Arano Y, Yabuki M, Yahata T, Horiuchi K, Yokoyama A
Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University, Japan.
Chem Pharm Bull (Tokyo). 1990 Nov;38(11):3099-101. doi: 10.1248/cpb.38.3099.
Modification of the chelate ring structure of technetium-99m (99mTc) dithiosemicarbazone (DTS) chelate was carried out in pursuit of a more stable and lipophilic compound. A new DTS chelating molecule, pentane-2,4-dione bis(N-methylthiosemicarbazone) (PETS), with a 5-6-5 membered chelate ring structure, was synthesized and labeled with 99mTc, PETS generated two 99mTc compounds as major products. Both had much higher stability and lipophilicity than a 5-5-5 membered 99mTc DTS compound, as well as great stability in plasma. Both 99mTc-PETS compounds were rapidly extracted by the brain and heart when injected into mice. Thus, the modified chelate ring structure afforded a preferable characteristics to DTS chelate as for the chelating site for technetium radiopharmaceuticals.
为了获得更稳定且亲脂性更强的化合物，对锝-99m（99mTc）二硫代氨基脲（DTS）螯合物的螯合环结构进行了修饰。合成了一种具有5-6-5元螯合环结构的新型DTS螯合分子戊烷-2,4-二酮双（N-甲基硫代氨基脲）（PETS），并用99mTc进行标记，PETS生成了两种主要产物作为99mTc化合物。这两种产物的稳定性和亲脂性均远高于5-5-5元的99mTc DTS化合物，在血浆中也具有很高的稳定性。将两种99mTc-PETS化合物注入小鼠体内后，它们能迅速被脑和心脏摄取。因此，就锝放射性药物的螯合位点而言，修饰后的螯合环结构赋予了DTS螯合物更优良的特性。
