Design and synthesis of new potent, silent 5-HT1A antagonists by covalent coupling of aminopropanol derivatives with selective serotonin reuptake inhibitors

Authors
Perez, M Pauwels, PJ Pallard-Sigogneau, I Fourrier, C Chopin, P Palmier, C Colovray, V Halazy, S
Citation
M. Perez et al., Design and synthesis of new potent, silent 5-HT1A antagonists by covalent coupling of aminopropanol derivatives with selective serotonin reuptake inhibitors, BIOORG MED, 8(23), 1998, pp. 3423-3428
Citations number
18
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
8
Issue
23
Year of publication
1998
Pages
3423 - 3428
Database
ISI
SICI code
0960-894X(199812)8:23<3423:DASONP>2.0.ZU;2-A
Abstract
Hybrid molecules built up by covalent coupling of aminopropanol derivatives (especially pindolol) with antidepressant drugs like fluoxetine, paroxetin e or milnacipran were found to be potent and silent 5-HT1A antagonists (K-B < 1 nM for 7c and 9a). (C) 1998 Elsevier Science Ltd. All rights reserved.