English   español  
Please use this identifier to cite or link to this item: http://hdl.handle.net/10261/44389
Share/Impact:
Statistics
logo share SHARE logo core CORE   Add this article to your Mendeley library MendeleyBASE

Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL
Exportar a otros formatos:
Title

Structural-activity relationship study on C-4 carbon atom of the CB1 antagonist SR141716: synthesis and pharmacological evaluation of 1,2,4-triazole-3-carboxamides

AuthorsJagerovic, Nadine ; Hernández-Folgado, Laura ; Alkorta, Ibon ; Goya, Pilar ; Martín, María Isabel; Dannert, María Teresa; Alsasua, Ángela; Frigola, Jordi; Cuberes, María Rosa; Dordal, Alberto; Holenz, Jörg
Keywords1,2,4-Triazole
Cannabinoid
Mouse vas deferens
SR141716
Issue DateJan-2006
PublisherElsevier
CitationEuropean Journal of Medicinal Chemistry 41 : 114–120 (2006)
AbstractA series of 1,2,4-triazole-3-carboxamides has been prepared from alkyl-1,2,4-triazole-3-carboxylates under mild conditions. The ability of these triazoles to displace [3H]-CP55940 from CB1 cannabinoid receptor was measured. However, they showed only poor to moderate binding affinities, indicating that substitution of the C-4 pyrazole atom of the CB1 reference compound SR141716 by a nitrogen atom results in loss of affinity. Further investigations for functionality indicated that the compound 6a exhibited significant cannabinoid antagonistic properties in the mouse vas deferens functional assay. This leads us to the conclusion that 6a binds at a different CB1 binding site or at a new cannabinoid receptor subtype.
Publisher version (URL)http://dx.doi.org/10.1016/j.ejmech.2005.06.012
URIhttp://hdl.handle.net/10261/44389
DOI10.1016/j.ejmech.2005.06.012
ISSN0223-5234
Appears in Collections:(IQM) Artículos
Files in This Item:
There are no files associated with this item.
Show full item record
Review this work
 

Related articles:


WARNING: Items in Digital.CSIC are protected by copyright, with all rights reserved, unless otherwise indicated.