A group II mGluR inhibitor (EC50s = 2.69 and 4.48 nM

LY379268 – 5 mg

Brand:
Cayman
CAS:
191471-52-0
Storage:
4
UN-No:
Non-Hazardous - /

LY379268 is a potent, brain-permeable, and selective agonist of group II metabotropic glutamate receptors (mGluRs), subtypes mGluR2 and mGluR3.{34626} In an assay of second messenger response, LY379268 exhibits EC50 values of 2.69 and 4.48 nM for human mGluR2 and mGluR3, respectively, with at least 80-fold selectivity over group I and III mGluRs.{34626} In a displacement assay, LY379268 displays no agonist or antagonist activity against NMDA, AMPA, or kainate receptors up to a concentration of 100 µM.{34626} However, it may influence the level of AMPA receptor trafficking in rat prefrontal cortical neurons.{34629} LY379268 confers a neuroprotective effect to the CA1 of the hippocampus in a gerbil model of induced ischemia at a dose of 10 mg/kg.{34627} In rats, LY379268 (3 mg/kg) raises the extracellular dopamine level to 168% of the basal level in the prefrontal cortex.{34628}  

 

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Description

A group II mGluR inhibitor (EC50s = 2.69 and 4.48 nM, respectively for mGluR2 and mGluR3); over 80-fold selectivity over group I and III mGluRs; no agonist or antagonist activity against NMDA, AMPA, or kainate receptors up to a concentration of 100 µM; raises extracellular dopamine level in the prefrontal cortex to 168% basal level in treated rats (3 mg/kg)

Formal name: (1R,4R,5S,6R)-4-amino-2-oxabicyclo[3.1.0]hexane-4,6-dicarboxylic acid

Synonyms: 

Molecular weight: 187.2

CAS: 191471-52-0

Purity: ≥99%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Neuroprotection|Ischemia

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