Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
2154885 | Nuclear Medicine and Biology | 2007 | 9 Pages |
Abstract
The radioiodinated 3â²-fluorothymidine (FLT) analogue 3â²-fluoro-5-[131I]iodo-2â²-deoxyuridine ([131I]FLIdU) was synthesized, with iodine mimicking the methyl group of pyrimidine. [131I]FLIdU was accessible by direct electrophilic iodination using Iodogen as oxidant. Optimized amounts of the oxidant allowed radiochemical yields of about 70% after a reaction time of 10 min in an aqueous buffer medium at 90°C. The uptake of [131I]FLIdU in a DoHH2 leukemia xenograft mouse model and in healthy mice revealed moderate FLIdU accumulation, followed by a significant washout of activity in proliferating tissues such as splenic and tumor tissues. In contrast, intraperitoneal coinjection with [18F]FLT showed high uptake and high activity retention up to 2 h, in both splenic and tumor tissues. Uptake in stomach tissues and increasing fractions of [131I]iodide in urine indicated metabolic instability of [131I]FLIdU due to rapid deiodination. Therefore, [131I]FLIdU alone does not seem to be a promising compound, neither for diagnostic imaging nor for potential therapeutic applications.
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Authors
Andreas T.J. Vogg, Andreas K. Buck, Michaela Schmid, Bernd Neumaier, Katrin Wczasek, Boris D. Zlatopolskiy, Sven N. Reske,