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 journalArticlepeer-review

168 Scopus citations


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
Issue number2
StatePublished - Aug 12 1982
Externally publishedYes


  • naltrexone
  • opiate receptor
  • supersensitivity

ASJC Scopus subject areas

  • Developmental Biology
  • Molecular Biology
  • Clinical Neurology
  • General Neuroscience


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