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MPEP GluR antagonist

Cat.No.S2809

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

Chemical Structure

Molecular Weight: 193.24

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 193.24 Formula

C14H11N

 Storage (From the date of receipt)
CAS No. 96206-92-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=NC(=CC=C1)C#CC2=CC=CC=C2

Solubility

In vitro
Batch:

DMSO : 39 mg/mL (201.82 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 39 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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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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Mechanism of Action

Features
Inactive against other group I/II/III metabotropic glutamate receptors.
Targets/IC50/Ki
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, this compound 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, it inhibits DHPG-stimulated PI hydrolysis with IC50 of 8.0 nM, 20.5 nM, and 17.9 nM, respectively. [1] This chemical positively modulates the hmGluR4 in a recombinant expression system, and the effect 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, this compound produces a dose-dependent inhibition of DHPG-induced but not AMPA-induced excitations with a rapid onset of action. Oral administration of this chemical also exhibits excellent anti-hyperalgesic activity in the Complete Freund's Adjuvant and turpentine models of inflammatory pain. [1] It (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. This compound (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. It has no effect on locomotor activity or motor coordination. [2] This chemical significantly reduces fmr1 but not wild-type center square entries and duration. In open field tests, it reduces fmr1tm1Cgr center field behavior to one indistinguishable from wild-type. It produces a significant reduction of total locomotor activity in three of four groups tested, at both 10 mg/kg and 30 mg/kg. [4]
References

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