191471-52-0

LY 379268 is a group II metabotropic glutamate receptors (mGlu2/3) receptor agonist (1,2). Studies have shown that LY379268 significantly attenuated cocaine-induced increases in DA in nonhuman primates.

ChEBI: LY 379268 is an organic heterobicyclic compound that is (1R,5S)-2-oxabicyclo[3.1.0]hexane carrying amino, carboxy, and carboxy groups at positions 4R, 4R and 6R, respectively. It is a potent agonist of group II metabotropic glutamate receptors mGluR2 and mGluR3 (EC50 = 2.69 nM and 4.48 nM, respectively) that exhibits antipsychotic-like action in animal models of schizophrenia. It has a role as a metabotropic glutamate receptor agonist, a neuroprotective agent, an antipsychotic agent and an anxiolytic drug. It is an organic heterobicyclic compound, a bridged compound and an amino dicarboxylic acid.

Highly selective group II mGlu receptor agonist (EC 50 values are 2.69 and 4.48 nM for hmGlu 2 and hmGlu 3 respectively) that displays > 80-fold selectivity over group I and group III receptors. Provides protection against NMDA-mediated cell death in vitro and offers almost complete protection against CA1 hippocampal damage following global ischemia in gerbils. Orally and systemically active.

hmGluR2: 2.69 nM (EC₅₀); hmGluR3: 4.48 nM (EC₅₀); hmGluR2: 14.1 nM (Ki); hmGluR3: 5.8 nM (Ki)

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