Amphetamine induced endogenous opioid release in the human brain detected with [¹¹C]carfentanil PET: replication in an independent cohort

Int J Neuropsychopharmacol. 2014 Dec;17(12):2069-74. doi: 10.1017/S1461145714000704. Epub 2014 May 7.

Abstract

This study aimed to replicate a previous study which showed that endogenous opioid release, following an oral dose of amphetamine, can be detected in the living human brain using [11C]carfentanil positron emission tomography (PET) imaging. Nine healthy volunteers underwent two [11C]carfentanil PET scans, one before and one 3 h following oral amphetamine administration (0.5 mg/kg). Regional changes in [11C]carfentanil BPND from pre- to post-amphetamine were assessed. The amphetamine challenge led to significant reductions in [11C]carfentanil BPND in the putamen, thalamus, frontal lobe, nucleus accumbens, anterior cingulate, cerebellum and insula cortices, replicating our earlier findings. None of the participants experienced significant euphoria/'high', supporting the use of oral amphetamine to characterize in vivo endogenous opioid release following a pharmacological challenge. [11C]carfentanil PET is able to detect changes in binding following an oral amphetamine challenge that reflects endogenous opioid release and is suitable to characterize the opioid system in neuropsychiatric disorders.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Amphetamine / blood
  • Amphetamine / pharmacology*
  • Brain / diagnostic imaging*
  • Brain / drug effects*
  • Brain / metabolism
  • Brain Mapping
  • Carbon Radioisotopes
  • Central Nervous System Stimulants / blood
  • Central Nervous System Stimulants / pharmacology*
  • Cohort Studies
  • Fentanyl / analogs & derivatives
  • Humans
  • Magnetic Resonance Imaging
  • Male
  • Opioid Peptides / metabolism*
  • Positron-Emission Tomography
  • Radiopharmaceuticals

Substances

  • Carbon Radioisotopes
  • Central Nervous System Stimulants
  • Opioid Peptides
  • Radiopharmaceuticals
  • Amphetamine
  • carfentanil
  • Fentanyl