An updated synthesis of [11 C]carfentanil for positron emission tomography (PET) imaging of the μ-opioid receptor

J Labelled Comp Radiopharm. 2017 Jun 30;60(8):375-380. doi: 10.1002/jlcr.3513. Epub 2017 May 12.

Abstract

[11 C]Carfentanil ([11 C]CFN) is a selective radiotracer for in vivo positron emission tomography imaging studies of the μ-opioid system that, in our laboratories, is synthesized by methylation of the corresponding carboxylate precursor with [11 C]MeOTf, and purified using a C2 solid-phase extraction cartridge. Changes in the commercial availability of common C2 cartridges have necessitated future proofing the synthesis of [11 C]CFN to maintain reliable delivery of the radiotracer for clinical imaging studies. An updated synthesis of [11 C]CFN is reported that replaces a now obsolete purification cartridge with a new commercially available version and also substitutes the organic solvents used in traditional production methods with ethanol.

Keywords: C-11; PET radiochemistry; carbon-11; opioid; radiosynthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Carbon Radioisotopes*
  • Chemistry Techniques, Synthetic
  • Fentanyl / analogs & derivatives*
  • Fentanyl / chemical synthesis
  • Fentanyl / chemistry
  • Positron-Emission Tomography / methods*
  • Radiochemistry
  • Receptors, Opioid, mu / metabolism*

Substances

  • Carbon Radioisotopes
  • Carbon-11
  • Receptors, Opioid, mu
  • carfentanil
  • Fentanyl