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

Neuropsychopharmacology. 2000 Sep;23(3):326-34. doi: 10.1016/S0893-133X(00)00110-X.


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 mu opioid receptor (muOR) 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 muOR-selective radioligand [11C]carfentanil (CFN) and PET 4 hrs after BUP administration. BUP induced dose-dependent reductions in muOR availability, 36-50% at 2 mg and 79-95% at 16 mg relative to placebo. Heroin abusers also had greater muOR 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 muOR availability with BUP therapeutic actions, and the clinical implications of increased muOR binding during withdrawal.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Analgesics, Opioid
  • Brain / diagnostic imaging
  • Brain Chemistry
  • Buprenorphine / pharmacology*
  • Double-Blind Method
  • Fentanyl / analogs & derivatives
  • Heroin Dependence / diagnostic imaging
  • Heroin Dependence / metabolism*
  • Humans
  • Image Processing, Computer-Assisted
  • Male
  • Middle Aged
  • Narcotics / pharmacology*
  • Receptors, Opioid, mu / drug effects*
  • Tomography, Emission-Computed


  • Analgesics, Opioid
  • Narcotics
  • Receptors, Opioid, mu
  • Buprenorphine
  • carfentanil
  • Fentanyl