Reference : Chemical Modifications on 4-Arylpiperazine-Ethyl Carboxamide Derivatives Differentially ...

	Document type :	Scientific journals : Article
	Discipline(s) :	Human health sciences : Pharmacy, pharmacology & toxicology
	To cite this reference:	http://hdl.handle.net/2268/1419

Title :	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
Language :	English
Author, co-author :	Graulich, Amaury [> >]
	Léonard, Marc [Université de Liège - ULg > > Centre de recherches du cyclotron >]
	Résimont, Mélissa [> >]
	Huang, Xi-Ping [> >]
	Roth, Bryan L. [> >]
	Liégeois, Jean-François [Université de Liège - ULg > Département de pharmacie > Chimie pharmaceutique >]
Publication date :	2010
Journal title :	Australian Journal of Chemistry
Volume :	63
Pages :	56-67
Audience :	International
Abstract :	[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.
Research units :	CIRM
Funders :	F.R.S.-FNRS, Fonds Spéciaux pour la Recherche ULg
Target :	Researchers ; Professionals ; Students
Permalink :	http://hdl.handle.net/2268/1419
DOI :	10.1071/CH09353

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