Synthesis and biodistribution of a novel ~(99m)Tc-DMSA- metronidazole ester as a potential tumor hypoxia imaging agent

摘要

The dimercaptosuccinic acid metronidazole ester (DMSAMe) was synthesized and radiolabeled with ~(99m)Tc to form the ~(99m)Tc-DMSAMe complex in high yield. The radiochemical purity of the ~(99m)Tc-DMSAMe complex was over 90%, as measured by TLC and by HPLC, without any notable decomposition at room temperature over a period of 6 h. Its partition coefficient indicated that it was a lipophilic complex. The tumor cell experiment and the biodistribution in mice bearing S 180 tumor showed that the ~(99m)Tc-DMSAMe complex had a certain hypoxic selectivity and accumulated in the tumor with high uptake and good retention. The tumor/blood and tumor/muscle ratios increased with time, suggesting it would be a possible tumor hypoxia imaging agent.