title: Linker modification reduced the renal uptake of technetium-99m-labeled Arg-Ala-Asp-conjugated alpha-melanocyte stimulating hormone peptide.
abstract: 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.
authors: 2502 Marble NE, MSC09 5360, College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA.
authors: Jianquan
authors: J
authors: Yang
authors: 2502 Marble NE, MSC09 5360, College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA.
authors: Adam M
authors: AM
authors: Flook
authors: 2502 Marble NE, MSC09 5360, College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA.
authors: Changjian
authors: C
authors: Feng
authors: 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. Electronic address: ymiao@salud.unm.edu.
authors: Yubin
authors: Y
authors: Miao
mesh_terms: D000818:Animals; D007668:Kidney / Q000378:metabolism*; D008545:Melanoma / Q000175:diagnosis; D051379:Mice; D008810:Mice, Inbred C57BL; D015394:Molecular Structure; D009842:Oligopeptides / Q000737:chemistry / Q000493:pharmacokinetics*; D013667:Technetium / Q000737:chemistry / Q000493:pharmacokinetics*; D014018:Tissue Distribution; D000521:alpha-MSH / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D009842:Oligopeptides; D000521:alpha-MSH; D013667:Technetium; C047981:arginyl-glycyl-aspartic acid
keywords: Alpha-melanocyte stimulating hormone peptide; Melanocortin-1 receptor; Melanoma imaging; Renal uptake