Dipyridyl amines: potent metabotropic glutamate subtype 5 receptor antagonists

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4350-3. doi: 10.1016/j.bmcl.2005.06.059.

Abstract

Modulation of the metabotropic glutamate subtype 5 (mGlu5) receptor may be useful in the treatment of a variety of central nervous system disorders. Herein, we report on the discovery, synthesis, and biological evaluation of dipyridyl amines as small molecule mGlu5 antagonists.

MeSH terms

  • Amines / chemical synthesis*
  • Amines / pharmacokinetics
  • Amines / pharmacology
  • Animals
  • Excitatory Amino Acid Antagonists / chemical synthesis*
  • Excitatory Amino Acid Antagonists / pharmacokinetics
  • Excitatory Amino Acid Antagonists / pharmacology
  • Pharmacokinetics
  • Pyridines / chemical synthesis
  • Pyridines / pharmacokinetics
  • Pyridines / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Amines
  • Excitatory Amino Acid Antagonists
  • Pyridines
  • Receptor, Metabotropic Glutamate 5
  • Receptors, Metabotropic Glutamate