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Cipralisant(GT-2331)
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。
Cipralisant(GT-2331)图片
CAS NO:213027-19-1
包装与价格:
包装价格(元)
250mg电议
500mg电议

产品介绍
Cipralisant (GT-2331) (GT-2331) 是一种具有口服活性、低毒、强效、选择性、高亲和力组胺 H3 受体的体内完全拮抗剂,在体外是一种激动剂,对组胺 H3 受体的 pKi 为 9.9,大鼠组胺 H3 受体的 Ki 为 0.47 nM。
Cas No.213027-19-1
别名GT-2331
Canonical SMILESCC(C)(C)CCC#C[C@H]1[C@H](C2=CN=CN2)C1
分子式C14H20N2
分子量216.32
溶解度Soluble in DMSO
储存条件Store at -20°C
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

Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has entered in clinical trials for the treatment of attention-deficit hyperactivity disorder.

Cipralisant (GT-2331) is a potent histamine H3 receptor antagonist with a pKi of 9.9[1] and a Ki of 0.47 nM for rat histamine H3 receptor[2]. Cipralisant acts as a full agonist at the recombinant rat histamine H3 receptor in vitro, and potently inhibits forskolin-induced cAMP accumulation with an EC50 of 0.23 nM. Cipralisant increases the basal [35S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC50, 5.6 nM)[2].

Cipralisant (GT-2331) acts as an antagonist of histamine H3 receptor, and blocks R-α-methylhistamine (a histamine H3 receptor agonist)-induced water intake at 10 mg/kg via oral administration in rats[2].

[1]. Tedford CE, et al. High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models. Eur J Pharmacol. 1998 Jun 26;351(3):307-11. [2]. Ito S, et al. Detailed pharmacological characterization of GT-2331 for the rat histamine H3 receptor. Eur J Pharmacol. 2006 Jan 4;529(1-3):40-6.