An antagonist of 5-HT6 (Ki = 2.3 nM for the human recombinant receptor), selective for 5-HT6 over 5-HT2A and 5-HT2C receptors (Kis = 130 and 23 nM, respectively), as well as 5-HT1A, 5-HT1B, 5-HT1E, 5-HT3, and 5-HT7 receptors (Kis = 720, 9,200, 4,220, 2,390, and 600 nM, respectively), decreases cAMP production induced by 5-HT in HEK293 cells expressing 5-HT6 (pA2 = 8.88 nM), potentiates drug discrimination induced by (+)-amphetamine, but has no effect on cocaine or (-)-nicotine (Item No. 20887) drug discrimination in rats at 5 mg/kg
