Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1alpha metabotropic glutamate receptor

Neuropharmacology. 1998 Dec;37(12):1645-7. doi: 10.1016/s0028-3908(98)00132-4.


In transfected CHO cells expressing the human metabotropic glutamate receptor mGlu1alpha, 7-(hydroxyimino)cyclopropan[b]-chromen-1a-carboxylic acid ethylester (CPCCOEt) was found to antagonize L-quisqualate-induced phosphoinositide hydrolysis in a non-competitive and reversible manner (apparent pKi value, 4.76+/-0.18; n=3). This suggests that CPCCOEt antagonizes type 1alpha metabotropic glutamate receptor activation by interacting with a site distinct from the agonist binding site.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CHO Cells
  • Chromones / pharmacology*
  • Cricetinae
  • Excitatory Amino Acid Antagonists / pharmacology*
  • Humans
  • Kinetics
  • Phosphatidylinositols / metabolism*
  • Quisqualic Acid / pharmacology
  • Receptors, Metabotropic Glutamate / antagonists & inhibitors*
  • Recombinant Proteins / antagonists & inhibitors
  • Transfection


  • 7-(hydroxyimino)cyclopropan(b)chromen-1a-carbxoylic acid ethyl ester
  • Chromones
  • Excitatory Amino Acid Antagonists
  • Phosphatidylinositols
  • Receptors, Metabotropic Glutamate
  • Recombinant Proteins
  • metabotropic glutamate receptor type 1
  • Quisqualic Acid