代谢型谷氨酸受体1(mGluR1)作为代谢型谷氨酸受体的重要成员之一,在中枢神经系统的信号传导中起着重要作用。选择性mGluR1拮抗剂可以阻断mGluR1介导的信号通路,发挥镇痛、抗焦虑、抗抑郁等一系列生理功能。目前,选择性mGluR1拮抗剂的发现和优化成为人们研究的热点。本文对近10年选择性mGluR1拮抗剂的各类结构和构效关系进行综述。 Metabotropic glutamate receptor 1 (mGluR1), as an important member of metabotropic glutamate receptors, plays an important role in the signaling of the central nervous system. Selective mGluR1 antagonists block the mGluR1-mediated signaling pathway and exert a series of physiological functions such as analgesia, anti-anxiety and anti-depression. Currently, the discovery and optimization of selective mGluR1 antagonists has become a hot research topic. This review summarizes the structure and structure-activity relationship of the selective mGluR1 antagonists in the recent 10 years.