Loberg M D, Cooper M, Harvey E, Callery P, Faith W
J Nucl Med. 1976 Jul;17(7):633-8.
A new approach to radiopharmaceutical design is demonstrated, in which small chelating groups capable of binding gamma-emitting radiometals are attached to biologically active molecules, thus producing radiopharmaceuticals based on bifunctional drug and biochemical analogs. The chelating group iminodiacetic acid has been evaluated for this role by examining two N-substituted iminodiacetic acids: methyliminodiacetic acid (MIDA) and N-(2,6-dimethylphenylcarbamoylmethyl)iminodiacetic acid (HIDA). Radiochemical and biologic studies showed that both agents were obtained in high radiochemical purity, were stable in vitro and in vivo, and possessed biologic distributions governed almost exclusively by the N-substituted group. These characteristics of 99mTc-labeled N-substituted iminodiacetic acids, prepared using an "instant kit" method, provide the basis for a valuable new class of radiopharmaceuticals based on bifunctional drug and biochemical analogs.
展示了一种放射性药物设计的新方法，其中能够结合发射γ射线的放射性金属的小螯合基团被连接到生物活性分子上，从而产生基于双功能药物和生化类似物的放射性药物。通过研究两种N-取代亚氨基二乙酸：甲基亚氨基二乙酸（MIDA）和N-（2,6-二甲基苯基氨基甲酰基甲基）亚氨基二乙酸（HIDA），评估了螯合基团亚氨基二乙酸在这方面的作用。放射化学和生物学研究表明，两种试剂均具有高放射化学纯度，在体外和体内均稳定，并且其生物学分布几乎完全由N-取代基团决定。使用“即时试剂盒”方法制备的99mTc标记的N-取代亚氨基二乙酸的这些特性，为基于双功能药物和生化类似物的一类有价值的新型放射性药物提供了基础。
