Abstract
7-Hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester (CPCCOEt) has previously been shown to be a selective non-competitive antagonist at the metabotropic glutamate (mGlu) receptor subtype 1. In this study we have tested the effect of CPCCOEt on mGlu1b, the calcium sensing receptor (CaR) and a chimeric receptor consisting of the agonist binding amino-terminal domain (ATD) of CaR and the seven transmembrane (7TM) domain of mGlu1b (named Ca/1b). CPCCOEt inhibited responses of (S)-glutamic acid and Ca2+ at mGlu1b and Ca/1b, applied at EC50 values, with IC50 values of 10.2 microM and 13.4 microM, respectively, whereas it was weak as an antagonist of Ca2+ at CaR. These data provides strong evidence that CPCCOEt exerts its antagonistic effect on mGlu1 solely by binding to the 7TM domain.
| Original language | English |
|---|---|
| Journal | NeuroReport |
| Volume | 10 |
| Issue number | 18 |
| Pages (from-to) | 3923-5 |
| Number of pages | 3 |
| ISSN | 0959-4965 |
| Publication status | Published - 1999 |
Keywords
- Cell Line
- Chimera
- Chromones
- Excitatory Amino Acid Antagonists
- Protein Isoforms
- Receptors, Calcium-Sensing
- Receptors, Cell Surface
- Receptors, Metabotropic Glutamate