STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF CNS AGENTS .14. STRUCTURALREQUIREMENTS FOR THE 5-HT1A AND 5-HT2A RECEPTOR SELECTIVITY OF SIMPLE1-(2-PYRIMIDINYL)PIPERAZINE DERIVATIVES

Authors
MOKROSZ JL STREKOWSKI L DUSZYNSKA B HARDEN DB MOKROSZ MJ BOJARSKI AJ
Citation
Jl. Mokrosz et al., STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF CNS AGENTS .14. STRUCTURALREQUIREMENTS FOR THE 5-HT1A AND 5-HT2A RECEPTOR SELECTIVITY OF SIMPLE1-(2-PYRIMIDINYL)PIPERAZINE DERIVATIVES, Die Pharmazie, 49(11), 1994, pp. 801-806
Citations number
25
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
Journal title
Die Pharmazie → ACNP
ISSN journal
00317144
Volume
49
Issue
11
Year of publication
1994
Pages
801 - 806
Database
ISI
SICI code
0031-7144(1994)49:11<801:SRSOCA>2.0.ZU;2-O
Abstract
The 5-HT1A and 5-HT2A receptor affinity of model 1-(2-pyrimidinyl)-pip erazine derivatives 15-21 and 23-32 has been determined. 2-(N-Methylpi perazino)-4,6-di (2-thienyl)pyrimidine 26 is a new, highly active and selective 5-HT2A receptor ligand. The topography of a molecule and the stereoelectronic effects of the thiophene rings are the major factors responsible for the high affinity and selectivity of 26 towards 5-HT2 A sites.