English   español  
Please use this identifier to cite or link to this item: http://hdl.handle.net/10261/90597
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 | DATACITE
Exportar a otros formatos:

Title

New serotonin 5-HT1A receptor agonists with neuroprotective effect against ischemic cell damage

AuthorsPlanas, Anna M. ; López-Rodríguez, María L.
Issue Date2011
PublisherAmerican Chemical Society
CitationJournal of Medicinal Chemistry 54(23): 7986-7999 (2011)
AbstractWe report the synthesis of new compounds 4–35 based on structural modifications of different moieties of previously described lead UCM-2550. The new nonpiperazine derivatives, representing second-generation agonists, were assessed for binding affinity, selectivity, and functional activity at the 5-HT1A receptor (5-HT1AR). Computational β2-based homology models of the ligand–receptor complexes were used to explain the observed structure–affinity relationships. Selected candidates were also evaluated for their potential in vitro and in vivo neuroprotective properties. Interestingly, compound 26 (2-{6-[(3,4-dihydro-2H-chromen-2-ylmethyl)amino]hexyl}tetrahydro-1H-pyrrolo[1,2-c]imidazole-1,3(2H)-dione) has been characterized as a high-affinity and potent 5-HT1AR agonist (Ki = 5.9 nM, EC50 = 21.8 nM) and exhibits neuroprotective effect in neurotoxicity assays in primary cell cultures from rat hippocampus and in the MCAO model of focal cerebral ischemia in rats.
URIhttp://hdl.handle.net/10261/90597
DOIhttp://dx.doi.org/10.1021/jm2007886
Identifiersdoi: 10.1021/jm2007886
issn: 1347-6297
e-issn: 1748-6963
Appears in Collections:(IIBB) Artículos
Files in This Item:
File Description SizeFormat 
accesoRestringido.pdf15,38 kBAdobe PDFThumbnail
View/Open
Show full item record
Review this work
 


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