Characterization of Technetium-99m Complexes of Pentane-2,4-dione Bis(N-methylthiosemicarbazone)
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概要
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Further characterization of the two neutral technetium-99m (^<99m>Tc) complexes of pentane-2,4-dione bis-(N-methylthiosemicarbazone) (PETS) was carried out using a new dianionic PETS derivative, 3,3-dimethyl-pentane-2,4-dione bis(N-methylthiosemicarbazone) (DM-PETS), and the well characterized ^<99m>Tc complex of 2,2,9,9-tetramethyl-4,7-diaza-1,10-decanedithiol (DADT) as references. While PETS generated two neutral ^<99m>Tc complexes, ^<99m>Tc-PETS-L_1 and ^<99m>Tc-PETS-L_2,by both the stannous reduction method and the ligand exchange reaction with six-coordinated ^<99m>Tc(V) complex of N, N'-ethylenebis(acetylacetone imine), DM-PETS formed only one neutral ^<99m>Tc complex. ^<99m>Tc-PETS-L_2,the more lipophilic complex of the two ^<99m>Tc-PETS, was obtained with a much higher yield than ^<99m>Tc-PETS-L_1 by the ligand exchange reaction of PETS with the five-coordinated ^<99m>Tc(V) complex of glucoheptonate. In addition, while ^<99m>Tc-PETS-L_2 and ^<99m>Tc-DADT remained unchanged in the presence of CN^- anions, a breakdown of the original complexes was observed in ^<99m>Tc-PETS-L_1 and ^<99m>Tc-DM-PETS. All four ^<99m>Tc complexes exhibited similar brain, heart and pancreas extraction when injected into mice. These cummulative results imply that ^<99m>Tc-PETS-L_1 and ^<99m>Tc-DM-PETS are six-coordinated mononuclear ^<99m>Tc(V) complexes and that ^<99m>Tc-PETS-L_2 is a five-coordinated mononuclear ^<99m>Tc(V) complex. These results also suggest that while the chelate ring structure of the ^<99m>Tc-dithiosemicarbazone (DTS) chelate played a singificant role in its stability, ionization of the third proton of the PETS molecule and the subsequent resonating structure afforded further stability to the ^<99m>Tc-PETS complex. Markedly high lipophilicity of the ^<99m>Tc-PETS-L_2 may also be explained by assuming that ^<99m>Tc-PETS-L_2 is the five-coordinated resonating structure.
- 公益社団法人日本薬学会の論文
- 1991-01-25
著者
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横山 陽
Department Of Radiopharmaceutical Chemistry Faculty Of Pharmaceutical Sciences Kyoto University
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荒野 泰
千葉大 大学院薬学研究院
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荒野 泰
千葉大学薬学部
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荒野 泰
Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University
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矢吹 昌司
Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University
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JONES Alun
Department of Radiology, Harvard Medical School
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矢吹 昌司
Department Of Radiopharmaceutical Chemistry Faculty Of Pharmaceutical Sciences Kyoto University
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Jones Alun
Department Of Radiology Harvard Medical School
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