Abstract
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 language | English |
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Pages (from-to) | 371-377 |
Number of pages | 7 |
Journal | Biological Psychiatry |
Volume | 72 |
Issue number | 5 |
DOIs | |
Publication status | Published - 1 Sept 2012 |
Externally published | Yes |
Keywords
- 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