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Iodothiouracil as a melanoma localizing agent.

Abstract
Thiouracil and various derivatives are selectively incorporated into the melanin pigment of melanomas during biosynthesis by serving as false melanin precursors. Using the transplantable Harding-Passey melanoma carried in BALB/c mice, we have extended our previous studies with sulfur-35 (35S) thiouracil. The persistence of high levels of [35S]thiouracil in tumor for periods of up to 2 wk has been demonstrated; during this time the drug content in normal tissues returned to near background levels. The variety of iodine isotopes available makes iodothiouracil a particularly promising melanoma-localizing agent. Tumor uptake and biodistribution of [35S]thiouracil and iodothiouracil (both iodine-127 (127I) and iodine-125 (125I) labeled) have been compared and were found to be essentially the same. The selectivity of [125I]thiouracil for melanoma has been qualitatively demonstrated by autoradiography of whole-body sections and quantitated by analysis of tumor and selected tissues. Iodothiouracil was also shown to localize in remote secondary metastases using a metastatic variant of the Harding-Passey melanoma currently being developed in our laboratory. These studies confirm the melanoma localizing capabilities of an iodinated thiouracil, and therefore the potential of using iodinated thiouracil derivatives for diagnosis and therapy of melanotic melanomas.
AuthorsJ A Coderre, S Packer, R G Fairchild, D Greenberg, B Laster, P Micca, I Fand
JournalJournal of nuclear medicine : official publication, Society of Nuclear Medicine (J Nucl Med) Vol. 27 Issue 7 Pg. 1157-64 (Jul 1986) ISSN: 0161-5505 [Print] United States
PMID3723191 (Publication Type: Comparative Study, Journal Article, Research Support, U.S. Gov't, Non-P.H.S., Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • Iodine Radioisotopes
  • Sulfur Radioisotopes
  • Thiouracil
  • iodothiouracil
Topics
  • Animals
  • Female
  • Iodine Radioisotopes
  • Melanoma (diagnostic imaging, metabolism)
  • Mice
  • Mice, Inbred BALB C
  • Neoplasm Transplantation
  • Radionuclide Imaging
  • Sulfur Radioisotopes
  • Thiouracil (analogs & derivatives, metabolism)
  • Tissue Distribution

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