page_title: Metabotropic glutamate receptor 1
section_title: Ligands
hierarchical_section_title: Metabotropic glutamate receptor 1 / Ligands
caption_attribution_description: English: Created myself using Cambridgesoft ChemDraw
context_page_description: The glutamate receptor, metabotropic 1, also known as GRM1, is a human gene which encodes the metabotropic glutamate receptor 1 protein.
context_section_description: In addition to the orthosteric  site (the site where the endogenous ligand glutamate binds) at least two distinct allosteric binding sites exist on the mGluR1. A respectable number of potent and specific allosteric ligands – predominantly antagonists/inhibitors – has been developed in recent years, although no orthosteric subtype-selective ligands have yet been discovered (2008).
  JNJ-16259685: highly potent, selective non-competitive antagonist
  R-214,127 and [³H]-analog: high-affinity,  selective allosteric inhibitor
  YM-202,074: high-affinity, selective allosteric antagonist
  YM-230,888: high-affinity, selective allosteric antagonist
  YM-298,198 and [³H]-analog: selective non-competitive antagonist
  FTIDC:  highly potent and selective allosteric antagonist/inverse agonist
  A-841,720: potent non-competitive antagonist; minor hmGluR5 binding
  VU-71: potentiator
  Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides: orally available PAMs
  Cyclothiazide: non-selective non-competitive antagonist
caption: Chemical structures of mGluR1 selective ligands.
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