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Synthesis and biological evaluation of a novel 99mTc nitrido radiopharmaceutical with deoxyglucose dithiocarbamate,showing tumor uptake
Authors:Junbo Zhang  Jialei Ren  Xiao Lin  Xuebin Wang
Affiliation:Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China
Abstract:The deoxyglucose dithiocarbamate (DGDTC) was synthesized and radiolabelled with [99mTcN]2+ intermediate to form the 99mTcN–DGDTC complex. The radiochemical purity of the 99mTcN–DGDTC complex was over 90%, as measured by TLC and by HPLC, without any notable decomposition at room temperature over a period of 6 h. The partition coefficient and electrophoresis results indicated that this complex was hydrophilic and neutral. The biodistribution of 99mTcN–DGDTC in mice bearing S 180 tumor showed that the complex accumulated in the tumor with high uptake and good retention. The tumor/blood and tumor/muscle ratios increased with time and reached 2.32 and 1.68 at 4 h post-injection, suggesting it would be a promising candidate for tumor imaging.
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