产品
编 号:F259128
分子式:C20H23Cl2N3O3S2
分子量:488.45
产品类型
结构图
CAS No: 209481-24-3
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产品详情
生物活性:
SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM).
体内研究:
SB 271046 Hydrochloride (10?mg/kg; p.o.) 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.Animal Model:Male Sprague Dawley rats
Dosage:10?mg/kg
Administration:P.o.
Result:Produced 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?1 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.
体外研究:
SB 271046 Hydrochloride (SB 271046A) shows pKi values of 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and SB 271046 Hydrochloride 相关抗体: