张迎宾,何海冰,韩民,范孟娜,何毅,段中余
ZHANG Yingbin,HE Haibing,HAN Min,FAN Mengna,HE Yi,DUAN Zhongyu

• 1:河北工业大学化工学院
• 2:天士力控股集团有限公司研究院
• 3:创新中药关键技术国家重点实验室
• 4:沈阳药科大学药学院

摘要(Abstract)：

目的 探讨三重再摄取抑制剂(triple reuptake inhibitors, TRIs)抗抑郁药物的结构设计及其研究进展。方法 通过查阅总结近几年相关文献，综述了TRIs的化学结构、抗抑郁作用、作用机制及其发展方向等内容。结果 TRIs能同时抑制5-羟色胺(5-HT)、多巴胺(dopamine, DA)和去甲肾上腺素(noradrenaline, NE)的重吸收，从而达到快速起效的目的，其抗抑郁活性与化合物的化学结构有关，并在大量构效关系研究基础之上形成了TRIs的药效团模型，为后续的化合物设计和优化提供了指导。结论 TRIs作为多靶点的新型抗抑郁药物，特异性更强，作用更快，不良反应很少，可以弥补传统抗抑郁药物在临床应用中的不足，是新型抗抑郁药物的重点研究方向。
Objective To approach the molecular structural design and research progress of triple reuptake inhibitors(TRIs)as antidepressants.Methods This article reviewed the chemical structures, antidepressant effect, mechanism and research progress of TRIs by referring to the relevant literatures in recent years.Results TRIs can simultaneously enhance the extracellular levels of 5-hydroxytryptamine(5-HT),dopamine(DA)and norepinephrine(NE)to achieve rapid onset of antidepressant effects.Its antidepressant activity was related to the chemical structure of the compounds.The pharmacophore model of TRIs was formed based on a large number of structure-activity relationship studies, which provided guidance for the design and optimization of candidate compounds.Conclusion As novel multi-target antidepressants, TRIs have stronger specificity, faster effect and fewer adverse reactions, which can overcome the shortcomings of traditional antidepressants in clinical application, and have become an important direction of the next generation of antidepressants.

关键词(KeyWords)： 抑郁症;三重再摄取抑制剂;多巴胺;重吸收;抗抑郁药物
depression;triple reuptake inhibitors;dopamine;reabsorption;antidepressants

Abstract:

Keywords:

基金项目(Foundation):

作者(Author): 张迎宾,何海冰,韩民,范孟娜,何毅,段中余
ZHANG Yingbin,HE Haibing,HAN Min,FAN Mengna,HE Yi,DUAN Zhongyu

DOI: 10.14066/j.cnki.cn21-1349/r.2021.0268

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