5-HT1A AND 5-HT2A LIGANDS WITH ANXIOLYTIC AND ANTIPANIC-LIKE PROPERTIES

Authors
DIOUF O CARATO P DEPREUX P BONTE JP CAIGNARD DH GUARDIOLALEMAITRE B RETTORI MC BELZUNG C LESIEUR D
Citation
O. Diouf et al., 5-HT1A AND 5-HT2A LIGANDS WITH ANXIOLYTIC AND ANTIPANIC-LIKE PROPERTIES, Bioorganic & medicinal chemistry letters, 7(20), 1997, pp. 2579-2584
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
20
Year of publication
1997
Pages
2579 - 2584
Database
ISI
SICI code
0960-894X(1997)7:20<2579:5A5LWA>2.0.ZU;2-9
Abstract
A series of new benzothiazolin-2-one, benzoxazolin-2-one and benzoxazi n-3-one derivatives were synthesized and their binding profile at 5-HT 1A, 5-HT2A, 5-HT2C as well as D-2 and alpha(1) receptors was determine d. All studied compounds displayed high to moderate affinity for both 5-HT1A and 5-HT2A receptor subtypes. Among these, one compound (29) em erged since it exhibited potent antagonist activities at 5-HT1A, 5-HT2 A, D-2 and alpha(1) central receptors and showed anxiolytic and antipa nic-like effects in mice. 29 is currently undergoing preclinical evalu ation. (C) 1997 Elsevier Science Ltd.