以5-羟色胺2A受体为靶点的抗抑郁药研究进展  

Research Progress of Antidepressants Targeting Serotonin 2A Receptor

作　　者：徐祥清[1] 常山泉 XU Xiangqing;CHANG Shanquan(Jiangsu Key Laboratory of Central Nervous System Drug Research and Development,Jiangsu Nhwa Pharmaceutical Co.,Ltd,Xuzhou 221116,China)

机构地区：[1]江苏恩华药业股份有限公司江苏省中枢神经药物研究重点实验室,徐州221116

出　　处：《医药导报》2023年第7期1061-1066,共6页Herald of Medicine

基　　金：江苏省中枢神经药物研究重点实验室资助项目(BM2019004)。

摘　　要：抑郁症的发病机制非常复杂,至今尚未完全阐明。大量临床及临床前研究表明,5-羟色胺(5-HT)能神经功能障碍可能是导致抑郁症的关键因素之一。在5-HT神经系统中,除5-羟色胺转运体(SERT)外,有多种5-HT受体亚型与抑郁症有关,尤以5-HT 1A及5-HT 2A受体与抑郁症关系最为密切。5-HT 2A受体在大脑中广泛分布,是调节情绪的重要物质基础,对情绪、感知的调控具有重要作用。5-HT 2A受体可以直接或间接调节单胺类递质释放,调节脑中单胺类递质水平,参与抑郁症发病过程。5-HT 2A受体拮抗剂可以增强5-羟色胺再摄取抑制剂等抗抑郁药对难治性抑郁症的治疗效果并减少性功能障碍及睡眠障碍等不良反应。目前有不少以5-HT 2A受体为靶点的抗抑郁药应用于临床,也有大量化合物处于临床及临床前研究。该文对5-HT 2 A受体与抑郁症的关系及以5-HT 2A受体为靶点的抗抑郁药研究进展进行简要综述,以期为新型抗抑郁药物的研发提供参考。The pathogenesis of depression is highly complicated and has not been fully elucidated.Numerous clinical and preclinical studies suggested that serotonergic(5-HT)neurological dysfunction critically contributed to depression.In addition to the serotonin transporter(SERT),multiple subtype receptors in the 5-HT nervous system are related to depression.Among them,5-HT 1A and 5-HT 2A receptors are most closely associated.Brain widely distributed 5-HT 2A receptors provide a fundamental basis for regulating mood and perception.5-HT 2A receptors modulate the level of monoamine transmitters in the brain by directly or indirectly regulating monoamine transmitters'release to participate in depression development.5-HT 2A receptors antagonists enhanced the therapeutic effects of antidepressants such as selective serotonin reuptake inhibitors(SSRIs)for treatment-resistant depression and reduced adverse reactions such as sexual dysfunction and sleep disorder.Several 5-HT 2A receptor-targeted antidepressants were approved for clinical treatment,and many compounds are currently being researched in clinical or preclinical studies.This review briefly discussed the relationship between 5-HT 2A receptors and depression and summarized the research progress of antidepressants targeting 5-HT 2A receptors to provide information for antidepressant research.

关 键 词：抗抑郁药 5-HT 2A受体 抑郁症 增效 

分 类 号：R971[医药卫生—药品]