As an important member of metabotropic glutamate receptors (mGluR), metabotropic glutamate receptor 1 (mGluR1) plays an important role in the signal transduction of central nervous system.  Selective mGluR1 antagonists can block the signaling pathway activated by mGluR1 and exert a series of physiological actions including analgesia, antianxiety, antidepression, etc.  Currently, the discovery and modification of selective mGluR1 antagonists have become a hot research focus.  This paper reviews the structural catalogs of selective mGluR1 antagonists and their structure-activity relationships in the last decade.