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Synthesis and biodistribution of a novel 99mTc-DMSA-metronidazole ester as a potential tumor hypoxia imaging agent

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Abstract

The dimercaptosuccinic acid metronidazole ester (DMSAMe) was synthesized and radiolabeled with 99mTc to form the 99mTc-DMSAMe complex in high yield. The radiochemical purity of the 99mTc-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 99mTc-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.

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Acknowledgments

The work was financially supported by National Natural Science Foundation of China (20771018) and by Beijing Normal University. The assistance of Ms. Huafan Huang and Prof. Taiwei Chu, College of Chemistry and Molecular Engineering, Peking University, in cellular accumulation study is gratefully acknowledged.

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Authors and Affiliations

  1. Key Laboratory of Radiopharmaceuticals, Ministry of Education, 100875, Beijing, People’s Republic of China

    Junbo Zhang, Qian Yu, Jinfeng Huo, Yan Pang, Sheng Yang, Yining He, Tingting Tang, Chenchen Yang & Xuebin Wang

  2. College of Chemistry, Beijing Normal University, 100875, Beijing, People’s Republic of China

    Junbo Zhang, Qian Yu, Jinfeng Huo, Yan Pang, Sheng Yang, Yining He, Tingting Tang, Chenchen Yang & Xuebin Wang

  3. The Affilated Hospital of Medical College QingDao University, QingDao, People’s Republic of China

    Qian Yu

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  1. Junbo Zhang
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  2. Qian Yu
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  3. Jinfeng Huo
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  4. Yan Pang
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  8. Chenchen Yang
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  9. Xuebin Wang
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Correspondence to Junbo Zhang.

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Zhang, J., Yu, Q., Huo, J. et al. Synthesis and biodistribution of a novel 99mTc-DMSA-metronidazole ester as a potential tumor hypoxia imaging agent. J Radioanal Nucl Chem 283, 481–485 (2010). https://doi.org/10.1007/s10967-010-0455-2

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  • DOI: https://doi.org/10.1007/s10967-010-0455-2

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