~3H和~(35)S双标记抗癌药物环硫铂(SHP)
DUAL LABELLING OF SHP WITH ~3H AND ~(35)S
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摘要: <正> 1969年Rosenberg等人,首次报道了顺铂络合物具有广谱性的抗癌活性,得到医学界的关注。由于药代动力学研究的需要,因此对铂络合物进行了氚标记,同时也开展了~3H和~(85)S双标记环硫铂的研究工作。环己二胺二氯铂(简称:环氯铂,DDP)为黄色结晶粉末;环已二胺硫酸铂(Sulfato-1,2-diaminocyclohexane-platinum,简称环硫铂SHP)为白色结晶粉末,易溶于水。化学反应式示于图1。Abstract: The sulfato-1,2-diarnino-cyclohexane platinum (SHP) is a new antitumorigenesis medicine The ~3H-~(34)S-SHP is used for the study of drug metabolism in animals. The dually labelled medicine was prepared by isotope exchange combined with synthesis. The ~3H-dichloro-1, 2-diaminocy-clohexane platinum (DDP) was prepared by electric-discharge in tritium gas. ~3H-~(35)S-SHP was prepared by the reaction of ~3H-DDP with silver sulphate-~(35)S in water. The specific activity of ~3H-~(35)S-SHP was: tritium, 12.7MBq/mg (0.34mCi/mg); sulphur-35, 11.6MBq/mg (0.31mCi/mg). Radiochemical purity was more than 92%. The products were analysed by thin-layer chromatography and infra-red spectrometry.