The 5-HT 1A agonism potential of substituted piperazine-ethyl- amide derivatives is conserved in the hexyl homologues: Molecular modeling and pharmacological evaluation

Sébastien Dilly, Jacqueline Scuvée-Moreau, Johan Wouters, Jean François Liégeois

Research output: Contribution to journalArticlepeer-review

Abstract

In a series of carboxamide and sulphonamide alkyl (ethyl to hexyl) piperazine analogues, although the size of the linker is very different, ethyl and hexyl derivatives possess a high affinity for 5-HT 1A receptors. Docking studies clearly show that hexyl and ethyl compounds favorably interact with the binding site of the active conformation of 5-HT 1A receptors, thus confirming a possible agonist profile. This activity is effectively detected in electrophysiological experiments in which all four compounds inhibit the activity of rat dorsal raphe serotonergic neurons.

Original languageEnglish
Pages (from-to)2961-2966
Number of pages6
JournalJournal of chemical information and modeling
Volume51
Issue number11
DOIs
Publication statusPublished - 28 Nov 2011

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