[利用62Cu-二硫代氨基脲（DTS）螯合物开发中性和双功能放射性药物——64Cu螯合物的基础研究]
[Development of neutral and bifunctional radiopharmaceuticals using 62Cu-dithiosemicarbazone (DTS) chelate--basic studies on 64Cu chelates].
作者信息
Yokoyama A, Hosotani T, Arano Y, Horiuchi K
出版信息
Radioisotopes. 1986 May;35(5):249-55. doi: 10.3769/radioisotopes.35.5_249.
Recent plausibility of generator produced 62Cu, a positron emitter is attracting the interest of those working in the development of bifunctional radiopharmaceuticals (BR). In our development of bifunctional radiopharmaceuticals containing a neutral dithiosemicarbazone (DTS) metal chelate, tertiary (p-DPA-DTS) and quaternary (p-TPA-DTS) amino DTS derivatives were synthesized. As for the basic understanding of their divalent metal (Cu2+, Ni2+, Zn2+) complex formation and stability, spectrophotometrical studies were carried out, comparatively with KTS. Upon assessment of preferential behavior of Cu chelate, the radiolabeled 64Cu-DTS derivative chelates were tested in mice, and potential use with 62Cu in positron nuclear medicine is discussed.
最近，由发生器产生的正电子发射体62Cu具有一定可行性，这引起了从事双功能放射性药物（BR）研发人员的兴趣。在我们开发含中性二硫代氨基脲（DTS）金属螯合物的双功能放射性药物过程中，合成了叔胺（对二苯基丙胺 - DTS）和季胺（对三苯基丙胺 - DTS）氨基DTS衍生物。为了对它们与二价金属（Cu2 +、Ni2 +、Zn2 +）形成络合物及稳定性有基本了解，我们进行了分光光度研究，并与KTS进行了比较。在评估铜螯合物的优先行为后，对放射性标记的64Cu - DTS衍生物螯合物在小鼠体内进行了测试，并讨论了其在正电子核医学中与62Cu的潜在用途。
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