Preparation, in vitro and in vivo evaluation of (99m)Tc-Annexin B1: a novel radioligand for apoptosis imaging.
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.
Luo
Quan-Yong
QY
Department of Nuclear Medicine, Shanghai Sixth People's Hospital, Shanghai Jiao Tong University, Shanghai 200233, China. lqyn@sh163.net
Zhang
Zhi-Yong
ZY
Wang
Fang
F
Lu
Han-Kui
HK
Guo
Yu-Zhi
YZ
Zhu
Rui-Sen
RS
D000818:Animals; D017302:Annexins / Q000737:chemistry / Q000493:pharmacokinetics*; D017209:Apoptosis / Q000502:physiology*; D001792:Blood Platelets / Q000000981:diagnostic imaging* / Q000502:physiology*; D002478:Cells, Cultured; D004355:Drug Stability; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D051379:Mice; D008807:Mice, Inbred BALB C; D009928:Organ Specificity; D015609:Organotechnetium Compounds / Q000737:chemistry / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000737:chemistry / Q000493:pharmacokinetics; D015203:Reproducibility of Results; D014018:Tissue Distribution
D017302:Annexins; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C505230:technetium 99m annexin B1