SB 271046 hydrochloride

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

SB 271046 盐酸盐是选择性、口服活性的 5-HT6 拮抗剂。

SB 271046 hydrochloride is selective, orally active 5-HT6 antagonist (pKi values are 9.02-8.92, 6.35, 6.55, 6.27 at 5-HT6, 5-HT1A, 5-HT1D and D3, and 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively) and is > 200-fold selective over 55 other receptors, enzymes and ion channels. It increases extracellular aspartate and glutamate in the frontal cortex and exhibits anticonvulsant activity (EC50: 0.16 μM).

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 < 4.99 at 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively. SB-271046 Hydrochloride competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71.

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 ratsDosage: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.

SB 271046A

Metabolic Enzyme/Protease

Transferase

5-HT6

Neurological Disease

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209481-24-3

488.45

C20H22ClN3O3S2·HCl

>98% (HPLC)

DMSO : 50 mg/mL. 102.36 mM;

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