Springer Nature is making SARS-CoV-2 and COVID-19 research free. View research | View latest news | Sign up for updates

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

  • 36 Accesses

  • 22 Citations


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.

This is a preview of subscription content, log in to check access.


  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

Download references

Author information

Correspondence to A. van Langevelde.

Rights and permissions

Reprints and Permissions

About this article

Cite this article

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

Download citation


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