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代谢型谷氨酸受体:治疗焦虑障碍的潜在药物靶点?

The metabotropic glutamate receptors: potential drug targets for the treatment of anxiety disorders?

机构信息

Department of Pharmacology, School of Medicine, University of Thessaly, Mezourlo, P.O. Box 1400, 411-10 Larissa, Greece.

出版信息

Eur J Pharmacol. 2014 Jan 15;723:181-4. doi: 10.1016/j.ejphar.2013.12.019. Epub 2013 Dec 18.

DOI:10.1016/j.ejphar.2013.12.019
PMID:24361306
Abstract

Anxiety-related disorders are a common public health issue. Several lines of evidence suggest that altered glutamatergic neurotransmission underlies anxiety. Thus, novel molecules targeting glutamatergic neurotransmission, such as ligands of the metabotropic glutamate receptors (mGlurs) might be promising candidates for the treatment of anxiety disorders. To date, several ligands selective for each mGlu receptor (mGlur) have been synthesized, and pharmacological significances of these compounds have been demonstrated mainly in animal models. Here we critically review advances in research of these emerging molecular targets for the treatment of anxiety, discuss their advantages over currently used anxiolytics as well as remaining challenges.

摘要

焦虑相关障碍是一个常见的公共卫生问题。有几条证据表明,谷氨酸能神经传递的改变是焦虑的基础。因此,靶向谷氨酸能神经传递的新型分子,如代谢型谷氨酸受体(mGluRs)的配体,可能是治疗焦虑障碍的有前途的候选药物。迄今为止,已经合成了几种针对每种 mGlu 受体(mGlur)的选择性配体,并且这些化合物的药理学意义主要在动物模型中得到了证实。在这里,我们批判性地回顾了这些新兴分子靶点在治疗焦虑方面的研究进展,讨论了它们相对于目前使用的抗焦虑药物的优势以及仍然存在的挑战。

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