High affinity, selective metabotropic glutamate receptor type 1 (mGlu1
) antagonist. Binds an allosteric site of the rat mGlu1
receptor with a Ki
of 4.8 nM. Inhibits mGlu1
-mediated inositol phosphates production (IC50
= 8.6 nM in rat cerebellar granule cells). Neuroprotective in vivo
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Neuroprotective effects of the selective type 1 metabotropic glutamate receptor antagonist YM-202074 in rat stroke models.
Kohara et al.
Brain Res., 2008;1191:168
Metabotropic glutamate 1 receptor: current concepts and perspectives.
Ferraguti et al.
Radiosynthesis and evaluation of [11C]YM-202074 as a PET ligand for imaging the metabotropic glutamate receptor type 1.
Yanamoto et al.