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

J L Mokrosz; L Strekowski; B Duszyńska; D B Harden; M J Mokrosz; A J Bojarski

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

Pharmazie. 1994 Nov;49(11):801-6.

Authors

J L Mokrosz¹, L Strekowski, B Duszyńska, D B Harden, M J Mokrosz, A J Bojarski

Affiliation

¹ Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, Kraków.

PMID: 7838864

Abstract

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.

MeSH terms

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

Substances

Central Nervous System Agents
Piperazines
Receptors, Serotonin
Serotonin Antagonists