Quantification of brain mu-opioid receptors with [11C]carfentanil: reference-tissue methods

Nucl Med Biol. 2003 Feb;30(2):177-86. doi: 10.1016/s0969-8051(02)00411-0.


[(11)C]Carfentanil (CFN) is a mu-opioid agonist used for in vivo positron emission tomography (PET) studies of mu-opioid receptors. Previously, a tissue-ratio method was validated for the quantification of CFN binding. However, since that initial validation, several other blood independent (reference-tissue) methods have become available. To evaluate these methods, CFN PET studies with arterial blood sampling were acquired in six healthy male control subjects. Specific binding estimates obtained from reference-tissue methods were compared to those obtained with a more rigorous blood input modeling technique. It was determined that both a graphical method, and a simplified reference tissue model, were more accurate than the tissue-ratio method for quantification of CFN binding.

Publication types

  • Clinical Trial
  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.
  • Validation Study

MeSH terms

  • Adult
  • Animals
  • Brain / diagnostic imaging
  • Brain / metabolism*
  • Carbon Radioisotopes / blood
  • Carbon Radioisotopes / pharmacokinetics
  • Computer Simulation
  • Cytochromes
  • Electron Transport Complex IV
  • Fentanyl / analogs & derivatives*
  • Fentanyl / blood*
  • Fentanyl / pharmacokinetics*
  • Humans
  • Male
  • Mice
  • Models, Biological
  • Nitrite Reductases
  • Radioisotope Dilution Technique / standards
  • Radiopharmaceuticals / blood
  • Radiopharmaceuticals / pharmacokinetics
  • Receptors, Opioid, mu / metabolism*
  • Reference Standards
  • Tissue Distribution
  • Tomography, Emission-Computed / methods*
  • Tomography, Emission-Computed / standards*


  • Carbon Radioisotopes
  • Cytochromes
  • Radiopharmaceuticals
  • Receptors, Opioid, mu
  • Nitrite Reductases
  • nitrite reductase (NO-forming)
  • Electron Transport Complex IV
  • carfentanil
  • Fentanyl