Benzazoles as allosteric potentiators of metabotropic glutamate receptor 2 (mGluR2): efficacy in an animal model for schizophrenia

Bioorg Med Chem Lett. 2005 Sep 15;15(18):4068-72. doi: 10.1016/j.bmcl.2005.06.017.

Abstract

Metabotropic glutamate receptor 2 (mGluR2) has been implicated in a variety of CNS disorders, including schizophrenia. Disclosed herein is the development of a new series of allosteric potentiators of mGluR2. Structure-activity relationship studies in conjunction with pharmacokinetic data led to the discovery of indole 5, which is active in an animal model for schizophrenia.

MeSH terms

  • Acetophenones / chemistry
  • Acetophenones / pharmacokinetics
  • Acetophenones / pharmacology*
  • Allosteric Regulation / drug effects
  • Animals
  • Brain / drug effects
  • Brain / metabolism
  • Cross-Linking Reagents / chemistry
  • Disease Models, Animal*
  • Humans
  • Ketamine / pharmacology
  • Molecular Structure
  • Rats
  • Receptors, Metabotropic Glutamate / metabolism*
  • Schizophrenia / chemically induced
  • Schizophrenia / drug therapy*
  • Schizophrenia / metabolism*
  • Structure-Activity Relationship

Substances

  • Acetophenones
  • Cross-Linking Reagents
  • Receptors, Metabotropic Glutamate
  • metabotropic glutamate receptor 2
  • Ketamine