2. Academic Validation
  3. Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1alpha metabotropic glutamate receptor

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.
E Hermans 1,  S R Nahorski,  R A Challiss
Affiliations

Affiliation

  • 1 Department of Cell Physiology and Pharmacology, University of Leicester, UK. [email protected]
PMID: 9886688 DOI: 10.1016/s0028-3908(98)00132-4
Abstract

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.

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