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Interaction of CPCCOEt With a Chimeric mGlu1b and Calcium Sensing Receptor

Interaction of CPCCOEt With a Chimeric mGlu1b and Calcium Sensing Receptor

H Bräuner-Osborne, A A Jensen, P Krogsgaard-Larsen

Neuroreport. 1999 Dec 16;10(18):3923-5.

PMID: 10716234

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP179067993	CPCCOEt		179067-99-3	Price

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