Bisaryl cyclic ureas have been identified as high affinity 5-HT2C receptor antagonists with selectivity over 5-HT2A and 5-HT2B. Compounds such as 8 and 22 have shown oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function in rodents.
Psychiatry Centre of Excellence in Drug Discovery, GlaxoSmithkline Pharmaceuticals, Third Avenue, Harlow, Essex CM19 5AW, UK. Caroline_Goodacre@GSK.com