MPEP is a potent (IC50 = 36 nM for quisqualate-stimulated phosphoinositide hydrolysis) and selective (over mGlu1b, -2, -3, -4a, -6, -7b, and -8a) antagonist of the metabotropic glutamate receptor subtype 5 (mGlu5).1 It is a positive allosteric modulator of human mGlu4.2 MPEP inhibition of mGlu5 has been studied for the treatment of many CNS disorders including Parkinsons3,4, Fragile X syndrome5, and addiction6.
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