Cole W C, DeNardo S J, Meares C F, McCall M J, DeNardo G L, Epstein A L, O'Brien H A, Moi M K
Int J Rad Appl Instrum B. 1986;13(4):363-8. doi: 10.1016/0883-2897(86)90011-5.
Simple chelates and chelate conjugated monoclonal antibodies labeled with 111In, 57Co and 67Cu demonstrate marked differences in stability when exposed to a serum environment. Among these radiometals, on DTPA, the order of stability is 111In greater than 57Co much greater than 67Cu. On benzyl-EDTA, the order of stability is 111In congruent to 57Co much greater than 67Cu. Among those investigated, the only serum stable 67Cu chelate found was 67Cu-TETA. The order of stability observed for 57Co vs 67Cu is contrary to published equilibrium constants. These in vitro studies suggest that the in vivo behavior of metal chelates exposed to a complex molecular environment may not be predicted by classically determined equilibrium constants.
用铟 - 111、钴 - 57和铜 - 67标记的简单螯合物以及螯合偶联单克隆抗体在血清环境中稳定性存在显著差异。在这些放射性金属中，对于二乙三胺五乙酸（DTPA），稳定性顺序为铟 - 111大于钴 - 57远大于铜 - 67。对于苄基乙二胺四乙酸（benzyl - EDTA），稳定性顺序为铟 - 111与钴 - 57相当远大于铜 - 67。在所研究的物质中，发现的唯一血清稳定的铜 - 67螯合物是铜 - 67 - 四乙烯五胺（67Cu - TETA）。观察到的钴 - 57与铜 - 67的稳定性顺序与已发表的平衡常数相反。这些体外研究表明，暴露于复杂分子环境中的金属螯合物的体内行为可能无法通过经典测定的平衡常数来预测。
