Reference : The 5-HT1A agonism potential of substituted-piperazine-ethyl-amide derivatives is conser...
Scientific journals : Article
Engineering, computing & technology : Computer science
Human health sciences : Pharmacy, pharmacology & toxicology
http://hdl.handle.net/2268/99156
The 5-HT1A agonism potential of substituted-piperazine-ethyl-amide derivatives is conserved in the hexyl homologues: molecular modeling and pharmacological evaluation
English
Dilly, Sébastien mailto [Université de Liège - ULg > Département de Pharmacie / GIGA-Neuroscience > Chimie Pharmaceutique / Pharmacologie > >]
Scuvée-Moreau, Jacqueline mailto [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Pharmacologie >]
Wouters, Johan [Université de Namur > Département de Chimie > > >]
Liégeois, Jean-François mailto [Université de Liège - ULg > Département de pharmacie > Chimie pharmaceutique >]
2011
Journal of Chemical Information & Modeling
American Chemical Society
51
11
2961-2966
Yes (verified by ORBi)
International
1549-9596
1549-960X
[en] homologous series ; agonist ; GPCR ; homology modeling ; docking ; serotonergic neurons ; extracellular recordings ; brain slice ; dorsal raphe ; rat
[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
Researchers ; Professionals ; Students
http://hdl.handle.net/2268/99156

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