Synthesis and biodistribution of 18F-labeled fluoronitroimidazoles: Potential in vivo markers of hypoxic tissue

Paul A. Jerabek, Timothy B. Patrick, Michael R. Kilbourn, Douglas D. Dischino, Michael J. Welch

Research output: Contribution to journalArticlepeer-review

95 Scopus citations


Three 18F labeled fluoronitroimidazoles have been prepared as potential in vivo markers of hypoxic cells in tumors, and ischemic areas of the heart and brain. 1-(2-Nitroimidazolyl)-3-[18F]fluoro-2-hydroxypropanol (18F]fluoro-normethoxymisonidazole) 4, 1-(2-[18F]fluoroethyl)-2-nitroimidazole 7, and 1-(2-[18F]fluoroethyl)-2-methyl-5-nitroimidazole ([18F]fluoro-norhydroxymetronidazole) 10 were prepared in average radiochemical yields of <1%, 23% and 15-43% (8% at the no carrier-added level) respectively at end-of-synthesis. The in vivo biodistribution in rats was determined for each of the 18F labeled fluoronitroimidazoles. At 1 and 3 h after administration, the tissue distribution of each of the 18F labeled nitroimidzaoles was quite uniform and consistent with that of nitroimidazoles previously studied. These results suggest the need for a suitable animal model to evaluate their potential as in vivo markers of hypoxic tissue in the brain.

Original languageEnglish (US)
Pages (from-to)599-605
Number of pages7
JournalInternational Journal of Radiation Applications and Instrumentation. Part
Issue number7
StatePublished - 1986
Externally publishedYes

ASJC Scopus subject areas

  • Radiation
  • Engineering(all)

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