Reference : Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part I...
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
Physical, chemical, mathematical & earth Sciences : Chemistry
http://hdl.handle.net/2268/3996
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II: Influence of the substitution on the benzyl moiety on the affinity for D-2L, D-4.2, and 5-HT2A receptors
English
Carato, P. [> > > >]
Graulich, Amaury [Université de Liège - ULiège > > Chimie pharmaceutique >]
Jensen, N. [> > > >]
Roth, B. L. [> > > >]
Liégeois, Jean-François mailto [Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique >]
15-Mar-2007
Bioorganic and Medicinal Chemistry Letters
Pergamon-Elsevier Science Ltd
17
6
1570-1574
Yes (verified by ORBi)
International
0960-894X
Oxford
[en] D-4.2 receptors ; 5-HT2A receptors ; antagonist ; schizophrenia
[en] In continuation of our work on N-(piperidin-4-yl)-naphthamides, the effect of substituted benzyl groups on D-2L, D-4.2, and 5-HT2A receptor affinity was evaluated. In the 1-naphthamide series most compounds were highly selective for D-4.2 over D-2L, and 5-HT2A receptors. Halogen and methyl substitution in position 3 or 4 of the benzyl group increased D-4.2 affinity. In the 2-naphthamide series a similar high D-4.2 over D-2L selectivity was retained while 5-HT2A affinity was increased. 3-Methoxy, 3-methyl, and 4-methyl substituents were favorable for D-4.2 affinity while halogens reduced affinity. 2-Naphthamides with a 3-bromo- or a 3-methyl group were mixed D-4.2/5-HT2A ligands similar to their unsubstituted parent compound. All compounds from both series with significant affinity for D-4.2 and 5-HT2A receptors were antagonists. (c) 2007 Elsevier Ltd. All rights reserved.
Researchers ; Professionals ; Students
http://hdl.handle.net/2268/3996
10.1016/j.bmcl.2006.12.106

File(s) associated to this reference

Fulltext file(s):

FileCommentaryVersionSizeAccess
Restricted access
BMCL07b.pdfPublisher postprint140.99 kBRequest copy

Bookmark and Share SFX Query

All documents in ORBi are protected by a user license.