Author/Authors :
O. Diouf، نويسنده , , P. Carato، نويسنده , , P. Depreux، نويسنده , , J. P. Bonte، نويسنده , , D. H. Caignard، نويسنده , , B. Guardiola-Lemaitre، نويسنده , , M. C. Rettori، نويسنده , , C. Belzung، نويسنده , , Daniel Lesieur، نويسنده ,
Abstract :
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 D2 and α1 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, D2 and α1 central receptors and showed anxiolytic and antipanic-like effects in mice. 29 is currently undergoing preclinical evaluation.
