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5-羟色胺1A受体部分激动剂坦度螺酮在中枢神经系统疾病治疗中的作用及潜在机制。

Role of tandospirone, a 5-HT1A receptor partial agonist, in the treatment of central nervous system disorders and the underlying mechanisms.

作者信息

Huang Xuefei, Yang Jing, Yang Sijin, Cao Shousong, Qin Dalian, Zhou Ya, Li Xiaoli, Ye Yun, Wu Jianming

机构信息

Department of Clinical Pharmacy, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, 646000, China.

Laboratory of Chinese Materia Medica, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, 646000, China.

出版信息

Oncotarget. 2017 Oct 27;8(60):102705-102720. doi: 10.18632/oncotarget.22170. eCollection 2017 Nov 24.

Abstract

5-hydroxytryptamine (5-HT, serotonin) is an important neurotransmitter in the modulation of the cognitive, behavioral and psychological functions in animals and humans. Among the fourteen subtypes of 5-HT receptor, 5-HT1A receptor has been extensively studied. Tandospirone, an azapirone derivative with strong and selective agonist effect on 5-HT1A receptor, has been used for the treatment of anxiety disorders especially generalized anxiety disorder for decades. Recently, tandospirone showed the efficacy in relieving the syndromes of social anxiety disorder and post-traumatic stress disorder as well as in potentiating the effect of antidepressants in the treatment of depression in both preclinical and clinical studies. More impressively, the beneficial effect of tandospirone has been revealed on improvement of motor dysfunction of Parkinson's disease and cognitive deficits of schizophrenia either in monotherapy or in combination with other drugs. This review discusses the superiority of tandospirone in the treatment of the disorders and associated mechanisms in central nervous system from the literature.

摘要

5-羟色胺(5-HT,血清素)是调节动物和人类认知、行为及心理功能的一种重要神经递质。在5-HT受体的14种亚型中,5-HT1A受体已得到广泛研究。坦度螺酮是一种氮杂螺环酮衍生物,对5-HT1A受体具有强效且选择性的激动作用,数十年来一直用于治疗焦虑症,尤其是广泛性焦虑症。最近,在临床前和临床研究中均显示,坦度螺酮在缓解社交焦虑障碍和创伤后应激障碍症状以及增强抗抑郁药治疗抑郁症的效果方面具有疗效。更令人印象深刻的是,无论是单药治疗还是与其他药物联合使用,坦度螺酮在改善帕金森病运动功能障碍和精神分裂症认知缺陷方面的有益作用已得到揭示。本文综述从文献角度探讨坦度螺酮在治疗这些疾病方面的优势及其在中枢神经系统中的相关机制。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7d0a/5731992/aafc5e781598/oncotarget-08-102705-g001.jpg

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