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  • Title: Preparation, in vitro and in vivo evaluation of (99m)Tc-Annexin B1: a novel radioligand for apoptosis imaging.
    Author: Luo QY, Zhang ZY, Wang F, Lu HK, Guo YZ, Zhu RS.
    Journal: Biochem Biophys Res Commun; 2005 Oct 07; 335(4):1102-6. PubMed ID: 16105648.
    Abstract:
    To develop a radiopharmaceutical for apoptosis imaging, Annexin B1, a new Ca2+-dependent phosphatidylserine (PS)-binding protein, was directly radiolabeled with (99m)Tc. This procedure yields up to 96% of radiochemical purity and higher radiolabeling efficiency. The preparation has been found to be sufficiently stable in vitro. Binding assay with human activated platelets indicated that (99m)Tc-Annexin B1 retained its PS binding activity. Biodistribution in mice revealed that (99m)Tc-Annexin B1 rapidly cleared from the blood and predominantly accumulated in the kidney. The increase in hepatic uptake in anti-Fas antibody treated mice correlated to histologic evidence of fulminant hepatic apoptosis. These data suggest that (99m)Tc-Annexin B1 can be used as a novel radiotracer to detect apoptosis in vivo.
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