Isocyanide is a strong coordination ligand that can coordinate with [^99mTc(I)(CO)₃]⁺ core and [^99mTc(I)]⁺ core to produce stable ^99mTc complexes, therefore developing a ^99mTc‐labeled isocyanide complex for single‐photon emission computed tomography (SPECT) imaging is considered to be of great interest. In order to develop potential tumor imaging agents with satisfied tumor uptake and suitable pharmacokinetic properties in vivo, a novel d‐glucosamine isocyanide derivative, 4‐isocyano‐N‐(2,4,5‐trihydroxy‐6‐(hydroxymethyl)tetrahydro‐2H‐pyran‐3‐yl)butanamide (CN3DG), was synthesized and radiolabeled with [^99mTc(I)]⁺ and [^99mTc(CO)₃]⁺ cores to obtain [^99mTc(CN3DG)₆]⁺ and [^99mTc(CO)₃(CN3DG)₃]⁺ in high radiolabeling yields (>95%). Both of the complexes showed good hydrophilicity and great stability in vitro. Cell uptake studies performed in S180 cells demonstrated they were transported into cells by glucose transporters. Biodistribution studies of the two complexes in mice bearing S180 tumor showed they had high tumor uptakes and rapid clearance from muscle and blood so that the tumor/blood and tumor/muscle ratios were high. By comparison, [^99mTc(CN3DG)₆]⁺ was superior to [^99mTc(CO)₃(CN3DG)₃]⁺ in regard to tumor uptake, tumor/blood and tumor/liver ratios. S180 tumors could be seen clearly from the SPECT/CT images with [^99mTc(CN3DG)₆]⁺. Considering its favorable properties, [^99mTc(CN3DG)₆]⁺ would be a promising tumor imaging agent and needs to be further studied.

中文翻译：

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评价和比较具有不同99mTc核心的99mTc标记的d-葡萄糖胺衍生物作为潜在的肿瘤显像剂

异氰酸酯是一种强配位配体，可以与[ ^99m Tc（I）（CO）₃ ] ⁺核芯和[ ^99m Tc（I）] ⁺核芯配位，生成稳定的^99m Tc络合物，因此开发了^99m Tc标记的异氰酸酯络合物单光子发射计算机断层扫描（SPECT）成像被认为是非常令人感兴趣的。为了开发具有令人满意的肿瘤吸收和体内合适的药代动力学特性的潜在肿瘤显像剂，一种新型的d-氨基葡萄糖异氰酸酯衍生物4-异氰基N-（2,4,5-三羟基-6-（羟甲基）四氢-2 H合成了吡喃-3-基丁酰胺（CN3DG），并用[ ^99m Tc（I）] ⁺和[ ^99m Tc（CO）₃ ] ⁺核进行了放射性标记，获得了[ ^99m Tc（CN3DG）₆ ] ⁺和[ ^99m Tc（CO）₃（CN3DG）₃ ] ⁺放射性标记产率高（> 95％）。两种配合物均表现出良好的亲水性和体外稳定性。在S180细胞中进行的细胞摄取研究表明，它们被葡萄糖转运蛋白转运到细胞中。两种复合物在患有S180肿瘤的小鼠中的生物分布研究表明，它们具有很高的肿瘤吸收率，并且可以从肌肉和血液中快速清除，因此肿瘤/血液和肿瘤/肌肉比率很高。相比之下，在肿瘤摄取，肿瘤/血液和肿瘤/肝脏比率方面，[ ^99m Tc（CN3DG）₆ ] ⁺优于[ ^99m Tc（CO）₃（CN3DG）₃ ] ⁺。从[ ^99m]的SPECT / CT图像中可以清晰地看到S180肿瘤Tc（CN3DG）₆ ] ⁺。考虑到其良好的性能，[ ^99m Tc（CN3DG）₆ ] ⁺将是一种很有前途的肿瘤成像剂，需要进一步研究。