Abstract
An amino acid, 3,5-dihydroxyphenylglycine (DHPG) induced current responses in Xenopus oocytes expressing a metabotropic glutamate receptor clone mGluR1. Apparent EC50 of DHPG for mGluR1 was slightly lower than that of (+-)-1-aminocyclopentane-trans-1,3-dicarboxylic acid (ACPD). DHPG responses were partially inhibited by 2-amino-3-phosphonopropionic acid (AP-3). DHPG had no effect on ionotropic glutamate receptors whose expression was induced in the oocytes following injection of poly(A)+ mRNA of rat brains. In hippocampal slices, DHPG produced slow excitation of pyramidal cells, resulting from a depression of Ca(2+)-dependent K+ current and a voltage-dependent K+ current. These results indicate that DHPG is a specific and potent agonist of mGluRs.
MeSH terms
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2-Amino-5-phosphonovalerate / pharmacology
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6-Cyano-7-nitroquinoxaline-2,3-dione
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Alanine / analogs & derivatives
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Alanine / pharmacology
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Animals
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Cycloleucine / analogs & derivatives
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Cycloleucine / pharmacology
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Egtazic Acid / pharmacology
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Glycine / analogs & derivatives*
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Glycine / pharmacology
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Hippocampus / drug effects
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Hippocampus / metabolism
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In Vitro Techniques
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Male
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Oocytes / drug effects
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Oocytes / metabolism
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Potassium Channels / drug effects
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Quinoxalines / pharmacology
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RNA, Messenger / biosynthesis
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Rats
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Rats, Wistar
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Receptors, Glutamate / drug effects*
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Resorcinols / pharmacology*
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Xenopus
Substances
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Potassium Channels
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Quinoxalines
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RNA, Messenger
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Receptors, Glutamate
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Resorcinols
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2-amino-3-phosphonopropionic acid
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Cycloleucine
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1-amino-1,3-dicarboxycyclopentane
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Egtazic Acid
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3,5-dihydroxyphenylglycine
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6-Cyano-7-nitroquinoxaline-2,3-dione
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2-Amino-5-phosphonovalerate
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Alanine
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Glycine