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MPEP

Catalog No. T6598   CAS 96206-92-7

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.

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MPEP Chemical Structure
MPEP, CAS 96206-92-7
Pack Size Availability Price/USD Quantity
5 mg In stock $ 35.00
10 mg In stock $ 47.00
25 mg In stock $ 98.00
50 mg In stock $ 180.00
100 mg In stock $ 289.00
200 mg In stock $ 475.00
1 mL * 10 mM (in DMSO) In stock $ 52.00
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Purity: 99.31%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Targets&IC50 mGluR5:36 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 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]
Molecular Weight 193.24
Formula C14H11N
CAS No. 96206-92-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 37 mg/mL (191.5 mM)

Ethanol: 37 mg/mL (191.5 mM)

TargetMolReferences and Literature

1. Gasparini F, et al. Neuropharmacology, 1999, 38(10), 1493-1503. 2. Tatarczyńska E, et al. Br J Pharmacol. 2001 Apr;132(7):1423-30. 3. Mathiesen JM, et al. Br J Pharmacol, 2003, 138(6), 1026-1030. 4. Yan QJ, et al. Neuropharmacology, 2005, 49(7), 1053-1066.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Glutamine Metabolism Compound Library Antidepressant Compound Library Anti-Parkinson's Disease Compound Library Inhibitor Library NO PAINS Compound Library Bioactive Compound Library Preclinical Compound Library Neurotransmitter Receptor Compound Library Neuronal Signaling Compound Library

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Keywords

MPEP 96206-92-7 Neuroscience GluR Metabotropic glutamate receptors inhibit mGluR Inhibitor inhibitor

 

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