A potent, highly selective mGlu5a receptor antagonist
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MPEP (hydrochloride)

Item No. 14536

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-methyl-6-(2-phenylethynyl)-pyridine, monohydrochloride
CAS Number
219911-35-0
Molecular Formula
C14H11N • HCl
Formula Weight
229.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlPBS (pH 7.2): 5 mg/ml
λmax
270, 303, 331 nm
SMILES
CC1=CC=CC(C#CC2=CC=CC=C2)=N1.Cl
InChi Code
InChI=1S/C14H11N.ClH/c1-12-6-5-9-14(15-12)11-10-13-7-3-2-4-8-13;/h2-9H,1H3;1H
InChi Key
PKDHDJBNEKXCBI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $54

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    10 mg

    $91

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    25 mg

    $209

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    50 mg

    $341

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    Product Description

    Glutamate, the major excitatory neurotransmitter in the brain, acts on both ionotropic and metabotropic glutamate receptors. Excessive metabotropic glutamate receptor (mGluR) transmission has been linked to epilepsy, ischemia, pain, anxiety, and depression. Eight subtypes (1-8) and multiple splice variants of the mGluR have been identified and grouped based on their pharmacological properties. Group I mGluRs (subtypes 1 and 5) activate the phosphatidyl inositol pathway, while Group II (2 and 3) and Group III (4, 6, 7 and 8) inhibit adenylyl cyclase. MPEP is a potent, highly selective non-competitive antagonist at the mGlu5a receptor subtype (IC50 = 36 nM) while having no agonist or antagonist activities at the mGlu1b receptor at concentrations up to 30 μM.1 MPEP is centrally active following systemic administration in vivo, inducing anxiolytic-like effects in rodent models of anxiety and depression when administered at 1-30 mg/kg.1 MPEP has also been reported as a positive allosteric modulator of mGluR4 at μM concentrations.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tatarczynska, E., Klodzinska, A., Chojnacka-Wójcik, E., et al. Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist. Br. J. Pharmacol. 132(7), 1423-1430 (2001).

    2. Mathiesen, J.M., Svendsen, N., Bräuner-Osborne, H., et al. Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP. Br. J. Pharmacol. 138(6), 1026-1030 (2003).