[CAS NO. 96206-92-7]  MPEP

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PRODUCTS SPECIFICATIONS [96206-92-7]

Catalog
SLK-S2809
Brand
Selleck
CAS
96206-92-7

DESCRIPTION [96206-92-7]

Overview

MDLMFCD03787983
Molecular Weight193.24
Molecular FormulaC14H11N
SMILESC(#CC1=CC=CC=C1)C=2N=C(C)C=CC2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM5.1749 mL25.8746 mL51.7491 mL
5 mM1.0350 mL5.1749 mL10.3498 mL
10 mM0.5175 mL2.5875 mL5.1749 mL
50 mM0.1035 mL0.5175 mL1.0350 mL

Description

MPEP is a selective receptor antagonist with 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 [S]-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. 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 -AP4.

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. 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. MPEP significantly reduces fmr1 but not wild-type center square entries and duration. In open field tests, MPEP reduces fmr1 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.


Synonyms

Pyridine, 2-methyl-6-(2-phenylethynyl)-
Pyridine, 2-methyl-6-(phenylethynyl)-
2-Picoline, 6-phenylethynyl-
2-Methyl-6-(2-phenylethynyl)pyridine
2-Methyl-6-(phenylethynyl)pyridine
MPEP