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Tissue distribution of [18F]-5-fluorouracil in mice: effects of route of administration, strain, tumour and dose

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Summary

In a study investigating the usefulness of 5-fluorouracil labelled with fluorine 18 ([18F]-5-FU) in cancer chemotherapy, the tissue distribution of the radiolabel was determined in mice at 2, 4 and 6 h after administration by varying several parameters such as the mode of administration, the strain of mouse, the presence of a tumour and the total dose of 5-FU. The tissue distribution of fluorine 18 after i. p. injection pointed to an altered behaviour of the drug and/or its metabolites when compared with values obtained after i.v. injection, but no difference was found in the accumulation of radiolabel in the tumour. A comparison of non-tumour-bearing BALB/c and C57Bl/6 mice revealed that the latter showed a higher radiolabel accumulation of the drug and its metabolites in the liver, kidney, intestines and coecum (P <0.05 at 2 and 4 h). In tumour-bearing mice, especially at 2 h, the tissue accumulation of radiolabel was found to be significantly higher than in non-tumour-bearing controls (in BALB/c mice bearing colon 26 carcinoma,P <0.05 for all tissues; in C57Bl/6 mice bearing colon 38 carcinoma,P <0.05 for the blood, lung, liver, kidney, large intestines, coecum and muscle). Finally, a comparison of injections of a tracer dose of [18F]-5-FU (2.5 mg/kg) vs a therapeutic dose (100 mg/kg) revealed only small differences in the accumulation of fluorine 18 in the liver and kidney.

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Authors and Affiliations

  1. Radio-Nuclide-Centre (RNC), Free University, P. O. Box 7161, 1007 MC, Amsterdam, The Netherlands

    Gerard W. M. Visser, Geertrui C. M. Gorree & Jacobus D. M. Herscheid

  2. Department of Oncology, Free University Hospital, P. O. Box 7057, 1007 MB, Amsterdam, The Netherlands

    Godefridus J. Peters

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  1. Gerard W. M. Visser
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  2. Geertrui C. M. Gorree
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  3. Godefridus J. Peters
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  4. Jacobus D. M. Herscheid
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Visser, G.W.M., Gorree, G.C.M., Peters, G.J. et al. Tissue distribution of [18F]-5-fluorouracil in mice: effects of route of administration, strain, tumour and dose. Cancer Chemother Pharmacol 26, 205–209 (1990). https://doi.org/10.1007/BF02897200

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  • DOI: https://doi.org/10.1007/BF02897200

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