Preparation and Evaluation of Novel Folate Isonitrile 99mTc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors |
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| Authors: | Junhong Feng Xuran Zhang Qing Ruan Yuhao Jiang Junbo Zhang |
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| Institution: | 1.Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China; (J.F.); (X.Z.); (Q.R.); (Y.J.);2.NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), Perking University, Beijing 100091, China |
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| Abstract: | In order to seek novel technetium-99m folate receptor-targeting agents, two folate derivatives (CN5FA and CNPFA) were synthesized and radiolabeled to obtain 99mTc]Tc-CN5FA and 99mTc]Tc-CNPFA complexes, which exhibited high radiochemical purity (>95%) without purification, hydrophilicity, and good stability in vitro. The KB cell competitive binding experiments indicated that 99mTc]Tc-CN5FA and 99mTc]Tc-CNPFA had specificity to folate receptor. Biodistribution studies in KB tumor-bearing mice illustrated that 99mTc]Tc-CN5FA and 99mTc]Tc-CNPFA had specific tumor uptake. Compared with 99mTc]Tc-CN5FA, the tumor/muscle ratios of 99mTc]Tc-CNPFA were higher, resulting in a better SPECT/CT imaging background. According to the results, the two 99mTc complexes have potential as tumor imaging agents to target folate receptors. |
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| Keywords: | 99mTc isonitrile folate receptor SPECT/CT imaging |
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