The identification of novel orally active mGluR5 antagonist GSK2210875

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7521-4. doi: 10.1016/j.bmcl.2010.09.120. Epub 2010 Nov 2.

Abstract

The identification of novel orally active mGluR5 antagonist GSK2210875 is described.

MeSH terms

  • Administration, Oral
  • Allosteric Regulation
  • Animals
  • Brain / drug effects
  • Brain / metabolism
  • Heterocyclic Compounds, 3-Ring / chemical synthesis
  • Heterocyclic Compounds, 3-Ring / chemistry*
  • Heterocyclic Compounds, 3-Ring / pharmacokinetics
  • Mice
  • Rats
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate / antagonists & inhibitors*
  • Receptors, Metabotropic Glutamate / metabolism
  • Structure-Activity Relationship

Substances

  • GSK2210875
  • Grm5 protein, mouse
  • Grm5 protein, rat
  • Heterocyclic Compounds, 3-Ring
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate