SB 271046 is a potent, selective and orally active5-HT6 receptorantagonist with apK_iof 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 functional studies on human 5-HT6 receptors SB 271046 competitively antagonized 5-HT-induced stimulation of adenylyl cyclase activity with a pA₂of 8.71^[1].

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 (EC₅₀of 0.16 μM) and brain concentrations of 0.01-0.04 μM at C_max^[1].

451.99

C₂₀H₂₂ClN₃O₃S₂

209481-20-9

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