Interaction of CPCCOEt with a chimeric mGlu1b and calcium sensing receptor

H Bräuner-Osborne; Anders A. Jensen; P Krogsgaard-Larsen

Interaction of CPCCOEt with a chimeric mGlu1b and calcium sensing receptor

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

28 Citationer (Scopus)

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.

Originalsprog	Engelsk
Tidsskrift	NeuroReport
Vol/bind	10
Udgave nummer	18
Sider (fra-til)	3923-5
Antal sider	3
ISSN	0959-4965
Status	Udgivet - 1999

Citationsformater

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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",

}

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

SN - 0959-4965

VL - 10

SP - 3923

EP - 3925

JO - NeuroReport

JF - NeuroReport

IS - 18

ER -

Interaction of CPCCOEt with a chimeric mGlu1b and calcium sensing receptor

Abstract

Fingeraftryk

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