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SB 271046
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。
SB 271046图片
CAS NO:209481-20-9
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
SB 271046 是一种有效的、选择性的、具有口服活性的5-HT6受体拮抗剂,pKi为 8.92-9.09。SB 271046 对 5-HT6 受体的选择性比其他受体、结合位点和离子通道高 200 倍以上。SB 271046 具有抗惊厥活性。
生物活性

SB 271046 is a potent, selective and orally active5-HT6 receptorantagonist with apKiof 8.92-9.09. SB 271046 show >200-fold selective for the 5-HT6 receptor over other receptors, binding sites and ion channels. SB 271046 has anticonvulsant activity[1].

IC50& Target[1]

5-HT6Receptor

8.92-9.09 (pKi)

体外研究
(In Vitro)

In functional studies on human 5-HT6 receptors SB 271046 competitively antagonized 5-HT-induced stimulation of adenylyl cyclase activity with a pA2of 8.71[1].

体内研究
(In Vivo)

SB 271046 produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ?0.1 mg/kg p.o. and maximum effect at 4 h post-dose. The level of anticonvulsant activity achieved correlated well with the blood concentrations of SB 271046 (EC50of 0.16 μM) and brain concentrations of 0.01-0.04 μM at Cmax[1].

分子量

451.99

Formula

C20H22ClN3O3S2

CAS 号

209481-20-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.