Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1804-9. doi: 10.1016/j.bmcl.2008.02.024. Epub 2008 Feb 14.

Abstract

The synthesis and the structure activity of a new series of pyrrolo[1,2-a]pyrazine is reported. These molecules are potent and selective non-competitive mGluR5 antagonists and may shed new light on the pattern of substitution tolerated by this receptor.

MeSH terms

  • Dopamine Plasma Membrane Transport Proteins / antagonists & inhibitors
  • Fluorescence
  • Humans
  • Molecular Structure
  • Norepinephrine Plasma Membrane Transport Proteins / antagonists & inhibitors
  • Pyrazines / chemical synthesis
  • Pyrazines / pharmacology*
  • Pyrroles / chemical synthesis
  • Pyrroles / pharmacology*
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Dopamine Plasma Membrane Transport Proteins
  • GRM5 protein, human
  • Norepinephrine Plasma Membrane Transport Proteins
  • Pyrazines
  • Pyrroles
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate