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MPEP

Name: MPEP
Brand: Selleck Chemicals
SKU: S2809
Rating: 5 (1 reviews)

Catalog No.S2809

For research use only.

MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.

CAS No. 96206-92-7

Selleck's MPEP has been cited by 1 Publication

1 Customer Review

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GluR Signaling Pathway Map

Biological Activity

Description

MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.

Features

Inactive against other group I/II/III metabotropic glutamate receptors.

Targets

mGluR5 ^[1]

36 nM

In vitro

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 μM. Furthermore, MPEP shows no appreciable agonist or antagonist activity in cAMP accumulation or [³⁵S]-GTPγS binding assays at the recombinant human group II and III metabotropic receptors (human mGlu2, -3, -4a, -6, -7b, -8a) as well as the human NMDA (NMDAR1A/2A, -1A/2B), rat AMPA (GluR3) and human kainate (GluR6) receptor subtypes. In slices of rat neonatal hippocampus, striatum, and cortex but not cerebellum, MPEP inhibits DHPG-stimulated PI hydrolysis with IC50 of 8.0 nM, 20.5 nM, and 17.9 nM, respectively. ^[1] 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. ^[3]

In vivo

When microiontophoretically applied into the brain of rats, MPEP reduces DHPG-induced excitations but not the excitations induced by AMPA. Following intravenous administration, MPEP produces a dose-dependent inhibition of DHPG-induced but not AMPA-induced excitations with a rapid onset of action. Oral administration of MPEP also exhibits excellent anti-hyperalgesic activity in the Complete Freund's Adjuvant and turpentine models of inflammatory pain. ^[1] MPEP (1-30 mg/kg) induces anxiolytic-like effects in the conflict drinking test and the elevated plus-maze test in rats as well as in the four-plate test in mice. MPEP (1-20 mg/kg) shortens the immobility time in a tail suspension test in mice, but it is inactive in the behavioural despair test in rats. MPEP has no effect on locomotor activity or motor coordination. ^[2] MPEP significantly reduces fmr1 but not wild-type center square entries and duration. In open field tests, MPEP reduces fmr1^tm1Cgr center field behavior to one indistinguishable from wild-type. MPEP produces a significant reduction of total locomotor activity in three of four groups tested, at both 10 mg/kg and 30 mg/kg. ^[4]

Protocol (from reference)

Animal Research:^[2]	Animal Models: Male Wistar rats, male Albino Swiss mice, or male C57BL/6J mice subjected to various tests Dosages: ~30 mg/kg Administration: Administered intraperitoneally (i.p.) or perorally (p.o.) at 60 minutes before the tests

References

[4] Yan QJ, et al. Neuropharmacology, 2005, 49(7), 1053-1066.

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Solubility (25°C)

In vitro


In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+5% Tween 80 For best results, use promptly after mixing. Click to purchase: PEG300 Tween 80	10mg/mL

Chemical Information

Molecular Weight	193.24
Formula	C₁₄H₁₁N
CAS No.	96206-92-7
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1=NC(=CC=C1)C#CC2=CC=CC=C2

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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