Methoxy-PEPy

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].

Product Specifications

CAS Number

[524924-76-3]

UNSPSC

12352005

Target

MGluR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Methoxy-PEPy.html

Purity

98.19

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C13H10N2O

Molecular Weight

210.23

References & Citations

[1]Cosford ND, et al. [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. Bioorg Med Chem Lett. 2003 Feb 10;13 (3) :351-4.|[2]Anderson JJ, et al. In vivo receptor occupancy of mGlu5 receptor antagonists using the novel radioligand [3H]3-methoxy-5- (pyridin-2-ylethynyl) pyridine) . Eur J Pharmacol. 2003 Jul 18;473 (1) :35-40.|[3]Salisbury BG, et al. Inducible expression and pharmacological characterization of the mouse metabotropic glutamate 5b receptor. Eur J Pharmacol. 2008 Jan 28;579 (1-3) :34-9.