Home Neuronal Signaling GluR antagonist MPEP For research use only.

MPEP

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.

MPEP Chemical Structure

MPEP Chemical Structure

CAS No. 96206-92-7

Purity & Quality Control

Batch: S280901 DMSO]39 mg/mL]false]Ethanol]39 mg/mL]false]Water]Insoluble]false Purity: 99.16%
99.16

MPEP Related Products

Signaling Pathway

GluR Signaling Pathways

GluR Signaling Pathway

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
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
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 fmr1tm1Cgr 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]
Animal Research 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

Chemical Information & Solubility

Molecular Weight 193.24 Formula

C14H11N
CAS No. 96206-92-7 SDF Download MPEP SDF
Smiles CC1=NC(=CC=C1)C#CC2=CC=CC=C2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 39 mg/mL ( (201.82 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 39 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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