Methoxy-PEPy [CAS 524924-76-3]

Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM. IC50 value: 1 nM [1] Target: mGlu5R inhibitor Administration 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 [2]. 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) [3].

[524924-76-3]

C13H10N2O

210.23

COC1=CC(C#CC2=NC=CC=C2)=CN=C1

MGluR

MGluR5

98.19

DMSO : 100 mg/mL (ultrasonic)

-20°C, 3 years; 4°C, 2 years (Powder)

Room Temperature