A novel orally active group 2 metabotropic glutamate receptor agonist: LY354740

Neuroreport. 1997 Apr 14;8(6):1463-6. doi: 10.1097/00001756-199704140-00027.

Abstract

Non-specific metabotropic glutamate receptor (mGluR) agonists have previously been shown to potentiate responses of spinal neurones to ionotropic glutamate receptor agonists. In this study we show that LY354740, which is a highly selective Group 2 mGluR agonist with nanomolar potency in vitro, also mimics the above effects following local ejection on spinal neurones in vivo, an action which is blocked by a Group 2 antagonist. Despite its polar nature, LY354740 is also active given either by the i.v. or the oral route (2.5-20 mg/kg) and thus will be a useful agent for investigating the role of Group 2 mGluRs both physiologically and clinically.

MeSH terms

  • Administration, Oral
  • Animals
  • Bridged Bicyclo Compounds / pharmacology*
  • Drug Evaluation, Preclinical
  • Excitatory Amino Acid Agonists / pharmacology*
  • Female
  • Injections, Intravenous
  • Injections, Spinal
  • Iontophoresis
  • Neurons / drug effects
  • Rats
  • Rats, Wistar
  • Receptors, Metabotropic Glutamate / agonists*
  • Spinal Cord / cytology
  • Spinal Cord / drug effects
  • Stereoisomerism

Substances

  • Bridged Bicyclo Compounds
  • Excitatory Amino Acid Agonists
  • Receptors, Metabotropic Glutamate
  • eglumetad