Metastatic melanoma imaging using a novel Tc-99m-labeled lactam-cyclized alpha-MSH peptide

利用新型Tc-99m标记的内酰胺环化α-MSH肽进行转移性黑色素瘤成像

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Abstract

The purpose of this study was to determine the metastatic melanoma imaging property of (99m)Tc(EDDA)-HYNIC-Aoc-Nle-CycMSH(hex) {hydrazinonicotinamide-8-aminooctanoic acid-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-CONH(2)}. HYNIC-Aoc-Nle-CycMSH(hex) was synthesized using fluorenylmethyloxy carbonyl (Fmoc) chemistry. The IC(50) value of HYNIC-Aoc-Nle-CycMSH(hex) was 0.78 ± 0.13 nM for B16/F10 melanoma cells. (99m)Tc(EDDA)-HYNIC-Aoc-Nle-CycMSH(hex) displayed significantly higher uptake (14.26 ± 2.74 and 10.45 ± 2.31% ID/g) in B16/F10 metastatic melanoma-bearing lung than that in normal lung (0.90 ± 0.15 and 0.53 ± 0.14% ID/g) at 2 and 4 h post-injection, respectively. B16/F10 pulmonary metastatic melanoma lesions were clearly visualized by SPECT/CT using (99m)Tc(EDDA)-HYNIC-Aoc-Nle-CycMSH(hex) as an imaging probe at 2 h post-injection, underscoring its potential as an imaging probe for metastatic melanoma detection.

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