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5-羟色胺 6 受体作为一个新的治疗靶点。

The serotonin-6 receptor as a novel therapeutic target.

机构信息

Biomedical Research Institute, Korea Institute of Science and Technology, Seoul 136-791, Korea.

出版信息

Exp Neurobiol. 2011 Dec;20(4):159-68. doi: 10.5607/en.2011.20.4.159. Epub 2011 Dec 29.

DOI:10.5607/en.2011.20.4.159
PMID:22355260
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3268149/
Abstract

Serotonin (5-hydroxytryptamine, 5-HT) is an important neurotransmitter that is found in both the central and peripheral nervous systems. 5-HT mediates its diverse physiological responses through 7 different 5-HT receptor families: 5-HT(1), 5-HT(2), 5-HT(3), 5-HT(4), 5-HT(5), 5-HT(6), and 5-HT(7) receptors. Among them, the 5-HT(6) receptor (5-HT(6)R) is the most recently cloned serotonin receptor and plays important roles in the central nervous system (CNS) and in the etiology of neurological diseases. Compared to other 5-HT receptors, the 5-HT(6)R has been considered as an attractive CNS therapeutic target because it is expressed exclusively in the CNS and has no known isoforms. This review evaluates in detail the role of the 5-HT(6)R in the physiology and pathophysiology of the CNS and the potential usefulness of 5-HT(6)R ligands in the development of therapeutic strategies for the treatment of CNS disorders. Preclinical studies provide support for the use of 5-HT(6)R ligands as promising medications to treat the cognitive dysfunction associated with Alzheimer's disease, obesity, depression, and anxiety.

摘要

血清素（5-羟色胺，5-HT）是一种重要的神经递质，存在于中枢和外周神经系统中。5-HT 通过 7 种不同的 5-HT 受体家族：5-HT（1）、5-HT（2）、5-HT（3）、5-HT（4）、5-HT（5）、5-HT（6）和 5-HT（7）受体，来介导其多样化的生理反应。其中，5-HT（6）受体（5-HT（6）R）是最近克隆的血清素受体，在中枢神经系统（CNS）和神经疾病的发病机制中发挥着重要作用。与其他 5-HT 受体相比，5-HT（6）R 被认为是一个有吸引力的中枢神经系统治疗靶点，因为它仅在中枢神经系统表达，并且没有已知的同工型。本综述详细评估了 5-HT（6）R 在中枢神经系统生理和病理生理学中的作用，以及 5-HT（6）R 配体在开发治疗中枢神经系统疾病的治疗策略中的潜在用途。临床前研究为使用 5-HT（6）R 配体作为治疗与阿尔茨海默病、肥胖、抑郁和焦虑相关的认知功能障碍的有前途的药物提供了支持。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0972/3268149/2587f04109df/en-20-159-g001.jpg

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Activation of 5-HT6 receptors inhibits corticostriatal glutamatergic transmission.5-HT6 受体的激活抑制皮质纹状体谷氨酸能传递。
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ST1936 stimulates cAMP, Ca2+, ERK1/2 and Fyn kinase through a full activation of cloned human 5-HT6 receptors.ST1936 通过完全激活克隆的人 5-HT6 受体来刺激 cAMP、Ca2+、ERK1/2 和 Fyn 激酶。
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