Endogenous opioid release in the human brain reward system induced by acute amphetamine administration

Alessandro Colasanti, Graham E. Searle, Christopher J. Long, Samuel P. Hill, Richard R. Reiley, Darren Quelch, David Erritzoe, Andri C. Tziortzi, Laurence J. Reed, Anne R. Lingford-Hughes, Adam D. Waldman, Koen R.J. Schruers, Paul M. Matthews, Roger N. Gunn, David J. Nutt, Eugenii A. Rabiner

Research output: Contribution to journalArticlepeer-review


Background: We aimed to demonstrate a pharmacologically stimulated endogenous opioid release in the living human brain by evaluating the effects of amphetamine administration on [11C]carfentanil binding with positron emission tomography (PET). Methods: Twelve healthy male volunteers underwent [11C]carfentanil PET before and 3 hours after a single oral dose of d-amphetamine (either a "high" dose,.5 mg/kg, or a sub-pharmacological "ultra-low" dose, 1.25 mg total dose or approximately.017 mg/kg). Reductions in [11C]carfentanil binding from baseline to post-amphetamine scans (ΔBPND) after the "high" and "ultra-low" amphetamine doses were assessed in 10 regions of interest. Results: [11C]carfentanil binding was reduced after the "high" but not the "ultra-low" amphetamine dose in the frontal cortex, putamen, caudate, thalamus, anterior cingulate, and insula. Conclusions: Our findings indicate that oral amphetamine administration induces endogenous opioid release in different areas of human brain, including basal ganglia, frontal cortex areas, and thalamus. The combination of an amphetamine challenge and [11C]carfentanil PET is a practical and robust method to probe the opioid system in the living human brain. © 2012 Society of Biological Psychiatry.
Original languageEnglish
Pages (from-to)371-377
Number of pages7
JournalBiological Psychiatry
Issue number5
Publication statusPublished - 1 Sept 2012
Externally publishedYes


  • Amphetamine
  • carfentanil
  • dopamine
  • neuroimaging
  • opioids
  • PET
  • psychostimulants
  • amphetamine
  • carfentanil c 11
  • opiate
  • opiate receptor
  • tracer
  • unclassified drug
  • anterior cingulate
  • article
  • brain function
  • caudate nucleus
  • chemical binding
  • dose response
  • frontal cortex
  • human
  • human experiment
  • insula
  • male
  • normal human
  • physiological process
  • priority journal
  • putamen
  • reward
  • thalamus


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