L)ALKYL]-3-DIPHENYLMETHYLENE-2,5-PYRROLIDINEDIONES AS 5-HT1A RECEPTORLIGANDS - STUDY OF THE STERIC REQUIREMENTS OF THE TERMINAL AMIDE FRAGMENT ON 5-HT1A AFFINITY SELECTIVITY/

Authors
LOPEZRODRIGUEZ ML MORCILLO MJ ROVAT TK FERNANDEZ E SANZ AM ORENSANZ L
Citation
Ml. Lopezrodriguez et al., L)ALKYL]-3-DIPHENYLMETHYLENE-2,5-PYRROLIDINEDIONES AS 5-HT1A RECEPTORLIGANDS - STUDY OF THE STERIC REQUIREMENTS OF THE TERMINAL AMIDE FRAGMENT ON 5-HT1A AFFINITY SELECTIVITY/, Bioorganic & medicinal chemistry letters, 8(6), 1998, pp. 581-586
Citations number
28
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
6
Year of publication
1998
Pages
581 - 586
Database
ISI
SICI code
0960-894X(1998)8:6<581:LA5R>2.0.ZU;2-7
Abstract
In the present paper, we report the synthesis and the binding profile on 5-HT1A, alpha(1), and D-2 receptors of a new series of imide-arylpi perazines 3. The study oft he length of the alkyl chain and the imide substructure allows us to suggest some important differences between t he no-pharmacophoric sites of both 5-HT1A and alpha(1)-adrenergic rece ptors, which could be of great importance in order to design new selec tive ligands. (C) 1998 Elsevier Science Ltd. All rights reserved.