【摘要】 合成了4种斑蝥素衍生物及其与二乙三氨五乙酸环二酸酐偶联(BDTPAA)得到的偶联物,并分别进行99Tcm标记,在SnCl2浓度为3 0mmol/L,pH=7～8,反应温度为100℃,反应时间为30min时,标记率大多达到90%以上。选择其中2种标记率较高的配合物进行动物体内分布试验。结果表明,99Tcm N 氨基 5,6 二溴去甲基斑蝥素在肝、胆中浓集较高,99Tcm DTPA N 氨基 5,6 二溴去甲基斑蝥素在肾中浓集较高,两者在血液中的清除都较快。更多还原

【Abstract】 Four kinds of norcantharidin derivatives are synthesized and the coupling compounds are prepared individually. The compounds are labeled by))~99)Tc~m and the labeling yield is mostly over 90% under the best condition (3.0 mmol/L SnCl2;pH=7～8; reaction temperature, 100 ℃;reaction time, 30 min). Two samples are chosed for biodistribution experiments. The reaults show that the labeled N-animo-5,6-bibromine norcantharidin has a higher uptake in liver and gallbladder, and the labeled DTPA-N-)animo-5,6-bibromine norcantharidin is mainly concentrated in kidney. Both labeled compounds clear quickly in blood.更多还原