title: Synthesis and biodistribution of 18F-labeled fluoronitroimidazoles: potential in vivo markers of hypoxic tissue.
abstract: 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 less than 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.
mesh_terms: D000818:Animals; D005461:Fluorine; D000860:Hypoxia / Q000000981:diagnostic imaging*; D008795:Metronidazole / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D008920:Misonidazole / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D009593:Nitroimidazoles / Q000138:chemical synthesis; D011868:Radioisotopes; D011877:Radionuclide Imaging; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution
chemical_list: D009593:Nitroimidazoles; D011868:Radioisotopes; C031843:fluoromisonidazole; C050612:1-(2-fluoroethyl)-2-nitroimidazole; C050611:1-(2-fluoroethyl)-2-methyl-5-nitroimidazole; D008795:Metronidazole; D005461:Fluorine; D008920:Misonidazole