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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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CHO Cells
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Chromones / pharmacology*
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Cricetinae
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Excitatory Amino Acid Antagonists / pharmacology*
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Humans
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Kinetics
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Phosphatidylinositols / metabolism*
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Quisqualic Acid / pharmacology
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Receptors, Metabotropic Glutamate / antagonists & inhibitors*
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Recombinant Proteins / antagonists & inhibitors
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Transfection
Substances
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7-(hydroxyimino)cyclopropan(b)chromen-1a-carbxoylic acid ethyl ester
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Chromones
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Excitatory Amino Acid Antagonists
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Phosphatidylinositols
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Receptors, Metabotropic Glutamate
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Recombinant Proteins
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metabotropic glutamate receptor type 1
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Quisqualic Acid