Identification of a novel NR2B-selective NMDA receptor antagonist using a virtual screening approach

  • Bioorg Med Chem Lett. 2010 Sep 15;20(18):5552-8. doi: 10.1016/j.bmcl.2010.07.043.
Laetitia Mony  1 ,  Nicolas Triballeau ,  Pierre Paoletti ,  Francine C Acher ,  Hugues-Olivier Bertrand
Affiliations
  • 1. Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, CNRS UMR 8601, Université Paris Descartes, 45 rue des Saints Pères, 75006 Paris, France.
PMID: 20692832 DOI: 10.1016/j.bmcl.2010.07.043
Abstract

We report the identification of a novel NR2B-selective NMDAR antagonist with an original scaffold, LSP10-0500. This compound was identified by a virtual high-throughput screening approach on the basis of a quantitative pharmacophore model of NR2B-specific NMDAR antagonists. A SAR study around LSP10-0500 is also described.