Imaging δ- and μ-opioid receptors by PET in lung carcinoma patients

Igal Madar, Badredin Bencherif, John Lever, Richard F. Heitmiller, Stephen C. Yang, Malcolm Brock, Julie Brahmer, Hayden Ravert, Robert Dannals, James J. Frost

Research output: Contribution to journalArticlepeer-review

39 Scopus citations


In the present study, we measured the kinetics and distribution in vivo of the selective δ-opioid antagonist 11C-methylnaltrindole ( 11C-MeNTI) and the μ-opioid agonist 11C-carfentanil (11CCFN) in patients with lung carcinoma using PET. Methods: Paired measurements of 11C-MeNTI and 11C-CFN binding were performed in biopsy-proven small-cell (n = 2), squamous (n = 2), and adenocarcinoma (n = 3) lung cancer patients. Dynamic PET scans of increasing duration (0.5-8 min) were acquired over 90 min after an intravenous bolus injection of 370 MBq of tracer. Time-activity curves for tumor and normal lung parenchyma binding were generated using the region-of-interest (ROI) method. The mean activity at equilibrium was measured, and the specific-to-nonspecific binding ratio (tumor 2 lung)/lung was calculated. Four of 7 patients underwent an additional static 18F-FDG PET scan for clinical indications. Three of 7 patients underwent surgery, and stained sections of tumor were inspected for inflammation, necrosis, and scar tissue. Results: Increased binding of 11C-MeNTI and 11C-CFN was detected in all tumor types studied. 11C-MeNTI binding in tumor and healthy lung tissue was significantly more intense than that of 11C-CFN. The average specific-to-nonspecific binding ratio across cell types for 11C-MeNTI (4.32 ± 1.31; mean ± SEM) was greater than that of 11C-CFN (2.42 ± 1.17) but lower than that of 18FFDG (7.74 = 0.53). Intravenous naloxone produced 50% and 44% decreases in the specific-to-nonspecific binding ratios of 11C-MeNTI and 11C-CFN, respectively. Conclusion: These data provide in vivo evidence for the presence of δ- and μ-opioid receptor types in the 3 major human lung carcinomas and suggest the suitability of 11C-MeNTI and 11C-CFN as investigational probes of lung carcinoma biology.

Original languageEnglish (US)
Pages (from-to)207-213
Number of pages7
JournalJournal of Nuclear Medicine
Issue number2
StatePublished - Feb 1 2007


  • Lung carcinoma
  • Opioid receptor
  • PET

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging


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