SB 271046

SB 271046 is a potent, selective and orally active 5-HT6 receptor antagonist with a pK_i of 8.92-9.09. SB 271046 show >200-fold selective for the 5-HT6 receptor over other receptors, binding sites and ion channels. SB 271046 has anticonvulsant activity^[1]. In Vitro: In functional studies on human 5-HT6 receptors SB 271046 competitively antagonized 5-HT-induced stimulation of adenylyl cyclase activity with a pA₂ of 8.71^[1]. In Vivo: SB 271046 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. 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 C_max^[1].