碘标锰卟啉及其小鼠体内分布  

Radioiodine-Labeling of MnTBAP and Its Biodistribution in Mice

作　　者：刁尧[1] 刘新宁 官文征[3] 赵文瑾[1] 刘洁[1] 赵恂[1] 于成国[1] 

机构地区：[1]中国医科大学实验技术中心,辽宁沈阳110001 [2]阜新市第二人民医院,辽宁阜新123000 [3]中国医科大学第94期临床医学七年制英文班,辽宁沈阳110001

出　　处：《核化学与放射化学》2012年第5期316-320,共5页Journal of Nuclear and Radiochemistry

基　　金：辽宁省自然科学基金资助项目(No 20092118);辽宁省科学计划项目(No 2009415005);沈阳市科学技术项目(No F11-241-00)

摘　　要：通过131I标记锰卟啉(MnTBAP)探讨锰卟啉在小鼠体内的分布代谢。采用Iodogen法对锰卟啉进行131I标记;以聚酰胺薄膜为支持介质、生理盐水为展开剂,测定标记物的标记率和放化纯度;KM小鼠尾静脉注射131I-MnTBAP(每只185kBq,n=6),分别于注射后5、10、30、60、120、240、1 440min取各脏器,称重、测定计数率,计算每克组织摄取注射剂量的百分率(%ID/g)。结果表明,131I-MnTBAP标记率达96.3%,其放化纯在标记后2、24、48h分别为96%、95%、94.5%;动物实验显示131I-MnTBAP在小鼠体内广泛分布,主要经肝和肾脏进行代谢,肝、肾的放射性摄取在注入后5min时分别为8.34%ID/g、12.23%ID/g,4h时则分别下降为0.34%ID/g、0.73%ID/g,血液中放射性清除较快,注入后5min时血液中放射性摄取为5.55%ID/g,4h为0.86%ID/g。因此,碘标记锰卟啉的标记物体外稳定,体内主要经肝、肾代谢,可用于进一步的微量示踪研究。To investigate the preparation of radioiodinated MnTBAP and its biodistribution in mice,MnTBAP was labeled with 131I using the iodogen method.the radiolabeled compound was characterized by polymide TLC,in which the substratum of saline was used as developing agent.Biodistribution studies were carried out in KM mice.At different times after radiopharmaceutical i.v.administration（185 kBq 131I-MnTBAP/mouse,n=6）,the animals were sacrificed.Blood samples and the tissues of interested were collected,weighted and counted.The percent injected does per gram（%ID/g） was calculated for each sample.The labeling yield of 131I-MnTBAP is 96.3% and its radiochemical purity（RCP） are 96%,95% and 94.5% at 2,24 and 48 h,respectively.Biodistribution in mice demonstrates that 131I-MnTBAP is extensive,and it is metabolized mainly in liver and kidney,as indicated by their uptake of 8.34%ID/g and 12.23%ID/g at 5 min,0.34%ID/g and 0.73%ID/g at 4 h,respectively.The results also show that 131I-MnTBAP could not penetrate the blood-brain barrier.The activity in thyroid increases with time.In conclusion,131I-MnTBAP is stable and it is metabolized mainly in liver and kidney,worthy of further investigation to trace the compound in vivo and in vitro.

关 键 词：锰卟啉 放射性碘标记 体内分布 

分 类 号：R817[医药卫生—影像医学与核医学]