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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
规格:98%
分子量:254.16
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
α2-adrenoceptor agonist
CAS:36067-72-8
分子式:C9H15N3O.2HCl
分子量:254.16
纯度:98%
存储:Store at -20°C

Background:

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