Abstract
To develop18F-fluoroalkyl derivatives of methionine (MET) as a tumor detecting agent by mean of clinical PET, a pilot study assessing the potential of their parent compounds,11C-labeled ethionine (11C-ETH) and propionine (11C-PRO), was performed.11C-ETH and11C-PRO were prepared by the reaction ofl-homocysteine thiolactone and corresponding11C-alkyl iodides. After i.v. injection of a mixture of3H-MET,14C-ETH and11C-PRO into mice bearing FM3A mammary carcinoma, the highest FM3A uptake was found in14C-ETH, followed by3H-MET and11C-PRO, while the FM3A-to-brain and FM3A-to-muscle ratios were nearly the same for all three compounds. The FM3A uptake of14C-ETH and11C-PRO were nearly equal or slightly higher than the liver uptake. In the pancreas, liver, FM3A and brain tissues, incorporation of14C-ETH into acid-precipitable materials was much lower than that of3H-MET, whereas no incorporation of11C-PRO was found. Brain uptake of all three compounds was significantly reduced by carrier MET-loading (5 min p.i.) or by cycloheximide treatment to inhibit protein synthesis (60 min p.i.), whereas the FM3A uptake was not affected. Incorporation of14C-ETH into acid-precipitable materials was inhibited by the cycloheximide. The results suggest that11C-labeled ETH has a similar potential for tumor detection by PET as11C-MET, and that11C-PRO has similar properties to those of other artificial amino acids. The development of18F-fluoroalkyl derivatives of MET is of interest as the next step.
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Ishiwata, K., Kasahara, C., Hatano, K. et al. Carbon-11 labeled ethionine and propionine as tumor detecting agents. Ann Nucl Med 11, 115–122 (1997). https://doi.org/10.1007/BF03164819
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DOI: https://doi.org/10.1007/BF03164819