3,5-Dihydroxyphenyl-glycine: a potent agonist of metabotropic glutamate receptors

Neuroreport. 1992 Nov;3(11):1013-6.

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

  • 2-Amino-5-phosphonovalerate / pharmacology
  • 6-Cyano-7-nitroquinoxaline-2,3-dione
  • Alanine / analogs & derivatives
  • Alanine / pharmacology
  • Animals
  • Cycloleucine / analogs & derivatives
  • Cycloleucine / pharmacology
  • Egtazic Acid / pharmacology
  • Glycine / analogs & derivatives*
  • Glycine / pharmacology
  • Hippocampus / drug effects
  • Hippocampus / metabolism
  • In Vitro Techniques
  • Male
  • Oocytes / drug effects
  • Oocytes / metabolism
  • Potassium Channels / drug effects
  • Quinoxalines / pharmacology
  • RNA, Messenger / biosynthesis
  • Rats
  • Rats, Wistar
  • Receptors, Glutamate / drug effects*
  • Resorcinols / pharmacology*
  • Xenopus

Substances

  • Potassium Channels
  • Quinoxalines
  • RNA, Messenger
  • Receptors, Glutamate
  • Resorcinols
  • 2-amino-3-phosphonopropionic acid
  • Cycloleucine
  • 1-amino-1,3-dicarboxycyclopentane
  • Egtazic Acid
  • 3,5-dihydroxyphenylglycine
  • 6-Cyano-7-nitroquinoxaline-2,3-dione
  • 2-Amino-5-phosphonovalerate
  • Alanine
  • Glycine