Intracellular Metabolic Fate of Radioactivity after Injection of Technetium-99m-Labeled Hydrazino Nicotinamide Derivatized Proteins

作者: Masahiro Ono , Yasushi Arano , Tomoya Uehara , Yasushi Fujioka , Kazuma Ogawa

DOI: 10.1021/BC980105F

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摘要: Hydrazino nicotinate (HYNIC) has been shown to produce technetium-99m (99mTc)-labeled proteins and peptides of high stability with specific activities. However, persistent localization radioactivity was observed in nontarget tissues such as the liver kidney after administration [99mTc]HYNIC-labeled peptides, which compromises diagnostic accuracy radiopharmaceuticals. Since lysosomes are principal sites intracellular catabolism 99mTc−HYNIC-labeled galactosyl-neoglycoalbumin (NGA) prepared using tricine a co-ligand investigate fate radiolabel lysosomal proteolysis hepatocytes. When injected into mice, over 90% accumulated 10 min injection. At 24 h postinjection, ca. 40% still remained lysosomes. Size-exclusion HPLC analyses homogenates at postinjection showed broad peak ranging from mole...

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