TY - JOUR
T1 - Synthesis and biodistribution of 18F-labeled fluoronitroimidazoles
T2 - Potential in vivo markers of hypoxic tissue
AU - Jerabek, Paul A.
AU - Patrick, Timothy B.
AU - Kilbourn, Michael R.
AU - Dischino, Douglas D.
AU - Welch, Michael J.
N1 - Funding Information:
Acknowledgements-The authors would like to acknowledge MS Lucia Hoerr, MS Carla Mathias, and MS Terry Sconcef or their technicaal ssistancwe ith thea nimals tudies. We also thank the Washington University Mass Spec-trometryR esources upportedb y NIH Grant RR00954f or providingl ow resolutionm asss pectraa nd J. Carter Cook of the NSF RegionalI nstrumentationF acility of the University of Illinois for providing the high resolutionm ass spectraT. his work wass upportedin part by grantsf rom the National Instituteso f Health (NS 06833a nd HL 13851).
PY - 1986
Y1 - 1986
N2 - 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.
AB - 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.
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U2 - 10.1016/0883-2889(86)90079-1
DO - 10.1016/0883-2889(86)90079-1
M3 - Article
C2 - 3021662
AN - SCOPUS:0022437135
VL - 37
SP - 599
EP - 605
JO - Applied Radiation and Isotopes
JF - Applied Radiation and Isotopes
SN - 0969-8043
IS - 7
ER -