compound introduction
Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM.IC50 value: 1 nM Target: mGlu5R inhibitorAdministration of [3H]methoxy-PEPy (50 microCi/kg i.v.) to mGlu5 receptor-deficient mice revealed binding at background levels in forebrain, whereas wild-type mice exhibited 14-fold higher binding in forebrain relative to cerebellum. The calcium transients stimulated by these agonists were potently inhibited by reference allosteric mGlu5 antagonists - 2-methyl-6-(phenylethynyl)pyridine (MPEP), 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) and 3-methoxy-5-(pyridine-2-ylethynyl)pyridine (methoxy-PEPy) (IC(50) ranges: 0.8-66 nM) Form:Solid IC50& Target:mGlu5 Receptor 1 nM (IC 50 )
