SB-243213 is an inverse agonist of the serotonin (5-HT) receptor subtype 5-HT2C.1 It is selective for 5-HT2C over 5-HT2A and 5-HT2B receptors (Kis = 0.001, 0.158, and 0.1 ?M, respectively) and the cytochrome P450 (CYP) isoforms CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 (IC50s = >100, 23, >100, >100, and >100 ?M, respectively). SB-243213 reduces the basal activity of 5-HT2C in HEK293 cells expressing the human 5-HT2C receptor (pKB = 9.5). It reverses mCPP-induced hypolocomotion in rats (ID50 = 0.7 mg/kg). SB-243213 (0.2-5 mg/kg) has anxiolytic-like activity in the social interaction test in rats.
1.Bromidge, S.M., Dabbs, S., Davies, D.T., et al.Biarylcarbamoylindolines are novel and selective 5-HT2C receptor inverse agonists: Identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agentJ. Med. Chem.43(6)1123-1134(2000)