| Summary: | In order to seek novel technetium-99m folate receptor-targeting agents, two folate derivatives (CN5FA and CNPFA) were synthesized and radiolabeled to obtain [<sup>99m</sup>Tc]Tc-CN5FA and [<sup>99m</sup>Tc]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 [<sup>99m</sup>Tc]Tc-CN5FA and [<sup>99m</sup>Tc]Tc-CNPFA had specificity to folate receptor. Biodistribution studies in KB tumor-bearing mice illustrated that [<sup>99m</sup>Tc]Tc-CN5FA and [<sup>99m</sup>Tc]Tc-CNPFA had specific tumor uptake. Compared with [<sup>99m</sup>Tc]Tc-CN5FA, the tumor/muscle ratios of [<sup>99m</sup>Tc]Tc-CNPFA were higher, resulting in a better SPECT/CT imaging background. According to the results, the two <sup>99m</sup>Tc complexes have potential as tumor imaging agents to target folate receptors.
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