title: The 5-HT(1A) agonism potential of substituted piperazine-ethyl-amide derivatives is conserved in the hexyl homologues: molecular modeling and pharmacological evaluation.
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.
authors.affiliation: Laboratory of Medicinal Chemistry and C.I.R.M., University of Liège , Avenue de l'Hôpital, B-4000 Liège 1, Belgium.
authors.forename: Sébastien
authors.initials: S
authors.lastname: Dilly
authors.forename: Jacqueline
authors.initials: J
authors.lastname: Scuvée-Moreau
authors.forename: Johan
authors.initials: J
authors.lastname: Wouters
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Liégeois
mesh_terms: D000200:Action Potentials / Q000187:drug effects* / Q000502:physiology; D000577:Amides / Q000737:chemistry; D000818:Animals; D001933:Brain Stem / Q000187:drug effects* / Q000502:physiology; D003198:Computer Simulation; D018360:Crystallography, X-Ray; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008297:Male; D008867:Microtomy; D010879:Piperazines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism*; D016415:Sequence Alignment; D059326:Serotonergic Neurons / Q000187:drug effects* / Q000502:physiology; D017366:Serotonin Receptor Agonists / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014422:Turkeys
chemical_list: D000577:Amides; D010879:Piperazines; D017366:Serotonin Receptor Agonists; D044282:Receptor, Serotonin, 5-HT1A