MS 245 (oxalate)

MS 245 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 2.3 nM for the human recombinant receptor).{42927} It is 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). MS 245 decreases cAMP production induced by 5-HT in HEK293 cells expressing 5-HT6 (pA2 = 8.88 nM). It potentiates drug discrimination induced by (+)-amphetamine, but has no effect on cocaine or (–)-nicotine (Item No. 20887) drug discrimination in rats when administered at a dose of 5 mg/kg.{42928,42929}