Structure-activity relationship studies of CNS agents, XIX: Quantitative analysis of the alkyl chain effects on the 5-HT1A and 5-HT2 receptor affinities of 4-alkyl-1-arylpiperazines and their analogs.
The 5-HT1A and 5-HT2 receptor affinity of a set of 44 N-alkylated 1-aryl-piperazines and their analogs has been analyzed: the n-hexyl derivatives were the most potent and the most selective 5-HT1A ligands of all the investigated N-alkyl homologues. The alkyl chain may stabilize the 5-HT1A receptor-ligand complex by hydrophobic forces. A set of the alkyl substituent contributions (CHT1A) for prediction of the 5-HT1A affinity of N-alkyl derivatives of 1-arylpiperazines and related compounds have been defined on the basis of the Free-Wilson analysis.
Mokrosz
J L
JL
Department of Medicinal Chemistry, Polish Academy of Sciences, Kraków.
Mokrosz
M J
MJ
Charakchieva-Minol
S
S
Paluchowska
M H
MH
Bojarski
A J
AJ
Duszyńska
B
B
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D010879:Piperazines / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D011869:Radioligand Assay; D051381:Rats; D011985:Receptors, Serotonin / Q000378:metabolism*; D018490:Serotonin Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D010879:Piperazines; D011985:Receptors, Serotonin; D018490:Serotonin Agents