在获取二硫代氨基脲（DTS）衍生物：99mTc-KTS的中性且紧凑的单体配合物过程中。
In the procurement of a neutral and compact monomeric complex of dithiosemicarbazone (DTS) derivative: 99mTc-KTS.
作者信息
Hosotani T, Yokoyama A, Arano Y, Horiuchi K, Wasaki H, Saji H, Torizuka K
出版信息
Int J Nucl Med Biol. 1986;12(6):431-7. doi: 10.1016/s0047-0740(86)80004-3.
As a basic structure of a bifunctional radiopharmaceutical (BR), dithiosemicarbazone (DTS) enables the formation of a small conjugated chelating ring with divalent metals (Cu2+, Zn2+, Ni2+), yielding stable and compact complexes. In the development of a neutral and compact monomeric DTS complex of technetium (99mTc), a DTS containing ligand, kethoxal-bis(thiosemicarbazone) (KTS) was selected. A well known monomeric Cu-KTS complex (or 64Cu-KTS) is taken as a model compound, and in vitro (TLC, EP, HPLC) and in vivo (mice biodistribution) studies were compared. Using the stannous chloride method, under conditions to avoid the hydrolytic polynucleation of technetium, a good yield of 99mTc-KTS with characteristics resembling the non-charged, compact and stable Cu-KTS is obtained, in in vitro as well as in vivo studies. The importance of DTS as the constituent of a BR is discussed.
作为双功能放射性药物（BR）的基本结构，二硫代氨基脲（DTS）能够与二价金属（Cu2+、Zn2+、Ni2+）形成一个小的共轭螯合环，生成稳定且紧密的配合物。在开发一种中性且紧密的锝（99mTc）单体DTS配合物时，选择了一种含DTS的配体，乙二醛双（硫代氨基脲）（KTS）。一种著名的单体Cu-KTS配合物（或64Cu-KTS）被用作模型化合物，并对其体外（薄层色谱法、电泳法、高效液相色谱法）和体内（小鼠生物分布）研究进行了比较。采用氯化亚锡法，在避免锝水解多核化的条件下，无论是体外研究还是体内研究，都能获得产率良好的99mTc-KTS，其特性类似于不带电荷、紧密且稳定的Cu-KTS。文中讨论了DTS作为BR组成部分的重要性。
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