In this study, the melanoma targeting property of ⁶⁷Ga-NODAGA-GGNle-CycMSH_hex {1,4,7-triazacyclononane,1-gluteric acid-4,7-acetic acid-GlyGlyNle-c[Asp-His-D-Phe-Arg-Trp-Lys]-CONH₂} was determined on B16/F10 melanoma-bearing C57 mice to demonstrate the feasibility of NODAGA as a radiometal chelator for facile room temperature radiolabeling of NODAGA-GGNle-CycMSH_hex. The IC₅₀ value of NODAGA-GGNle-CycMSH_hex was 0.87 ± 0.12 nM on B16/F10 melanoma cells. ⁶⁷Ga-NODAGA-GGNle-CycMSH_hex was readily prepared at room temperature with greater than 98% radiolabeling yield and displayed MC1R-specific binding on B16/F10 melanoma cells. The B16/F10 melanoma uptake of ⁶⁷Ga-NODAGA-GGNle-CycMSH_hex was 10.31 ± 0.78, 14.96 ± 1.34, 13.7 ± 3.33 and 10.4 ± 2.2% ID/g at 0.5, 2, 4 and 24 h post-injection, respectively. Approximately 85% of the injected dose was cleared out the body via urinary system at 2 h post-injection. ⁶⁷Ga-NODAGA-GGNle-CycMSH_hex showed high tumor/blood, tumor/muscle and tumor/skin uptake ratios after 2 h post-injection. Overall, ⁶⁷Ga-NODAGA-GGNle-CycMSH_hex could be easily prepared at room temperature and exhibited favorable melanoma targeting property, suggesting the potential use of NODAGA as a radiometal chelator for facile room temperature radiolabeling of α-MSH peptides.

在这项研究中，针对⁶⁷ Ga-NODAGA-GGNle-CycMSH _hex {1,4,7-三氮杂环壬烷，1-戊二酸-4,7-乙酸-GlyGlyNle-c [Asp-His-D-Phe -Arg-Trp-Lys] -CONH ₂ }在带有B16 / F10黑色素瘤的C57小鼠身上测定，证明了NODAGA作为放射性金属螯合剂对NODAGA-GGNle-CycMSH _hex进行方便的室温放射性标记的可行性。在B16 / F10黑色素瘤细胞上，NODAGA-GGNle-CycMSH _hex的IC ₅₀值为0.87±0.12 nM。⁶⁷ Ga-NODAGA-GGNle-CycMSH_十六进制在室温下可以很容易地制备出具有大于98％的放射标记产率的BMP1，并且在B16 / F10黑素瘤细胞上显示出MC1R特异性结合。注射后0.5、2、4和24小时，⁶⁷ Ga-NODAGA-GGNle-CycMSH _hex的B16 / F10黑色素摄取分别为10.31± 0.78、14.96 ± 1.34、13.7 ±3.33和10.4±2.2％ID / g 。注射后2 h，约有85％的注射剂量通过泌尿系统排出体外。注射后2 h，⁶⁷ Ga-NODAGA-GGNle-CycMSH _hex显示出较高的肿瘤/血液，肿瘤/肌肉和肿瘤/皮肤摄取率。总共^67个Ga-NODAGA-GGNle-CycMSH_十六进制 可以容易地在室温下制备并表现出有利的黑色素瘤靶向性能，这表明将NODAGA用作放射性金属螯合剂以方便地在室温下进行α-MSH肽的放射性标记。