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作 者:王静 高进贤[2] 高琲[2] 葛斌[2] 吴树金[2,3] WANG Jing;GAO Jin-xian;GAO Bei;GE Bin;WU Shu-jin(College of Pharmacy,Ningxia Medical University,Yinchuan 750004;Department of Pharmacy,Gansu People’s Hospital,Lanzhou 730000;College of Pharmacy,Lanzhou University,Lanzhou 730000)
机构地区:[1]宁夏医科大学药学院,银川750004 [2]甘肃省人民医院药剂科,兰州730000 [3]兰州大学药学院,兰州730000
出 处:《中南药学》2023年第2期481-487,共7页Central South Pharmacy
基 金:甘肃省自然科学基金项目(No.20JR10RA383);兰州大学中央高校优秀研究生创新项目(No.lzujbky-2021-it37)。
摘 要:代谢型谷氨酸受体(mGluR)是G蛋白偶联受体,通过与谷氨酸这一主要中枢神经递质结合后而激活。目前已有8种不同的mGluR亚型被鉴定出来,并根据其分子结构、药理学特性和信号转导机制分为Ⅰ、Ⅱ及Ⅲ型。mGluR介导了多种生理功能,如神经元兴奋性和突触可塑性,但它们同时也参与了如疼痛等多种病理条件下的调控。mGluR广泛表达于外周及中枢痛觉调控通路中,近些年来,随着Ⅲ型mGluR新的选择性配体及正性变构调节剂的开发,使得Ⅲ型mGluR在痛觉中的生理及病理性调控作用及机制逐渐明确,提示Ⅲ型mGluR可能是治疗病理性疼痛的潜在靶点。本文就Ⅲ型mGluR在痛觉调控中的作用进行综述。Metabotropic glutamate receptors(mGluR) are G-protein coupled receptors activated by the binding of glutamate, the main classical neurotransmitter of the nervous system. Eight mGluR subtypes have been cloned and classified as groupⅠ, Ⅱ, and Ⅲ based on their molecular,pharmacological and signaling properties. Several physiological functions are mediated such as neuronal excitability and synaptic plasticity by mGluR, which also involve in numerous pathological conditions including pain. Besides mGluR are widely expressed in the peripheral and central pain pathway. The availability of new and more selective allosteric modulators has led to significant advances in our knowledge about the role of the group Ⅲ mGluR in the pathophysiological mechanism of pain, indicating group Ⅲ mGluR may be a potential target in the treatment of pathological pain. This paper reviewed the role of group ⅢmGluR in pain regulation.
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