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

Résultats de recherche: Contribution à un journal/une revueArticleRevue par des pairs

Résumé

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.

langue originaleAnglais
Pages (de - à)2961-2966
Nombre de pages6
journalJournal of chemical information and modeling
Volume51
Numéro de publication11
Les DOIs
Etat de la publicationPublié - 28 nov. 2011

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