An endogenous ligand of the brain σ/PCP receptor antagonizes NMDA-induced neurotransmitter release

Stephen R. Zukin, R. Suzanne Zukin, Wylie Vale, Jean Rivier, Roxanne Nichtenhauser, Lawrence D. Snell, Kenneth M. Johnson

Research output: Contribution to journalArticle

27 Scopus citations

Abstract

The present study provides evidence for the presence of an endogenous ligand for the phencyclidine (PCP) receptor of mammalian brain. Partially purified bovine hippocampal extracts potently and dose dependently inhibit binding to PCP receptors of [3HN-(1[2-thienyl]-cyclohexyl)piperidine (TCP), a highly potent and specific ligand of PCP receptors. In addition to demonstrating PCP-like binding properties, the partially purified extract mimics biological actions of PCP upon neurotransmitter release. HPLC fractions active in the [3]TCP binding assay, by contrast to fractions inactive in the binding assay, potently elicited stimulation of spontaneous acetycholine and dopamine efflux and inhibited NMDA-stimulated release of acetylcholine and dopamine. The transmitter release assay provides validation of a PCP-like physiological activity exerted by bovine hippocampal extracts purified by HPLC.

Original languageEnglish (US)
Pages (from-to)84-89
Number of pages6
JournalBrain Research
Volume416
Issue number1
DOIs
StatePublished - Jul 21 1987

Keywords

  • N-Methyl-d-aspartate
  • Neurotransmitter release
  • Phencyclidine receptor
  • Phenycyclidine
  • Sigma receptor

ASJC Scopus subject areas

  • Developmental Biology
  • Molecular Biology
  • Clinical Neurology
  • Neuroscience(all)

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    Zukin, S. R., Suzanne Zukin, R., Vale, W., Rivier, J., Nichtenhauser, R., Snell, L. D., & Johnson, K. M. (1987). An endogenous ligand of the brain σ/PCP receptor antagonizes NMDA-induced neurotransmitter release. Brain Research, 416(1), 84-89. https://doi.org/10.1016/0006-8993(87)91499-5