Buprenorphine-induced changes in mu-opioid receptor availability in male heroin-dependent volunteers: A preliminary study

Jon Kar Zubieta, Mark K. Greenwald, Umberto Lombardi, James H. Woods, Michael R. Kilbourn, Douglas M. Jewett, Robert A. Koeppe, Charles R. Schuster, Chris Ellyn Johanson

Research output: Contribution to journalArticlepeer-review

105 Scopus citations


A principle of opioid pharmacotherapy is that high medication doses should occupy fractionally more opioid receptors that mediate heroin effects. In this preliminary study we examined in vivo μ opioid receptor (μOR) binding in three healthy opioid-dependent volunteers during maintenance on 2 and 16 mg sublingual buprenorphine (BUP) liquid, and after detoxification (0 mg) under double-blind, placebo-controlled conditions, and once in matched controls. Binding measures were obtained with the μOR-selective radioligand [11C]carfentanil (CFN) and PET 4 hrs after BUP administration. BUP induced dose-dependent reductions in μOR availability, 36-50% at 2 mg and 79-95% at 16 mg relative to placebo. Heroin abusers also had greater μOR binding potential in the inferofrontal cortex and anterior cingulate regions during placebo, compared to matched controls. Further studies are warranted to examine the relationship of μOR availability with BUP therapeutic actions, and the clinical implications of increased μOR binding during withdrawal. Copyright (C) 2000 American College of Neuropsychopharmacology.

Original languageEnglish (US)
Pages (from-to)326-334
Number of pages9
Issue number3
StatePublished - Sep 1 2000
Externally publishedYes


  • Buprenorphine
  • Carfentanil
  • Mu opioid receptors
  • Opiate dependence
  • Opiates
  • Positron emission tomography

ASJC Scopus subject areas

  • Pharmacology
  • Psychiatry and Mental health


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