Metabotropic glutamate receptors and the control of chronic pain
Metabotropic glutamate receptors and the control of chronic pain
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DOI：
10.1016/j.coph.2011.10.010
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发表时间：
2012-02-01
影响因子：
4
通讯作者：
Nicoletti, Ferdinando
中科院分区：
文献类型：
--
作者：
Chiechio, Santina;Nicoletti, Ferdinando
在过去的二十年里，代谢性谷氨酸(MGlu)受体配体被研究用于治疗不同的中枢神经系统(CNS)疾病，包括焦虑、抑郁、精神分裂症和神经退行性疾病。此外，已经广泛证明mGlu受体在炎症性和神经病理性疼痛模型中都能够调节疼痛的传递。大量结合使用选择性配体和基因敲除策略的临床前研究揭示了不同mGlu受体亚型在痛觉信息调制中的作用。本文将讨论mGlu受体在疼痛敏感性中的作用，重点介绍通过靶向特定的mGlu受体亚型来实现疼痛控制的不同策略。具体地说，将讨论旨在抑制I组mGlu受体介导的信号传递和/或增强II组和11组mGlu受体信号的药物干预，以及导致mGlu2受体表达增加的表观遗传学方法。
Over the past two decades metabotropic glutamate (mGlu) receptor ligands have been investigated for their potential therapeutic effects in different disorders of the central nervous system (CNS), including anxiety, depression, schizophrenia, and neurodegenerative diseases. In addition, it has been widely demonstrated that mGlu receptors are able to modulate pain transmission both in inflammatory and neuropathic pain models. A large number of preclinical studies combining the use of selective ligands with the knockout strategy have revealed more details about the role of the different mGlu receptor subtypes in the modulation of pain information. This review will address the role of mGlu receptors in pain sensitivity focusing on different strategies to achieve pain control by targeting specific mGlu receptor subtypes. Specifically, pharmacological interventions aimed at inhibiting group I mGlu receptor-mediated signaling and/or potentiating groups II and Ill mGlu receptor signaling together with an epigenetic approach leading to an increased expression of mGlu2 receptors will be discussed.