Document Report Card

ID: ALA2176878

Journal: J Med Chem

Title: Synthesis and biological characterization of 3-substituted 1H-indoles as ligands of GluN2B-containing N-methyl-D-aspartate receptors. Part 2.

Authors: Gitto R, De Luca L, Ferro S, Buemi MR, Russo E, De Sarro G, Chisari M, Ciranna L, Chimirri A.

Abstract: 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 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.

CiteXplore: 23140383

DOI: 10.1021/jm301508d