Linker modification reduced the renal uptake of technetium-99m-labeled Arg-Ala-Asp-conjugated alpha-melanocyte stimulating hormone peptide |
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| Institution: | 1. Department of Medical Education, Far Eastern Memorial Hospital, No. 21, Nan-Ya S. Rd., Ban-Chiao, New Taipei City 220, Taiwan;2. Department of Family Medicine, Far Eastern Memorial Hospital, No. 21, Nan-Ya S. Rd., Ban-Chiao, New Taipei City 220, Taiwan;3. Department of Physiology, National Taiwan University College of Medicine, No. 1, Jen-Ai Road, 1st Section, Taipei, 100, Taiwan;4. Department of Neurology, National Taiwan University Hospital, No. 7, Chung-Shan S. Road, Taipei, Taiwan |
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| Abstract: | The purpose of this study was to examine the biodistribution of 99mTc-RAD-Arg-(Arg11)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 99mTc-RAD-Arg-(Arg11)CCMSH. 99mTc-RAD-Arg-(Arg11)CCMSH exhibited rapid and high tumor uptake (17.98 ± 4.96% ID/g at 2 h post-injection) in B16/F1 melanoma-bearing C57 mice. As compared to 99mTc-RAD-Lys-(Arg11)CCMSH, the replacement of the Lys linker with an Arg linker dramatically decreased the renal uptake of 99mTc-RAD-Arg-(Arg11)CCMSH by 68%, 62%, 73% and 64% at 0.5, 2, 4 and 24 h post-injection, respectively. Flank B16/F1 melanoma lesions were clearly imaged at 2 h post-injection using 99mTc-RAD-Arg-(Arg11)CCMSH as an imaging probe. |
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| Keywords: | Alpha-melanocyte stimulating hormone peptide Melanocortin-1 receptor Renal uptake Melanoma imaging |
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