YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 ( mGluR1 ) antagonist with high affinity. YM-202074 fumarate binds to the allosteric site of rat mGluR1 with a K i of 4.8 nM. YM-202074 fumarate also inhibits mGluR1 -mediated inositol phosphate production in rat cerebellar granule cells with an IC 50 of 8.6 nM. YM-202074 fumarate has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models.
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