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In order to seek novel technetium-99m folate receptor-targeting agents, two folate derivatives (CN5FA and CNPFA) were synthesized and radiolabeled to obtain [ 99m Tc]Tc-CN5FA and [ 99m Tc]Tc-CNPFA complexes, which exhibited high radiochemical purity (&gt;95%) without purification, hydrophilicity, and good stability in vitro. The KB cell competitive binding experiments indicated that [ 99m Tc]Tc-CN5FA and [ 99m Tc]Tc-CNPFA had specificity to folate receptor. Biodistribution studies in KB tumor-bearing mice illustrated that [ 99m Tc]Tc-CN5FA and [ 99m Tc]Tc-CNPFA had specific tumor uptake. Compared with [ 99m Tc]Tc-CN5FA, the tumor/muscle ratios of [ 99m Tc]Tc-CNPFA were higher, resulting in a better SPECT/CT imaging background. According to the results, the two 99m Tc complexes have potential as tumor imaging agents to target folate receptors.

Preparation and Evaluation of Novel Folate Isonitrile 99mTc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors