New advances in small molecule drugs targeting NMDA receptors
文献类型：期刊论文
| 作者 | Zeng, Yue1,4,5; Qu, Zhi-yan1,5; Zhu, Qian-wen1; Wang, Hai-ying1,3; Zhou, Yu1,5; Gao, Zhao-bing1,2,5 |
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2025-11-04 |
| 页码 | 19 |
| 关键词 | |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/s41401-025-01675-8 |
| 英文摘要 | N-methyl-D-aspartate (NMDA) receptors are glutamate-gated ion channels that are ubiquitously expressed throughout the central nervous system (CNS) and serve as crucial mediators of neural development and synaptic plasticity. Dysregulation of NMDA receptor activity has been implicated in a wide spectrum of neurological and psychiatric disorders. In recent years, substantial progress has been made in the clinical development of small-molecule modulators targeting NMDA receptors. In this review, we summarize recent advances in this rapidly evolving field. Among various therapeutic indications, depression has emerged as an especially active area of investigation, with mechanistically diverse compounds ranging from broad-spectrum channel blockers (ketamine, dextromethorphan, esmethadone) to glycine site modulators (rapastinel, 4-chlorokynurenine, D-cycloserine) and allosteric modulators (apimostinel, zelquistinel), progressing through clinical pipelines. Beyond depression, NMDA receptor-targeted drug discovery is also advancing in other challenging CNS disorders, including neurodegenerative diseases (salzanemdor, NYX-458), pain (NYX-2925), epilepsy (radiprodil), and stroke (nelonemdaz, NP10679). Collectively, these developments reflect the maturation of NMDA receptor pharmacology and reaffirm the broad therapeutic potential of NMDA receptor modulation, while highlighting promising directions for future drug discovery. |
| WOS关键词 | D-ASPARTATE RECEPTOR ; TREATMENT-RESISTANT DEPRESSION ; GLYCINE MODULATORY SITE ; LONG-TERM POTENTIATION ; POSITIVE ALLOSTERIC MODULATION ; FUNCTIONAL PARTIAL AGONIST ; OPEN-CHANNEL BLOCK ; D-CYCLOSERINE ; SYNAPTIC PLASTICITY ; PRODRUG 4-CHLOROKYNURENINE |
| 资助项目 | Strategic Priority Research Program of the Chinese Academy of Sciences[XDB0830403] ; State Key Laboratory of Drug Research[SKLDR-2023-KF-01] ; State Key Laboratory of Drug Research[2021ZD0200900] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001607242100001 |
| 出版者 | NATURE PUBL GROUP |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/319730]  |
| 专题 | 国家级研究中心_原创新药研究全国重点实验室 |
| 通讯作者 | Zhou, Yu; Gao, Zhao-bing |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, Zhongshan 528400, Peoples R China 3.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China 4.Fudan Univ, Sch Pharm, Dept Pharmacol, Shanghai 200032, Peoples R China 5.Univ Chinese Acad Sci, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zeng, Yue,Qu, Zhi-yan,Zhu, Qian-wen,et al. New advances in small molecule drugs targeting NMDA receptors[J]. ACTA PHARMACOLOGICA SINICA,2025:19. |
| APA | Zeng, Yue,Qu, Zhi-yan,Zhu, Qian-wen,Wang, Hai-ying,Zhou, Yu,&Gao, Zhao-bing.(2025).New advances in small molecule drugs targeting NMDA receptors.ACTA PHARMACOLOGICA SINICA,19. |
| MLA | Zeng, Yue,et al."New advances in small molecule drugs targeting NMDA receptors".ACTA PHARMACOLOGICA SINICA (2025):19. |
入库方式： OAI收割
来源：上海药物研究所
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