Naltrexone-induced opiate receptor supersensitivity

R. Suzanne Zukin, Jonathan R. Sugarman, Melissa L. Fitz-Syage, Eliot L. Gardner, Stephen R. Zukin, Alan R. Gintzler

Research output: Contribution to journalArticle

168 Scopus citations

Abstract

Chronic administration of the long-lived narcotic antagonist naltrexone resulted in a marked increase in brain opiate receptors. Similar changes in receptor density were observed for binding of the putative μ agonist [3H]dihydromorphine, the μ antagonist [3H]naloxone, the putative δ ligand [3H]d-Ala2,d-Leu5-enkephalin and [3H]etorphine. In addition, the sensitivity of agonist binding to guanyl nucleotide inhibition increased significantly. In contrast, no such changes in opiate binding were observed following acute administration of naltrexone. The increase in opiate receptor number following chronic naltrexone was highest in the mesolimbic and frontal cortex areas, and lowest in the dorsal hippocampus and periaqueductal gray. These results indicate a degree of plasticity in the opiate receptor system that may correlate with specific functional pathways.

Original languageEnglish (US)
Pages (from-to)285-292
Number of pages8
JournalBrain research
Volume245
Issue number2
DOIs
StatePublished - Aug 12 1982

Keywords

  • naltrexone
  • opiate receptor
  • supersensitivity

ASJC Scopus subject areas

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

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  • Cite this

    Suzanne Zukin, R., Sugarman, J. R., Fitz-Syage, M. L., Gardner, E. L., Zukin, S. R., & Gintzler, A. R. (1982). Naltrexone-induced opiate receptor supersensitivity. Brain research, 245(2), 285-292. https://doi.org/10.1016/0006-8993(82)90811-3