Burns H D, Sowa D T, Worley P, Vaum R, Marzilli L G
J Pharm Sci. 1981 Apr;70(4):436-9. doi: 10.1002/jps.2600700424.
A new method for determining the charge on carrier-free 99mTc-labeled complexes is described. This method and mixed-ligand experiments were used to determine if the charge on the technetium 99m complex of N-(2,6-dimethylphenylcarbamoylmethyl)iminodiacetic acid (I) is - 1 and if the ligand to technetium ratio in the complex is 2:1. The preparation of an iodinated analog (II) of I and its 99mTc-labeled complex is described, as is the biodistribution of the 99mTc-labeled complex in mice. The synthesis of the 51Cr(III)- and 57Co(III)-labeled complexes also are described. The net biliary excretion in mice of both the 99mTc- and 51Cr-labeled complexes of II was significantly greater than that of the 99mTc-labeled complex of I.
本文描述了一种测定无载体99mTc标记配合物电荷的新方法。该方法和混合配体实验用于确定N-(2,6-二甲基苯基氨基甲酰甲基)亚氨基二乙酸(I)的99mTc配合物的电荷是否为-1,以及配合物中配体与锝的比例是否为2:1。文中还描述了I的碘化类似物(II)及其99mTc标记配合物的制备方法,以及99mTc标记配合物在小鼠体内的生物分布。文中还介绍了51Cr(III)和57Co(III)标记配合物的合成。II的99mTc和51Cr标记配合物在小鼠体内的净胆汁排泄量均显著高于I的99mTc标记配合物。