Kubiatowicz D O, Bolles T F, Nora J C, Ithakissios D S
J Pharm Sci. 1979 May;68(5):621-3. doi: 10.1002/jps.2600680528.
Kidney localization of low molecular weight 99mTc-dimercaptodicarboxylic acid complexes was examined in mice. The complexes 99mTc-dimercaptosuccinic acid, 99mTc-dimercaptoglutaric acid, and 99mmTc-dimercaptoadipic acid were formed by reducing sodium 99mTc-pertechnetate with stannous chloride in the presence of 2-10 fold excess ligand at pH 2.5 or 7.5. Kidney specificity decreased as chain length between the mercapto groups increased. Optimum kidney retention occurred with complexes formed at pH 2.5. Complexes prepared at pH 7.5 were rapidly excreted through the urine and feces. Kidney localization of complexes prepared at one pH was not altered if the pH was later changed.
在小鼠体内检测了低分子量99mTc-二巯基二羧酸配合物的肾脏定位情况。99mTc-二巯基琥珀酸、99mTc-二巯基戊二酸和99mTc-二巯基己二酸配合物是在pH值为2.5或7.5的条件下，用氯化亚锡还原高锝酸钠99mTc，同时存在2至10倍过量配体时形成的。随着巯基之间链长的增加，肾脏特异性降低。在pH值为2.5时形成的配合物肾脏保留效果最佳。在pH值为7.5时制备的配合物会通过尿液和粪便迅速排出。如果随后改变pH值，在一个pH值下制备的配合物的肾脏定位不会改变。
