SB271046

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SB271046 是一种有效、选择性和口服活性的 5-HT6 受体拮抗剂，pKi 为 8.9，选择性比其他 5-HT 受体亚型高 200 倍。

SB271046 is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes.

In functional studies on human 5-HT6 receptors SB 271046 competitively antagonized 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71.

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 (EC50 of 0.16?μM) and brain concentrations of 0.01-0.04?μM at Cmax.

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Cell Cycle/DNA Damage

GPR

5-HT6

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209481-20-9

451.99

C20H22ClN3O3S2

>98% (HPLC)

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CC1=C(SC2=C1C=C(C=C2)Cl)S(=O)(=O)NC3=CC(=C(C=C3)OC)N4CCNCC4.Cl

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(-20℃)

With Ice Pack

≥ 2 years