SB357134

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]. In Vitro:SB-357134 (0.1, 0.3, 1, and 3 μM) concentration-dependently inhibits the 5-HT-mediated increased level of cAMP, which is surmountable at high 5-HT concentrations, consistent with competitive antagonism^[1]. In Vivo:SB-357134 dose-dependently inhibits the specific [125I]SB-258585 binding^[1].
SB-357134 (0.03-30 mg/kg; 0-24 h; p.o.; single dose) produces a potent and dose-related anticonvulsant effect in the rat MEST model, with a minimum significantly effective dose of 0.1 mg/kg^[1].
Chronic administration of SB-357134 (10 mg/kg; p.o.; twice daily; 7 days) significantly shortens path length compared to vehicle and acute administration of SB-357134^[1].