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HIPDM(NNN′-三甲基-[2-羟基-3-甲基-5碘基]-1,3丙二胺)可通过简单的水相碘-碘交换反应进行标记,它能越过健全血脑屏障进入正常脑组织,是现今第二代脑放射性药物。但在实际标记过程中标记率常出现不规则的波动,其范围在(65—95)%之间,而临床应用要求标记率在95%以上。本文研究了各种氧化剂与还原剂的用量与标记率的关系,求出了在加氧化剂与不加氧化剂条件下,此交换反应的活化能分别为52.9kJ/mol和131kJ/mol,并得到如下结论:
HIPDM (NNN’-trimethyl- [2-hydroxy-3-methyl-5 iodo] -1,3 propanediamine) can be labeled by a simple aqueous iodine-iodine exchange reaction, Brain barrier into normal brain tissue, is now the second generation of brain radiopharmaceuticals. However, in the actual labeling process, the labeling rate often fluctuates irregularly, and its range is between (65-95)%, while the clinical application requires the labeling rate to be above 95%. In this paper, the relationship between the amount of oxidant and reducing agent and the labeling rate was studied. The activation energies of this exchange reaction were found to be 52.9kJ / mol and 131kJ / mol respectively with and without oxidant, in conclusion: