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B-HT 933 dihydrochloride
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
B-HT 933 dihydrochloride图片
CAS NO:36067-72-8
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Azepexole (B-HT 933) dihydrochloride 是一种有效的选择性 α 2-肾上腺素受体激动剂，α；2A-，α；2B-和 α；2C-肾上腺素受体亚型的 pKis 分别为 8.3、7.6 和 7.5。
Cas No.36067-72-8
别名B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride
化学名6-ethyl-5,6,7,8-tetrahydro-4H-oxazolo[4,5-d]azepin-2-amine dihydrochloride
Canonical SMILESNC1=NC2=C(CCN(CC)CC2)O1.Cl.Cl
分子式C9H15N3O.2HCl
分子量254.16
溶解度PBS (pH 7.2): 10 mg/ml
储存条件Desiccate at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 0.44 μM

The contractile effects of adrenaline and noradrenaline may be mediated by both postjunctional α2- and α2-adrenoceptors on vascular smooth muscle. B-HT 933 is a selective α2-adrenoceptor agonist.

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].

Clinical trial: Up to now, B-HT 933 is still in the preclinical development stage.

Reference:
[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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