Positive allosteric modulators of metabotropic glutamate 2 receptors in schizophrenia treatment

Amr Ellaithy, Jason Younkin, Javier González-Maeso, Diomedes E. Logothetis

Research output: Contribution to journalReview articlepeer-review

48 Scopus citations

Abstract

The past two decades have witnessed a rise in the 'NMDA receptor hypofunction' hypothesis for schizophrenia, a devastating disorder that affects around 1% of the population worldwide. A variety of presynaptic, postsynaptic, and regulatory proteins involved in glutamatergic signaling have thus been proposed as potential therapeutic targets. This review focuses on positive allosteric modulation of metabotropic glutamate 2 receptors (mGlu2Rs) and discusses how recent preclinical epigenetic data may provide a molecular explanation for the discrepant results of clinical studies, further stimulating the field to exploit the promise of mGlu2R as a target for schizophrenia treatment.

Original languageEnglish
Pages (from-to)506-516
Number of pages11
JournalTrends in Neurosciences
Volume38
Issue number8
DOIs
StatePublished - 1 Aug 2015

Keywords

  • 5-HT
  • Epigenetics
  • HDAC2
  • MGluR
  • PAMs
  • Schizophrenia

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