Ⅰ型mGluRs在急性脑损伤中的作用及药物研究进展  

The role of groupⅠmGluRs in acute brain injury and advances in drug research

作　　者：侯逢生(综述) 吴超然 刘刚 廖红(审校)[1] Hou Fengsheng;Wu Chaoran;Liu Gang;Liao Hong(New Drug Screening and Pharmacodynamics Evaluation Center,State Key Laboratory of Natural Medicines,China Pharmaceutical University,Nanjing 210009)

机构地区：[1]中国药科大学多靶标天然药物全国重点实验室新药筛选与药效评价中心,南京210009

出　　处：《安徽医科大学学报》2024年第11期2052-2058,共7页Acta Universitatis Medicinalis Anhui

基　　金：国家自然科学基金项目(编号:82073831、82372577)。

摘　　要：谷氨酸受体广泛分布于中枢神经系统并参与兴奋性神经递质的传递,包括离子型谷氨酸受体和代谢型谷氨酸受体。其中代谢型谷氨酸受体(mGluRs)可调节神经元兴奋性和突触可塑性,并且被分为Ⅰ型、Ⅱ型和Ⅲ型。Ⅰ型mGluRs(mGluR1和mGluR5)在精神类疾病和神经退行性疾病中的作用已经得到了广泛研究,其在急性脑损伤中扮演的重要角色近年来更是受到了众多研究者的密切关注。多项研究证实,Ⅰ型mGluRs能够参与改善急性脑损伤中的炎症反应、细胞凋亡、神经网络紊乱以及运动功能障碍等。因此,Ⅰ型mGluRs有望成为治疗急性脑损伤的潜在有效靶点。现对Ⅰ型mGluRs在中枢神经系统的分布、功能,及其在急性脑损伤中的作用进行概述,并探讨靶向Ⅰ型mGluRs的药物开发潜力。Glutamate receptors are widely distributed in the central nervous system(CNS)and participate in the delivery of excitatory neurotransmitters,including ionotropic glutamate receptors and metabotropic glutamate receptors.Metabotropic glutamate receptors(mGluRs)regulate neuronal excitability and synaptic plasticity,and are classified into groupⅠ,ⅡandⅢ.The roles of groupⅠmGluRs in psychiatric and neurodegenerative diseases have been extensively studied,especially in the pathological progression of acute brain injury.Several studies have shown that groupⅠmGluRs can be involved in eliminating inflammatory damage,suppressing cell apoptosis,regulating neural network disorders,and promoting brain function recovery after acute brain injury.Therefore,groupⅠmGluRs have the potential to be effective targets for the treatment of acute brain injury.This paper reviews the distribution and function of groupⅠmGluRs in CNS,the pathological role in acute brain injury,and explore the potential of the development of drugs targeting groupⅠmGluRs.

关 键 词：MGLUR5 MGLUR1 负变构调节剂 正变构调节剂 急性脑损伤 

分 类 号：R741[医药卫生—神经病学与精神病学]