SB357134_product_DataBase

Bioactivity	SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats[1].
Invitro	SB-357134（0.1、0.3、1 和 3 μM）浓度依赖性地抑制 5-HT 介导的 cAMP 水平升高，这在高 5-HT 浓度下是可以克服的，与竞争性拮抗作用一致[1]。
In Vivo	SB-258585 剂量依赖性地抑制特异性 [125I]SB-258585 结合[1]。SB-357134（0.03–30 mg/kg；0-24 小时；口服；单剂量）在大鼠 MEST 模型中产生有效的剂量相关抗惊厥作用，最小显著有效剂量为 0.1 mg/kg [1]。SB-357134（10 mg/kg；口服；每天两次；7 天）长期给药与对照组和SB-357134 急性给药相比，显著缩短路径长度[1]。 Animal Model:
Name	SB357134
CAS	219963-52-7
Formula	C17H18Br2FN3O3S
Molar Mass	523.21
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Stean TO, et al. Pharmacological profile of SB-357134: a potent, selective, brain penetrant, and orally active 5-HT(6) receptor antagonist. Pharmacol Biochem Behav. 2002 Apr;71(4):645-54.

PeptideDB