5-HT1A and 5-HT2A ligands with anxiolytic and antipanic-like properties

A series of new benzothiazolin-2-one, benzoxazolin-2-one and benzoxazin-3-one derivatives were synthesized and their binding profile at 5-HT1A, 5-HT2A, 5-HT2C as well as D-2 and alpha(1) receptors was determined. All studied compounds displayed high to moderate affinity for both 5-HT1A and 5-HT2A receptor subtypes. Among these, one compound (29) emerged since it exhibited potent antagonist activities at 5-HT1A, 5-HT2A, D-2 and alpha(1) central receptors and showed anxiolytic and antipanic-like effects in mice. 29 is currently undergoing preclinical evaluation. (C) 1997 Elsevier Science Ltd.