Arano Y, Yokoyama A, Magata Y, Horiuchi K, Saji H, Torizuka K
Int J Rad Appl Instrum A. 1986;37(7):587-92. doi: 10.1016/0883-2889(86)90077-8.
Recently, technetium-99m (99mTc) labeling of proteins through the use of a bifunctional chelating agent (BCA) has been reported. In previous work, a BCA containing a di(N-methylthiosemicarbazone) (DTS) moiety for 99mTc has offered good potential; however, conjugation with bulky proteins has induced some steric interference in the 99mTc labeling step using the stannous chloride method. In order to minimize this effect, changes in the hydrocarbon chain length (spacer) between the DTS and the protein binding site (carboxyl group), as well as the chemical state of the reducing agent, stannous chloride, were considered of interest. DTS molecules with variable spacer length (n = 0, 2, 4) were synthesized, coupled with human serum albumin and labeled with 99mTc. Also, stannous chloride prepared in different media was evaluated. Validity of the present approach is tested and discussed.
最近，有报道称通过使用双功能螯合剂（BCA）对蛋白质进行锝-99m（99mTc）标记。在先前的工作中，一种含有用于99mTc的二（N-甲基硫代氨基脲）（DTS）部分的BCA具有良好的潜力；然而，与大分子蛋白质结合在使用氯化亚锡法的99mTc标记步骤中引起了一些空间位阻。为了最小化这种影响，人们认为DTS与蛋白质结合位点（羧基）之间的烃链长度（间隔基）的变化以及还原剂氯化亚锡的化学状态值得关注。合成了具有可变间隔基长度（n = 0、2、4）的DTS分子，将其与人血清白蛋白偶联并用99mTc标记。此外，还评估了在不同介质中制备的氯化亚锡。对本方法的有效性进行了测试和讨论。
