SB-357134

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

一种有效、选择性、口服活性和中枢神经系统渗透性 5-HT6 受体拮抗剂，pKi 为 8.5。

A potent, selective, orally active and CNS penetrant 5-HT6 receptor antagonist with pKi of 8.5, displays 1300-fold selectivity over other 13 5-HT receptor subtypes; inhibits 5-HT-stimulated cAMP accumulation in with pA2 of 7.63, enhances memory and learning following chronic administration in mice.

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Animal Model:Sprague–Dawley ratsDosage:0.03–30 mg/kgAdministration:0-24 h; p.o.; 0.03–30 mg/kgResult:Produced a potent and dose-related anticonvulsant effect in the rat MEST model, with a minimum significantly effective dose of 0.1 mg/kg. Increased seizure threshold up to 123±12% at the highest dose tested of 30 mg/kg. At 10 mg/kg, exhibited a rapid onset of action, significantly increasing seizure threshold from a control value of 21.7 to 26.7 mA at 1 h postdose. Observed Peak activity within 4–6 h postdose. With the exception of an unexplained loss of activity at 12 h, had a long duration of action of 21 h in this model.Animal Model:Sprague–Dawley rats Dosage:10 mg/kg Administration:10 mg/kg; p.o.; twice daily; 7 days Result:Significantly shortened path length when administered chronically compared to vehicle and administered acutely.

SB 357134 | SB357134

Endocrinology/Hormones

5-HT Receptor

5-HT Receptor

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219963-52-7

523.22

C17H18Br2FN3O3S

>98% (HPLC)

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O=S(C1=CC=C(OC)C(N2CCNCC2)=C1)(NC3=CC(Br)=CC(F)=C3Br)=O

N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-(piperazin-1-yl)benzene-1-sulfonamide

(-20℃)

With Ice Pack

≥ 2 years