Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, CNRS UMR 8601, Université Paris Descartes, 45 rue des Saints Pères, 75006 Paris, France.
Bioorg Med Chem Lett. 2010 Sep 15;20(18):5552-8. doi: 10.1016/j.bmcl.2010.07.043. Epub 2010 Jul 15.
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.
我们报告了一种新型 NR2B 选择性 NMDAR 拮抗剂 LSP10-0500 的鉴定。该化合物是基于 NR2B 特异性 NMDAR 拮抗剂的定量药效基团模型的虚拟高通量筛选方法鉴定的。还描述了围绕 LSP10-0500 的 SAR 研究。
