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Título

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

Autor Planas, Anna M. ; López-Rodríguez, María L.
Fecha de publicación 2011
EditorAmerican Chemical Society
Citación Journal of Medicinal Chemistry 54(23): 7986-7999 (2011)
ResumenWe 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.
URI http://hdl.handle.net/10261/90597
DOI10.1021/jm2007886
Identificadoresdoi: 10.1021/jm2007886
issn: 1347-6297
e-issn: 1748-6963
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