Document Detail


Synthesis and Biological Characterization of 3-Substituted-1H-indoles as Ligands of GluN2B-containing N-Methyl-D-Aspartate Receptors. Part. 2.
MedLine Citation:
PMID:  23140383     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
In the course of the identification of new indole derivatives targeting GluN2B-subunit-containing N-methyl-D-Aspartate (NMDA) receptor, the (N-1H-indol-6-methanesulfonamide-3-yl)-2-(4-benzylpiperidin-1-yl)ethanone (10b) was identified as a potent ligand for this NMDA receptor subunit. It displays very high binding affinity (IC50 value of 8.9 nmol) for displacement of [3H]-ifenprodil thus showing improved potency with respect to the previously reported analogues as confirmed by functional assay. This finding was consistent with the docking pose of compound 10b within the binding pocket localized in the GluN1-GluN2B subunit interface of NMDA receptor tetraheteromeric complex.
Authors:
Rosaria Gitto; Laura De Luca; Stefania Ferro; Maria Rosa Buemi; Emilio Russo; Giovambattista De Sarro; Mariangela Chisari; Lucia Ciranna; Alba Chimirri
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-11-12
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  -     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-11-12     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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