Discovery of GluN2A subtype-selective N-methyl-D-aspartate(NMDA)receptor ligands

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外文摘要：The N-methyl-D-aspartate(NMDA)receptors,which belong to the ionotropic Glutamate receptors,constitute a family of ligand-gated ion channels.Within the various subtypes of NMDA receptors,the GluNl/2A subtype plays a significant role in central nervous system(CNS)disorders.The present article aims to provide a comprehensive review of ligands targeting GluN2A-containing NMDA receptors,encompassing negative allosteric modulators(NAMs),positive allosteric modula-tors(PAMs)and competitive antagonists.Moreover,the ligands'structure-activity relationships(SARs)and the binding models of representative ligands are also discussed,providing valuable in-sights for the clinical rational design of effective drugs targeting CNS diseases.

外文关键词：

NMDA receptorsGluN2A subtypeSubtype-selective ligandsSARsProtein ligand interactions

作者：

Liyang Jiang、Na Liu、Fabao Zhao、Boshi Huang、Dongwei Kang、Peng Zhan、Xinyong Liu

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作者单位：

Department of Medicinal Chemistry,Key Laboratory of Chemical Biology(Ministry of Education),School of Pharmaceutical Sciences,Cheeloo College of Medicine,Shandong University,Jinan 250012,China

基金：

国家自然科学基金International Postdoctoral Exchange Fellowship Program(Talent-Introduction Program)中国博士后科学基金山东省自然科学基金山东省自然科学基金

项目编号：

82204200YJ202102792022M711939ZR2022QH287ZR2022QH312

出版年：

2024

DOI：

10.1016/j.apsb.2024.01.004

药学学报(英文版)

CSTPCD

ISSN：

年,卷(期)：2024.14(5)

参考文献量114