STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF CNS AGENTS .14. STRUCTURAL REQUIREMENTS FOR THE 5-HT1A AND 5-HT2A RECEPTOR SELECTIVITY OF SIMPLE 1-(2-PYRIMIDINYL)PIPERAZINE DERIVATIVES

The 5-HT1A and 5-HT2A receptor affinity of model 1-(2-pyrimidinyl)-piperazine derivatives 15-21 and 23-32 has been determined. 2-(N-Methylpiperazino)-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 ef...

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Published inPharmazie Vol. 49; no. 11; pp. 801 - 806
Main Authors MOKROSZ, JL, STREKOWSKI, L, DUSZYNSKA, B, HARDEN, DB, MOKROSZ, MJ, BOJARSKI, AJ
Format Journal Article
LanguageEnglish
Published ESCHBORN GOVI-VERLAG GMBH 01.11.1994
Subjects
Chemistry
Chemistry, Medicinal
Chemistry, Multidisciplinary
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
SYSTEM
CHAIN
AMPLIFIERS
AFFINITY
DNA
SEROTONIN
CONFORMATIONAL-ANALYSIS
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Summary:The 5-HT1A and 5-HT2A receptor affinity of model 1-(2-pyrimidinyl)-piperazine derivatives 15-21 and 23-32 has been determined. 2-(N-Methylpiperazino)-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-HT2A sites.
ISSN:0031-7144