Automated radiosynthesis of [11C]morphine for clinical investigation

Appl Radiat Isot. 2011 Feb;69(2):431-5. doi: 10.1016/j.apradiso.2010.11.003. Epub 2010 Nov 11.

Abstract

To meet a multiple-dose clinical evaluation of the P-gp modulation of [(11)C]morphine delivery into the human brain, radiosynthesis of [(11)C]morphine was accomplished on an automated system by N-methylation of normorphine with [(11)C]CH(3)I. A methodology employing optimized solid phase extraction of the HPLC eluent was developed. Radiosynthesis took 45 min with a radiochemical yield ranging from 45% to 50% and specific activity ranging from 20 to 26 Ci/μmol (decay corrected to end-of-bombardment); radiochemical and chemical purities were >95% (n=28).

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Automation, Laboratory
  • Carbon Radioisotopes*
  • Isotope Labeling / methods*
  • Methylation
  • Morphine / chemistry*
  • Radiopharmaceuticals / chemical synthesis*
  • Solid Phase Extraction

Substances

  • Carbon Radioisotopes
  • Radiopharmaceuticals
  • Morphine