177Lu-DOTMP在荷瘤小鼠体内的生物分布和兔SPECT显像研究

摘要

以1,4,7,10-四氮杂环十二烷和亚磷酸为原料合成了1,4,7,10-四氮杂环十二烷-1,4,7,10-四甲撑膦酸(DOTMP),并对其进行了177Lu标记；观察了177 7Lu- DOTMP在骨转移癌模型鼠体内的生物分布,并对日本大耳白兔进行显像.荷瘤鼠体内的生物分布结果显示:177Lu- DOTMP可以选择性地在骨组织吸收,具有良好的靶向性,而且在血中清除较快,在其它脏器只有少量的摄取.日本大耳兔显像结果显示:177Lu -DOT-MP主要聚集于膀胱组织,即177Lu-DOTMP主要通过肾排泄；注射后22h骨骼放射性摄取明显,46 h骨骼中放射性积聚更多.以上结果表明,177Lu- DOTMP具有良好的骨靶向性,值得进一步研究.%Cyclend ,4,7,10-tetraazacyclododecane) and H3POS were used to synthesis DOT-MP (1, 4, 7, 10-tetraazacyclododecane-l, 4, 7, 10-Tetraaminomethylenephosphonate), and then DOTMP was labelled with l77Lu. The research of biodistribution of 177 Lu-DOTMP in model mice bearing S180 sarcoma and SPECT imaging in Japanese white rabbit were also carried out. The results of biodistribution of bearing S180 mice indicated that 177 Lu-DOTMP cleared rapidly from blood and was selectively delivered to target bone. The radioactivity uptake was mainly in bone and less in other organs and tissues. The results of SPECT imaging of Japanese white rabbit showed that the radioactivity was accumulated in bladder. l77Lu-DOTMP was mainly excreted by kidney. The uptake of the activity in the skeleton was observed significatantly within 22 h post-injection and it became quite significant at 46 h post-injection. It indicated that177 Lu-DOTMP has good bone targeting and is worthy of further study.