Cat. No. Name Size Price Add Cart
KI3700MPEP Hydrochloride10 mg$164
MPEP Hydrochloride50 mg$460

Chemical Characteristic

Product NameMPEP Hydrochloride
CAS No.219911-35-0
Molecular Weight 229.7
FormulaC14H12ClN
Smilesc1ccc(cc1)C#Cc1cccc(n1)C Cl
Chemical Structure

Biological activities

MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, and it exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors [1]. MPEP has no appreciable agonist or antagonist activity at the closely related recombinant human mGlu1b receptor expressed in CHO-K1 cells or a purinoreceptor endogenously expressed in L(tk-) cells up to concentrations of 100 ?M. MPEP inhibits DHPG-stimulated PI hydrolysis with IC50 of 8.0 nM, 20.5 nM, and 17.9 nM, respectively. MPEP positively modulates the hmGluR4 in a recombinant expression system, and the effect of MPEP is fully dependent on the activation of the orthosteric agonist L-AP4 [2]. In vivo, it can be used by 2.5-30 mg/kg/day in rats [3].

References

[1] Kumar J, Hapidin H, Bee YT, et al. Effects of the mGluR5 antagonist MPEP on ethanol withdrawal induced anxiety-like syndrome in rats. Behav Brain Funct. 2013, 9(43).
[2] Morin N, Morissette M, Gr?goire L, et al. Chronic treatment with MPEP, an mGlu5 receptor antagonist, normalizes basal ganglia glutamate neurotransmission in L-DOPA-treated parkinsonian monkeys. Neuropharmacology. 2013, 73:216-231.
[3] Gandhi RM, Kogan CS, Messier C. 2-Methyl-6-(phenylethynyl) pyridine (MPEP) reverses maze learning and PSD-95 deficits in Fmr1 knock-out mice. Front Cell Neurosci. 2014, 6(8):70.

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