连接子修饰降低了放射性核素 99m 标记的 Arg-Ala-Asp 偶联的α-黑色素细胞刺激激素肽的肾脏摄取。
Linker modification reduced the renal uptake of technetium-99m-labeled Arg-Ala-Asp-conjugated alpha-melanocyte stimulating hormone peptide.
机构信息
2502 Marble NE, MSC09 5360, College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA.
2502 Marble NE, MSC09 5360, College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA; Cancer Research and Treatment Center, University of New Mexico, Albuquerque, NM 87131, USA; Department of Dermatology, University of New Mexico, Albuquerque, NM 87131, USA.
出版信息
Bioorg Med Chem Lett. 2014 Jan 1;24(1):195-8. doi: 10.1016/j.bmcl.2013.11.042. Epub 2013 Nov 23.
The purpose of this study was to examine the biodistribution of (99m)Tc-RAD-Arg-(Arg(11))CCMSH in B16/F1 melanoma-bearing C57 mice to determine whether the replacement of the Lys linker with an Arg linker could decrease the renal uptake of (99m)Tc-RAD-Arg-(Arg(11))CCMSH. (99m)Tc-RAD-Arg-(Arg(11))CCMSH exhibited rapid and high tumor uptake (17.98±4.96% ID/g at 2h post-injection) in B16/F1 melanoma-bearing C57 mice. As compared to (99m)Tc-RAD-Lys-(Arg(11))CCMSH, the replacement of the Lys linker with an Arg linker dramatically decreased the renal uptake of (99m)Tc-RAD-Arg-(Arg(11))CCMSH by 68%, 62%, 73% and 64% at 0.5, 2, 4 and 24h post-injection, respectively. Flank B16/F1 melanoma lesions were clearly imaged at 2h post-injection using (99m)Tc-RAD-Arg-(Arg(11))CCMSH as an imaging probe.
这项研究的目的是研究 (99m)Tc-RAD-Arg-(Arg(11))CCMSH 在 B16/F1 黑色素瘤荷瘤 C57 小鼠中的生物分布，以确定用 Arg 接头替代 Lys 接头是否可以减少 (99m)Tc-RAD-Arg-(Arg(11))CCMSH 的肾脏摄取。(99m)Tc-RAD-Arg-(Arg(11))CCMSH 在 B16/F1 黑色素瘤荷瘤 C57 小鼠中表现出快速和高的肿瘤摄取（注射后 2 小时为 17.98±4.96% ID/g）。与 (99m)Tc-RAD-Lys-(Arg(11))CCMSH 相比，用 Arg 接头替代 Lys 接头可使 (99m)Tc-RAD-Arg-(Arg(11))CCMSH 的肾脏摄取分别在 0.5、2、4 和 24 小时时降低 68%、62%、73%和 64%。使用 (99m)Tc-RAD-Arg-(Arg(11))CCMSH 作为成像探针，在注射后 2 小时可以清晰地对侧位 B16/F1 黑色素瘤病变进行成像。
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