Reference : Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus ...
Scientific journals : Article
Physical, chemical, mathematical & earth Sciences : Chemistry
Human health sciences : Pharmacy, pharmacology & toxicology
http://hdl.handle.net/2268/123901
Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors
English
Mangin, Floriane [Université de Liège - ULg > Département de Pharmacie > Chimie Pharmaceutique > >]
Dilly, Sébastien mailto [Université de Liège - ULg > Département de Pharmacie / Giga-Neurosciences > Chimie pharmaceutique / Pharmacologie > >]
Joly, Benoît mailto [Université de Liège - ULg > > > 2e an. master sc. pharma., fin spéc. prat. offici.]
Scuvée, Jacqueline mailto [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Pharmacologie >]
Evans, Jon [University of North Carolina Chapel Hill Medical School > Department of Pharmacology School of Medicine > Division of Chemical Biology and Medicinal Chemistry > >]
Setola, Vincent [University of North Carolina Chapel Hill Medical School > Department of Pharmacology School of Medicine > Division of Chemical Biology and Medicinal Chemistry > >]
Roth, Bryan [University of North Carolina Chapel Hill Medical School > Department of Pharmacology School of Medicine > Division of Chemical Biology and Medicinal Chemistry > >]
Liégeois, Jean-François mailto [Université de Liège - ULg > Département de pharmacie > Chimie pharmaceutique >]
2012
Bioorganic & Medicinal Chemistry Letters
Elsevier Science
Yes (verified by ORBi)
International
0960-894X
1464-3405
Oxford
United Kingdom
[en] WAY-100635 ; dopamine ; serotonin ; receptor ; antagonist
[en] The selectivity for 5-HT1A versus D4 receptors is significantly increased when the basic side chain of WAY-100635 is replaced by a 4-phenylpiperazine (3e) or a 4-phenyl-1,2,3,6-tetrahydropyridine moiety (3i). The 4-phenyl-1,2,3,6-tetrahydropyridine compounds (3i-l) have a higher affinity for 5-HT1A receptors than do the corresponding unsubstituted phenylpiperazine analogues (3e-h). Compounds 3e and 3i appear to be selective for 5-HT1A receptors over other relevant receptors and still behave as neutral antagonists.
CIRM-Chimie Pharmaceutique
Fonds de la Recherche Scientifique-FNRS (F.R.S.-FNRS) ; Fonds Spéciaux pour la Recherche of the University of Liège
Development of novel antipsychotic drugs
Researchers ; Professionals ; Students
http://hdl.handle.net/2268/123901
10.1016/j.bmcl.2012.05.119

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