Interaction of CPCCOEt with a chimeric mGlu1b and calcium sensing receptor

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Interaction of CPCCOEt with a chimeric mGlu1b and calcium sensing receptor. / Bräuner-Osborne, H; Jensen, Anders A.; Krogsgaard-Larsen, P.

In: NeuroReport, Vol. 10, No. 18, 1999, p. 3923-5.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Bräuner-Osborne, H, Jensen, AA & Krogsgaard-Larsen, P 1999, 'Interaction of CPCCOEt with a chimeric mGlu1b and calcium sensing receptor', NeuroReport, vol. 10, no. 18, pp. 3923-5.

APA

Bräuner-Osborne, H., Jensen, A. A., & Krogsgaard-Larsen, P. (1999). Interaction of CPCCOEt with a chimeric mGlu1b and calcium sensing receptor. NeuroReport, 10(18), 3923-5.

Vancouver

Bräuner-Osborne H, Jensen AA, Krogsgaard-Larsen P. Interaction of CPCCOEt with a chimeric mGlu1b and calcium sensing receptor. NeuroReport. 1999;10(18):3923-5.

Author

Bräuner-Osborne, H ; Jensen, Anders A. ; Krogsgaard-Larsen, P. / Interaction of CPCCOEt with a chimeric mGlu1b and calcium sensing receptor. In: NeuroReport. 1999 ; Vol. 10, No. 18. pp. 3923-5.

Bibtex

@article{2b247951d4fa4dfbab73495d3cac8a33,
title = "Interaction of CPCCOEt with a chimeric mGlu1b and calcium sensing receptor",
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.",
keywords = "Cell Line, Chimera, Chromones, Excitatory Amino Acid Antagonists, Protein Isoforms, Receptors, Calcium-Sensing, Receptors, Cell Surface, Receptors, Metabotropic Glutamate",
author = "H Br{\"a}uner-Osborne and Jensen, {Anders A.} and P Krogsgaard-Larsen",
year = "1999",
language = "English",
volume = "10",
pages = "3923--5",
journal = "NeuroReport",
issn = "0959-4965",
publisher = "Lippincott Williams & Wilkins",
number = "18",

}

RIS

TY - JOUR

T1 - Interaction of CPCCOEt with a chimeric mGlu1b and calcium sensing receptor

AU - Bräuner-Osborne, H

AU - Jensen, Anders A.

AU - Krogsgaard-Larsen, P

PY - 1999

Y1 - 1999

N2 - 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.

AB - 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.

KW - Cell Line

KW - Chimera

KW - Chromones

KW - Excitatory Amino Acid Antagonists

KW - Protein Isoforms

KW - Receptors, Calcium-Sensing

KW - Receptors, Cell Surface

KW - Receptors, Metabotropic Glutamate

M3 - Journal article

C2 - 10716234

VL - 10

SP - 3923

EP - 3925

JO - NeuroReport

JF - NeuroReport

SN - 0959-4965

IS - 18

ER -

ID: 38485419