Automated radiosynthesis of [11C]morphine for clinical investigation.
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).
Department of Radiology, Washington University School of Medicine, 510 South Kingshighway Blvd. St. Louis, MO 63110, USA.
Jinda
J
Fan
Konrad
K
Meissner
Gregory G
GG
Gaehle
Shihong
S
Li
Evan D
ED
Kharasch
Robert H
RH
Mach
Zhude
Z
Tu
D057205:Automation, Laboratory; D002250:Carbon Radioisotopes; D007553:Isotope Labeling / Q000379:methods*; D008745:Methylation; D009020:Morphine / Q000737:chemistry*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D052616:Solid Phase Extraction
D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D009020:Morphine