A potent

MPEP (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
219911-35-0
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

A potent, highly selective, and centrally active antagonist at the mGlu5a receptor subtype (IC50 = 36 nM); also has been reported as a positive allosteric modulator of mGluR4 at higher concentrations

Formal name: 2-methyl-6-(2-phenylethynyl)-pyridine, monohydrochloride

Synonyms: 

Molecular weight: 229.7

CAS: 219911-35-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety

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