Glutamate release inhibiting properties of the novel mGlu(5) receptor antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP): complementary in vitro and in vivo evidence

Neuropharmacology. 2001 Sep;41(4):523-7. doi: 10.1016/s0028-3908(01)00091-0.

Abstract

We have previously demonstrated that neuronal release of the excitatory amino acid glutamate is facilitated by the selective activation of presynaptic Group I metabotropic autoreceptors. Here we report the release inhibiting actions of the novel mGlu(5) receptor-selective antagonist, 2-methyl-6-(phenylethynyl)-pyridine (MPEP), both in vitro and in vivo. These data provide compelling evidence for the presence of functional positive modulatory mGlu(5) subtype autoreceptors in the mammalian central nervous system.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain Chemistry / drug effects
  • Electric Stimulation
  • Excitatory Amino Acid Antagonists / pharmacology*
  • Glutamic Acid / metabolism*
  • Glycine / analogs & derivatives
  • Glycine / pharmacology
  • In Vitro Techniques
  • Male
  • Microdialysis
  • Pyridines / pharmacology*
  • Rats
  • Rats, Wistar
  • Receptors, Kainic Acid / antagonists & inhibitors*
  • Resorcinols / pharmacology

Substances

  • Excitatory Amino Acid Antagonists
  • Gluk1 kainate receptor
  • Pyridines
  • Receptors, Kainic Acid
  • Resorcinols
  • Glutamic Acid
  • 3,5-dihydroxyphenylglycine
  • 6-methyl-2-(phenylethynyl)pyridine
  • Glycine