4-Carboxy-3-hydroxyphenylglycine, an antagonist at type I metabotropic glutamate receptors.
The pharmacology of (DL)-4-carboxy-3-hydroxyphenylglycine was examined in baby hamster kidney cells which stably express the type I metabotropic glutamate receptor (mGluR1 alpha). DL-4-Carboxy-3-hydroxyphenylglycine dose-dependently inhibited glutamate-stimulated phosphoinositide hydrolysis in a competitive manner with a KB of 29 microM as estimated from Schild-plot analysis. The present report is the first demonstration of a potent and competitive antagonist of the mGluR1 alpha subtype.
Thomsen
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Department of Receptor Neurochemistry, Novo Nordisk A/S, Måløv, Denmark.
Suzdak
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PD
D000818:Animals; D002460:Cell Line; D006224:Cricetinae; D004305:Dose-Response Relationship, Drug; D018691:Excitatory Amino Acid Antagonists; D005998:Glycine / Q000031:analogs & derivatives* / Q000494:pharmacology; D006868:Hydrolysis; D010716:Phosphatidylinositols / Q000378:metabolism*; D017470:Receptors, Glutamate / Q000378:metabolism
D018691:Excitatory Amino Acid Antagonists; D010716:Phosphatidylinositols; D017470:Receptors, Glutamate; C078245:4-carboxy-3-hydroxyphenylglycine; D005998:Glycine