MPEP (hydrochloride)

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Cat No: 14536

Biochemicals - Receptor Pharmacology

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 depres...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

2-methyl-6-(2-phenylethynyl)-pyridine, monohydrochloride

Correlated keywords:

96206-92-7 glutamates excitatory neurotransmitters antagonists metabotropic receptors mGluR anxiety depression mGlu5a mGluR4 non-competitives noncompetitives non competitives active subtypes mGlu5a mGlu-5a mGlu 5a anxiolytic-like anxiolytic allosterics modulators mGlu-R4 Hcl brains ionotropics transmissions epilepsy ischemia pains anxiety depressions cyclases 1 2 3 4 5 6 7 8 groups I II III adenylyl mGlu1b centrally actives in vivo rodents rats mouse mice positive

Product Overview:
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.{22822} 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.{22822} MPEP has also been reported as a positive allosteric modulator of mGluR4 at μM concentrations.{22823}

Size	5 mg
Shipping	dry ice
CAS Number	219911-35-0
Molecular Formula	C₁₄H₁₁N • HCl
SMILES	CC1=CC=CC(C#CC2=CC=CC=C2)=N1.Cl
Molecular Weight	229,7
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.39
UNSPSC code	12352100

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Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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