[11C]Fentanyl: radiosynthesis and preclinical pet imaging for its pharmacokinetics
We successfully developed and automated the radiosynthesis of [<sup>11</sup>C]fentanyl, enabling PET imaging that revealed rapid brain kinetics and a critical role of P-gp/BCRP efflux in fentanyl disposition in brain. Prolonged retention in adipose tissue may delay brain clearance, potentially increasing the risk of re-narcotization (as has been reported in clinical cases after naloxone reversal). These findings advance our ability to quantify fentanyl tissue distribution and pharmacokinetics in the brain and body and provide a valuable tool for further studies in preclinical and clinical settings.
Authors
- Nora D. Volkow (ORCID: https://orcid.org/0000-0001-6668-0908)
- Wenjing Zhao (ORCID: https://orcid.org/0000-0003-4101-4065)
- Abolghasem Bakhoda (ORCID: https://orcid.org/0000-0002-3222-8873)
- Woochan Kim (ORCID: https://orcid.org/0000-0002-4908-4036)
- Jeih‐San Liow (ORCID: https://orcid.org/0000-0002-7878-1076)
- Kelly A. O’Conor
- Seth M. Eisenberg (ORCID: https://orcid.org/0000-0002-7144-7657)
- Michael L. Freaney
- Sung Won Kim (ORCID: https://orcid.org/0000-0002-4647-4899)
- Nathaniel J. Burkard
- Aaron K. Wozniak
- Ailen Costamagna-Soto
Institutions
- National Institutes of Health (US)
- National Institute on Alcohol Abuse and Alcoholism (US)
- National Institute of Mental Health (US)
Publication Details
- Journal
- EJNMMI Radiopharmacy and Chemistry
- Published
- 2025-10-28
- DOI
- https://doi.org/10.1186/s41181-025-00394-z
- Primary Topic
- Forensic Toxicology and Drug Analysis
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Institutes of Health
- National Institute of Mental Health
- NIH Clinical Center