~(99)Tc~m-AIPO的制备和初步动物实验
PREPARATION AND BIODISTRIBUTION OF ~(99)Tc~m-AIPO
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摘要: 合成了一种新的氨基肟配体 1 氨基 3 (1 咪唑基 )丙醛肟 (1 amino 3 (1 imidazolyl) propanaloxime,AIPO) ,研究了影响99Tcm AIPO标记率的各种因素。实验结果表明 ,在最佳标记条件下 ,标记率为 (94 8± 1 6) %。标记物亲水性高 ,体外稳定性好。纸上电泳结果表明 ,99Tcm AIPO在生理条件下不带电荷。99Tcm AIPO在小鼠体内的分布实验表明 ,肾的摄取最高 (注射后 10min ,摄取率为 2 7% /g) ,滞留时间长 ;该标记物在心肌中有一定的摄取 (注射后 10min ,摄取率为1 3 % /g) ,但清除很快 ;在血 ,肝 ,肺及其他器官中只有少量摄取并很快被清除。通过分子轨道理论计算推测出其可能的结构Abstract: A new hydroxamamide ligand, 1 amino 3 (1 imidazolyl) propanal oxime (AIPO) is synthesized. The experimental conditions for labeling of AIPO with 99 Tc m are optimized based on the examination of various factors influencing the labeling efficiency. By the recommended labeling procedure the mean labeling efficiency is (94.8±1.6) %. The complex shows high hydrophilicity and good stability in Vitro. The yielded complex 99 Tc m AIPO is found by paper electrophoresis to be electrically neutral at physiological condition. The biodistribution of 99 Tc m AIPO in mice demonstrates that 27 %/g selectively accumulates in kidneys at 10 min after injection and retains for a long time. It also accumulates in heart (1.3 %/g at 10 min after injection). However, the complex shows little uptake and quick clearance in blood, liver, lung and other organs. Two possible structures are comparatively studied by ab inito MO calculations and one of them is suggested to be the most reasonable structure.
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