Non-competitive regulation of phencyclidine/σ-receptors by the N-methyl-d-aspartate receptor antagonist d-(-)-2-amino-5-phosphonovaleric acid

Daniel C. Javitt, Alan Jotkowitz, Ratna Sircar, Stephen R. Zukin

Research output: Contribution to journalArticlepeer-review

49 Scopus citations

Abstract

d-(-)-2-Amino-5-phosphonovaleric acid (d(-)AP5), a selective, potent competitive antagonist of N-methyl-d-aspartate (NMDA)-type excitatory amino acid receptors was used to investigate the relationship between NMDA receptors and phencyclidine (PCP) binding. Incubation of rat brain membranes with d(-)AP5 decreased the apparent number of PCP/σ-receptors in dose-dependent fashion without affecting their affinity for [2-thienyl-3H]cyclohexylpiperidine (TCP). These data, taken together with electrophysiological evidence that PCP non-competitively antagonizes NMDA receptor-mediated transmission, are consistent with the hypothesis that the PCP/σ-receptor may be situated in or near a channel regulated by an NMDA receptor complex.

Original languageEnglish
Pages (from-to)193-198
Number of pages6
JournalNeuroscience Letters
Volume78
Issue number2
DOIs
StatePublished - 22 Jul 1987
Externally publishedYes

Keywords

  • Excitatory amino acid
  • Glutamic acid
  • N-Methyl-d-aspartic acid
  • Phencyclidine
  • Receptor
  • Schizophrenia

ASJC Scopus subject areas

  • Neuroscience (all)

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