5-HT(1a) and 5-HT(2A) ligands with anxiolytic and antipanic-like properties

Article abstract of DOI:10.1016/S0960-894X(97)10023-3

A series of new benzothiazolin-2-one, benzoxazolin-2-one and benzoxazin-3-one derivatives were synthesized and their binding profile at 5-HT(1A) 5-HT(2A), 5-HT(2C) as well as D₂ and α1 receptors was determined. All studied compounds displayed high to moderate affinity for both 5-HT(1A) and 5-HT(2A) receptor subtypes. Among these, one compound (29) emerged since it exhibited potent antagonist activities at 5-HT(1A), 5-HT(2A), D₂ and α₁ central receptors and showed anxiolytic and antipanic-like effects in mice. 29 is currently undergoing preclinical evaluation.