MPEP염산염

개요Glutamate, 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. 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. MPEP has also been reported as a positive allosteric modulator of mGluR4 at μM concentrations.

용도Glutamate, 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. 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. MPEP has also been reported as a positive allosteric modulator of mGluR4 at μM concentrations.

일반 설명GRIN2B (glutamate ionotropic receptor NMDA type subunit 2B) codes for N-methyl d-aspartate receptor subtype 2B (GluN2B). It belongs to the N-methyl-D-aspartate receptor (NMDAR) gene family. It is located on chromosome 12p13.1.

정의ChEBI: A methylpyridine that coinsists of 2-methylp[yridine bearing an additional phenylethynyl group at position 6. Potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw.