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
[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 Center/Unit :
CIRM - Centre Interdisciplinaire de Recherche sur le Médicament - ULiège
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Graulich, Amaury
Léonard, Marc ; Université de Liège - ULiège > Centre de recherches du cyclotron
Résimont, Mélissa
Huang, Xi-Ping
Roth, Bryan L.
Liégeois, Jean-François ; Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Language :
English
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
Publication date :
2010
Journal title :
Australian Journal of Chemistry
ISSN :
0004-9425
eISSN :
1445-0038
Publisher :
Commonwealth Scientific and Industrial Research Organization Publishing, Australia
Volume :
63
Pages :
56-67
Peer reviewed :
Peer Reviewed verified by ORBi
Funders :
F.R.S.-FNRS - Fonds de la Recherche Scientifique ULg FSR - Université de Liège. Fonds spéciaux pour la recherche
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