Automated radiosynthesis of [C-11]morphine for clinical investigation

作者：Fan Jinda; Meissner Konrad; Gaehle Gregory G; Li Shihong; Kharasch Evan D; Mach Robert H; Tu Zhude^*

来源：Applied Radiation and Isotopes, 2011, 69(2): 431-435.

DOI：10.1016/j.apradiso.2010.11.003

• [C-11]morphine
• Automated radiosynthesis
• Positron emission tomography

To meet a multiple-dose clinical evaluation of the P-gp modulation of [C-11]morphine delivery into the human brain, radiosynthesis of [(11)(C)]morphine was accomplished on an automated system by N-methylation of normorphine with [C-11]CH3I. 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/mu mol (decay corrected to end-of-bombardment): radiochemical and chemical purities were >95% (n=28).

• 出版日期2011-2