[en] 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-HT1A receptors. Docking studies clearly show that hexyl and ethyl compounds favourably interact with the binding site of the active conformation of 5-HT1A 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.
Département de pharmacie / Chimie pharmaceutique ; Giga-Neurosciences / Pharmacologie
Fonds de la Recherche Scientifique-FNRS (F.R.S.-FNRS) ; Fonds Spéciaux pour la Recherche de l'Université de Liège