FUNCTIONAL-CHARACTERISTICS OF A SERIES OF N4-SUBSTITUTED 1-(2,3-DIHYDRO-1,4-BENZODIOXIN-5-YL)PIPERAZINES AS 5-HT1A RECEPTOR LIGANDS - STRUCTURE-ACTIVITY-RELATIONSHIPS

Authors
VANSTEEN BJ VANWIJNGAARDEN I RONKEN E SOUDIJN W
Citation
Bj. Vansteen et al., FUNCTIONAL-CHARACTERISTICS OF A SERIES OF N4-SUBSTITUTED 1-(2,3-DIHYDRO-1,4-BENZODIOXIN-5-YL)PIPERAZINES AS 5-HT1A RECEPTOR LIGANDS - STRUCTURE-ACTIVITY-RELATIONSHIPS, Bioorganic & medicinal chemistry letters, 8(18), 1998, pp. 2457-2462
Citations number
6
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
18
Year of publication
1998
Pages
2457 - 2462
Database
ISI
SICI code
0960-894X(1998)8:18<2457:FOASON>2.0.ZU;2-W
Abstract
The agonistic/antagonistic profile of a series of 10 N4-substituted1-( 2,3-dihydro-1,4-benzodioxin- 5-yl)piperazines is evaluated in the in v itro adenylyl cyclase assay. The profile is severely affected by the c haracteristics of the N4-substituents ranging from full agonism (benza midoethyl derivative 1), mixed agonism/antagonism (phthalimidobutyl de rivative 7) to predominantly antagonism (saccharinbutyl derivate 9). A novel full antagonist 10, as potent as WAY 100635, is obtained by sub stitution of Cl at C-7 of the benzodioxinyl moiety in 9. (C) 1998 Else vier Science Ltd. All rights reserved.