Comparative serum stability of radiochelates for antibody radiopharmaceuticals.
Comparative serum stability of radiochelates for antibody radiopharmaceuticals.
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发表时间：
1987
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通讯作者：
W. Cole;S. Denardo;C. Meares;M. Mccall;G. Denardo;A. Epstein;H. O'Brien;M. K. Moi
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作者：
W. Cole;S. Denardo;C. Meares;M. Mccall;G. Denardo;A. Epstein;H. O'Brien;M. K. Moi
DTPA、benzyl-EDTA和benzyl-TETA标记的单克隆抗体螯合物与~（111）In、~（57）Co和~（67）Cu血清孵育的稳定性存在显著差异。在血清中，~（111）In-苄基-EDTA-抗体比~（111）In-DTPA-抗体稳定。钴-57或67 Cu螯合抗体的稳定性低于111 In螯合抗体; 67 Cu仅作为67 Cu-苄基-TETA-抗体牢固地附着于抗体。放射性金属螯合物自身在血清中的相对稳定性决定了放射性金属螯合抗体的相对稳定性。这些体外研究表明，暴露于复杂蛋白质环境的金属螯合物的体内行为不能通过经典的平衡常数来预测。
Serum incubation of monoclonal antibodies chelate labeled by DTPA, benzyl-EDTA and benzyl-TETA with 111In, 57Co, and 67Cu demonstrated marked differences in their stability. In serum, 111In-benzyl-EDTA-antibody was more stable than 111In-DTPA-antibody. Cobalt-57 or 67Cu chelated antibody were less stable than either 111In chelated antibody; 67Cu was only firmly attached to the antibody as 67Cu-benzyl-TETA-antibody. The relative stability of the radiometal chelated antibodies was paralleled by the relative stability in serum of the radiometal chelates themselves. These in vitro studies suggest that in vivo behavior of metal chelates exposed to a complex protein environment cannot be predicted by classical equilibrium constants.