5,4-d)azepinedihydrochloride
- 5,6,7,8-tetrahydro-6-ethyl-4h-oxazolo(4,5-d)azepin-2-aminedihydrochloride
- 5-d)azepin-2-amine,5,6,7,8-tetrahydro-6-ethyl-4h-oxazolo(dihydrochloride
- b-ht933
- B-HT 933 DIHYDROCHLORIDE SELECTIVE A2 AD RENORE
- Azepexole dihydrochloride, 6-Ethyl-5,6,7,8-tetrahydro-4H-oxazolo[4,5-d]azepin-2-amine dihydrochloride
- Azepexole hydrochloride
- Nsc310831
- CAS:
- 36067-72-8
- MF:
- C9H16ClN3O
- MW:
- 217.7
- Mol File:
- 36067-72-8.mol
B-HT 933 DIHYDROCHLORIDE Chemical Properties
- storage temp.
- Desiccate at RT
- solubility
- H2O: >20 mg/mL
- form
- solid
- color
- white to off-white
B-HT 933 DIHYDROCHLORIDE Usage And Synthesis
Description
B-HT 933 is an agonist of α2-adrenergic receptors (α2-ARs) with an EC50 value of 0.65 μM for contraction of canine sapheneous veins. It induces concentration-dependent inhibition of the twitch response in rat vas deferens and guinea pig ileum. B-HT 933 induces sedation and reduces motor activity in mice, an effect that is reversed by the α2-AR antagonist yohimbine . B-HT 933 decreases blood pressure and cardiac output in cats injected with 30 μg/kg intracisternally. It also exhibits antinociceptive effects in mice with ED50 values of 12.5, 20.5, and 6.1 mg/kg for the tail-immersion, tail-pinch, and acetic acid writhing tests, respectively.
Uses
B-HT 933 Dihydrochloride is a selective α2-adrenoceptor agonist and has less potent inhibitory effect on the sympathetic vasopressor responses in diabetic rats.
in vitro
b-ht 933, a selective α2-adrenoceptor agonist, contracts human subcutaneous resistance arteries by a mechanism largely dependent on the influx of extracellular ca2+, probably through voltage-operated calcium channels. this action involves a pertussis toxin-sensitive g protein, possibly gq [1].
in vivo
the dose-related effects of the selective α2-adrenoceptor agonist b-ht 933 on the body temperature of untreated and reserpine-treated mice were investigated. in untreated mice b-ht 933 induced a dose-related hypothermia. the highest dose of b-ht 933 elicited a marked hypothermia, whereas the maximal hypothermic effect of clonidine was less pronounced and reached a plateau at a dose of 0.5 mg/kg [2].
IC 50
0.44 μm
storage
Desiccate at RT
References
[1] n. a. parkinson & a.d. hughes. the mechanism of action of 1c2-adrenoceptors in human isolated subcutaneous resistance arteries. british journal of pharmacology (1995) 115, 1463-1468
[2] d. j. bill, i.e. hughes & r.j. stephens. the thermogenic actions of x2-adrenoceptor agonists in reserpinized mice are mediated via a central postsynaptic ac2-adrenoceptor mechanism. br. j. pharmacol. (1989), 96, 133-143
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