Glutamate-containing dipeptides enhance specific binding at glutamate receptors and inhibit specific binding at kainate receptors in rat brain

J. Ferkany, R. Zaczek, A. Markl, J. T. Coyle

Research output: Contribution to journalArticlepeer-review

Abstract

The dipeptide, l-phenylalanyl-l-glutamate (PG), augments the specific binding of the excitatory amino acid receptor antagonist, [3H]2-amino-7-phosphonoheptanoic acid (APH), to rat forebrain membranes by 5-fold at 100 μM with an EC50 of 4.9 μM. The increase in the specific binding of [3H]AHP induced by PG results exclusively from an increase in Bmax. In contrast, PG inhibits the specific binding of [3H]kainic acid to forebrain membranes with a Ki of 6.8 μM. Of several related peptides examined, active ones affected the two receptor sites in a reciprocal fashion. The results suggest an allosteric interaction between [3H]APH and kainate receptors modulated by glutamate-containing peptides.

Original languageEnglish (US)
Pages (from-to)281-286
Number of pages6
JournalNeuroscience Letters
Volume44
Issue number3
DOIs
StatePublished - Feb 24 1984

Keywords

  • amino-phosphono-heptanoic acid
  • excitatory receptors
  • kainic acid
  • l-glutamate
  • peptides

ASJC Scopus subject areas

  • Neuroscience(all)

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