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Potential radiopharmaceuticals for the detection of ocular melanoma. Part I. 5-iodo-2-thiouracil derivatives

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Abstract

The tissue distribution of a number of 5-[131I]-iodo-2-thiouracil derivatives was measured in Syrian golden hamsters with Greene melanoma. These compounds were rapidly (in less than 1 h) distributed in all tissues, while in most tissues fast elimination (T1/2 1–3 h) was observed. Because of retention of the 131I activity in the tumour, high tumour/non-tumour tissue ratios were found (e.g. tumour/eye 2.3–10, tumour/skin 1.5–3) suggesting that some of these compounds might be used as melanoma delineating agents, when labelled with 123I.

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References

  1. AlexanderWD, EvansV, MacAuleyA, GallagherTF, Londono J (1969) Metabolism of 35S-labelled antithyroid drugs in man. Br Med J ii: 290–291

  2. Bakker CNM, Kaspersen FM, van Langevelde A, Pauwels EKJ (1980) The synthesis of 131I-5-iodo-2-thiouracil with IodogenTM. Int J Appl Radiat Isot 31: 513–515

  3. Bakker CNM, Kaspersen FM (1981) The electrophilic iodination with 131I of N1-substituted uracils using chloramine-T as oxidant. Int J Appl Radiat Isot 32:176–178

  4. Barret HW, West RA (1956) Dehalogenation of substituted pyrimidines in vivo. J Amer Chem Soc 78: 1612–1615

  5. Blois MS (1968) Melanin binding properties of iodoquine. J Invest Dermatol 50:250–253

  6. Boyd CM, Beierwaltes WH, Lieberman LM, Bergstrom TJ (1971) 125I-labeled chloroquine analog in the diagnosis of ocular melanomas. JNM 12:601–605

  7. Broxterman HJ, Bakker CNM, Boer H, Journée-de Korver JG, Kaspersen FM, Kakebeeke-Kemme HM, van Langevelde A, Pauwels EKJ (in press) Incorporation of 5-(125I)iodo-2-thiour-acils in cultured hamster melanoma cells. J Cancer Res (in press)

  8. Bubeck B, Eisenhut M, Heinke U, zum Winkel K (1981) Melanoma affine radiopharmaceuticals I. A comparative study of 131I-labeled quinoline and tyrosine derivatives. Eur J Nucl Med 6:227–233

  9. Dencker L, Larsson B, Olander K, Ullberg S, Yokota M (1979) False precursors of melanin as selective melanoma seekers. Br J Cancer 39:449–452

  10. Goulding RW, Danpure HJ, Somaia S, Osman S, Gunasekera SW, Eakins MN (1979) Radio-iodine labelled 4-amino-7-iodo-quinolines for melanoma detection. J Lab Comp Radiopharmac 16:46–48

  11. Van Langevelde A, Bakker CNM, Ilmer TAM, Journée-de Korver JA, Kaspersen FM, Ooserhuis JA, Pauwels EKJ, Wouterlood MA (in preparation) Potential radiopharmaceuticals for the detection of ocular melanoma. Part II Iodoquinoline derivatives.

  12. Mazel P, Henderson JF, Axelrod J (1964) S-Demethylation by microsomal enzymes. J Pharmacol Exp Ther 143:1–6

  13. Packer S, Lambrecht RM, Atkins HL, Wolf AP (1976) Short lived radiopharmaceuticals for non-contact detection of ocular melanoma. In: Croll MN, Brady LW, Carmiachael P, Wallner RJ (eds) Nuclear Ophthalmology. Wiley & Sons, New York, p 111–121

  14. Packer S, Lambrecht RM, Christman DR, Ansari AN, Wolf AP, Atkins HL (1977) Metal isotopes used as radioactive indicators of ocular melanoma. Am J Ophthalmol 83:80–94

  15. Pauwels EKJ, van Langevelde A, Kaspersen FM, Boer Iwema R, Oosterhuis JA (1980) Non-invasive detection of ocular melanoma: a patient study with 67Ga-and 99mTc-citrate and animal studies with a iodoquinoline analogue. Nucl Med Comm 1:224–232

  16. Safi N, Blanquet P, Basse-Cathalina B, Ducassou D (1975) Radionuclidic explorations in ophthalmology. J Nucl Med Allied Sci 2:166–173

  17. Whittaker JR (1971) Biosynthesis of a thiouracil pheomelanin in embryonic pigment cells exposed to thiouracil. J Biol Chem 246:6217–6226

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Correspondence to A. van Langevelde.

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van Langevelde, A., Bakker, C.N.M., Broxterman, H.J. et al. Potential radiopharmaceuticals for the detection of ocular melanoma. Part I. 5-iodo-2-thiouracil derivatives. Eur J Nucl Med 8, 45–51 (1983). https://doi.org/10.1007/BF00252555

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Keywords

  • Public Health
  • Melanoma
  • Nuclear Medicine
  • Tissue Distribution
  • Golden Hamster