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Description: SB271046 (SB 271046; SB-271046; SB-271046A; SB271046A) is a novel, potent, selective and orally bioactive 5-HT6 receptor antagonist with important biological activity. It inhibits 5-HT6 with a pKi of 8.9, and exhibits 200-fold greater selectivity over other 5-HT receptor subtypes. SB-271046 substituted 125I-SB-258585 and 3H-LSD from human 5-HT6 receptors which recombinantly expressed in HeLa cells in vitro. SB-271046 also transfered 125I-SB-258585 from human caudate putamen and rat and pig striatum membranes. By 5-HT alone or after increasing concentrations of SB-271046 (10, 30, 100 and 300 nM) stimulates adenylyl cyclase activity in HeLa cells stably expressing human 5-HT6 receptors.
References: Br J Pharmacol. 2000 Aug; 130(7):1606-12; J Med Chem. 1999 Jan 28; 42(2):202-5.
Related CAS: 209481-24-3 (HCl salt)
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