Structure-activity relationship studies of CNS agents. Part 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 eff...

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Bibliographic Details
Published inPharmazie Vol. 49; no. 11; p. 801
Main Authors Mokrosz, J L, Strekowski, L, Duszyńska, B, Harden, D B, Mokrosz, M J, Bojarski, A J
Format Journal Article
LanguageEnglish
Published Germany 01.11.1994
Subjects
Alkylation
Animals
Central Nervous System Agents - chemical synthesis
Central Nervous System Agents - pharmacology
Models, Molecular
Piperazines - chemical synthesis
Piperazines - pharmacology
Radioligand Assay
Rats
Receptors, Serotonin - drug effects
Serotonin Antagonists - chemical synthesis
Serotonin Antagonists - pharmacology
Structure-Activity Relationship
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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