Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors: [11C]PEO

J Med Chem. 2009 Sep 24;52(18):5586-9. doi: 10.1021/jm900892x.


Antagonist radiotracers have shown only a low sensitivity for detecting competition from high-efficacy agonists at opioid receptors (ORs) in vivo. We report that [(11)C]PEO binds with high affinity to mu and kappa-opioid receptors, is a full agonist, and concentrates in brain regions of rats with a high density of the mu-OR after intravenous injection. Blocking studies with mu and kappa-OR selective compounds demonstrated that the binding of [(11)C]PEO is saturable and selective to the mu-OR in rat brain.

MeSH terms

  • Animals
  • Brain / diagnostic imaging
  • Brain / metabolism
  • CHO Cells
  • Carbon Radioisotopes / chemistry
  • Cricetinae
  • Cricetulus
  • Humans
  • Kinetics
  • Male
  • Morphinans / chemical synthesis*
  • Morphinans / metabolism
  • Morphinans / pharmacology*
  • Positron-Emission Tomography*
  • Rats
  • Rats, Wistar
  • Receptors, Opioid / agonists*
  • Receptors, Opioid / metabolism
  • Substrate Specificity


  • Carbon Radioisotopes
  • Morphinans
  • Receptors, Opioid
  • phenylethyl orvinol