ShanghaiTech University Knowledge Management System
| D-morphinan analogs with favorable pharmacokinetic profiles as dual-acting antidepressants | |
Ji, Jing1,4; Hu, Zhengtao5; Zheng, Fuqiang6  ; Zheng, Jiefang3,4; Cheng, Jiaxin3,4; Zayniddin, Nuriddinov3,4; Abduahadi, Safomuddin3,4; Wang, Guan7; Gong, Xudong7; Pan, Libiao7; Li, Pengcheng7; Zhao, Jiangyu1,4; Hu, Tianwen7; Zhu, Weiliang3,4; Shen, Jingshan3,4; Tian, Guanghui7; Aisa, Haji Akber1,2,4; He, Yang3,4
| |
| 2025-04-05 | |
| 发表期刊 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (IF:6.0[JCR-2023],6.1[5-Year]) |
| ISSN | 0223-5234 |
| EISSN | 1768-3254 |
| 卷号 | 287 |
| 发表状态 | 已发表 |
| DOI | 10.1016/j.ejmech.2025.117349Received |
| 摘要 | Dextromethorphan (DM) is a dual inhibitor of NMDAR and SERT (IC50 (NMDAR): IC50 (SERT) =31), but lacks therapeutic clinical value for the treatment of depression due to its low exposure in the human body. In this study, a series of d-morphinan derivatives were designed, synthesized and evaluated both in vitro and in vivo to identify dual inhibitors with improved metabolic stability. Structure-activity relationship studies revealed that a methyl group at the morphinan N-17 position is essential for maintaining SERT activity. Amino-morphinan compounds 24 and 27 exhibited moderate yet more balanced inhibitory activity against both NMDAR and SERT (1 |
| URL | 查看原文 |
| 收录类别 | SCI |
| 语种 | 英语 |
| 资助项目 | STI2030-Major Projects[2021ZD0200900] ; Fund of State Key Laboratory of Drug Research[SKLDR-2022-LH-09] |
| WOS研究方向 | Pharmacology & Pharmacy |
| WOS类目 | Chemistry, Medicinal |
| WOS记录号 | WOS:001428115600001 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 引用统计 | 正在获取...
|
| 文献类型 | 期刊论文 |
| 条目标识符 | https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/496887 |
| 专题 | 生命科学与技术学院 生命科学与技术学院_博士生 |
| 通讯作者 | Tian, Guanghui; Aisa, Haji Akber; He, Yang |
| 作者单位 | 1.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plants, Urumqi 830011, Peoples R China 2.Xinjiang Med Univ, Sch Pharm, Urumqi 830054, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 5.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China 6.Shanghai Tech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China 7.Vigonvita Shanghai Co Ltd, Shanghai 201210, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ji, Jing,Hu, Zhengtao,Zheng, Fuqiang,et al. D-morphinan analogs with favorable pharmacokinetic profiles as dual-acting antidepressants[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2025,287. |
| APA | Ji, Jing.,Hu, Zhengtao.,Zheng, Fuqiang.,Zheng, Jiefang.,Cheng, Jiaxin.,...&He, Yang.(2025).D-morphinan analogs with favorable pharmacokinetic profiles as dual-acting antidepressants.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,287. |
| MLA | Ji, Jing,et al."D-morphinan analogs with favorable pharmacokinetic profiles as dual-acting antidepressants".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 287(2025). |
| 条目包含的文件 | ||||||
| 文件名称/大小 | 文献类型 | 版本类型 | 开放类型 | 使用许可 | ||
修改评论
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。