Reference : Chemical Modifications on 4-Arylpiperazine-Ethyl Carboxamide Derivatives Differential...
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
Chemical Modifications on 4-Arylpiperazine-Ethyl Carboxamide Derivatives Differentially Modulate Affinity for 5-HT1A, D4.2, and alpha(2A) Receptors: Synthesis and In Vitro Radioligand Binding Studies
Graulich, Amaury [> >]
Léonard, Marc mailto [Université de Liège - ULiège > > Centre de recherches du cyclotron >]
Résimont, Mélissa [> >]
Huang, Xi-Ping [> >]
Roth, Bryan L. [> >]
Liégeois, Jean-François mailto [Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique >]
Australian Journal of Chemistry
[en] A series of substituted 4-aryl-piperazine ethyl heteroarylcarboxamides were prepared and tested in in vitro radioligand binding studies. The presence of a quinoxaline has a favourable impact in terms of serotonin 5-HT1A versus dopamine D4.2 receptor selectivity. Compounds with a 3-CF3 group at the distal phenyl ring are the most effective in terms of affinity and selectivity for 5-HT1A versus D4.2 receptors. A 4-phenyl-1,2,3,6-tetrahydropyridine in replacement of the corresponding 4-phenyl-piperazine side chain is also favourable not only for the affinity for 5-HT1A and D4.2 receptors but also in some cases for 2A-adrenoceptors.
F.R.S.-FNRS, Fonds Spéciaux pour la Recherche ULg
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