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[摘要]：The purpose of this study was to determine the melanoma targeting property of Tc-99m-RAD-Lys(Arg(11)) CCMSH in B16/F1 melanoma-bearing C57 mice and compare with Tc-99m-RGD-Lys-(Arg(11)) CCMSH we previously reported. Tc-99m-RAD-Lys-(Arg(11)) CCMSH exhibited rapid and high tumor uptake (19.91 +/- 4.02% ID/g at 2 h post-injection) in B16/F1 melanoma-bearing C57 mice. The tumor uptake of 99mTc-RAD-Lys-(Arg(11)) CCMSH was 1.51, 1.34 and 1.43 times the tumor uptake of Tc-99m-RGD-Lys-(Arg(11)) CCMSH at 0.5, 2 and 4 h post-injection, respectively. Flank B16/F1 melanoma lesions were clearly imaged at 2 h post-injection using Tc-99m-RAD-Lys-(Arg(11)) CCMSH as an imaging probe. The substitution of Gly with Ala significantly enhanced the melanoma uptake of Tc-99m-RAD-Lys-(Arg(11)) CCMSH compared to Tc-99m-RGD-Lys-(Arg(11)) CCMSH in B16/F1 melanoma-bearing C57 mice, providing a new insight into the design of alpha-MSH peptides for melanoma targeting. (C) 2012 Elsevier Ltd. All rights reserved. |
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