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 effects of the thiophene rings are the major factors responsible for the high affinity and selectivity of 26 towards 5-HT2A sites.
Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, Kraków.
J L
JL
Mokrosz
L
L
Strekowski
B
B
Duszyńska
D B
DB
Harden
M J
MJ
Mokrosz
A J
AJ
Bojarski
D000478:Alkylation; D000818:Animals; D002491:Central Nervous System Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D008958:Models, Molecular; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects*; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D002491:Central Nervous System Agents; D010879:Piperazines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists