Up-regulation of glutamatergic transmission in the forebrain has been associated with the symptomology of schizophrenia.  Activation of the metabotropic glutamate receptor 2 (mGluR2) regulates glutamate hyperactivity and represents a novel approach toward the treatment of the disease. Clinical proof-of-concept has been demonstrated in a Phase II study with orthosteric mGluR2/3 agonist, LY404039. Alternatively, positive allosteric modulators (potentiators) of mGluR2 may offer distinct advantages over orthosteric mGluR2/3 agonists due to their unique mode of action and selectivity. The discovery of a novel class of azabenzimidazolone-derived mGluR2 potentiators (represented by 1  ) is described herein.

Development of an amino-azabenzimidazolone class of mGluR2 positive allosteric modulators for the treatment of schizophrenia

243rd National Meeting (2012)

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