177Lu-DOTMP在荷瘤小鼠体内的生物分布和兔SPECT显像研究

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¹⁷⁷Lu-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-DOTMP主要聚集于膀胱组织，即¹⁷⁷Lu-DOTMP主要通过肾排泄；注射后22 h 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。

The Research on Biodistribution of Bearing Sarcoma Mice and Rabbit SPECT Imaging of 177Lu-DOTMP

Cyclen（1,4,7,10-tetraazacyclododecane） and H3 PO3 were used to synthesis DOT- MP （ 1, 4, 7, 10-tetraazacyclododecane-1, 4, 7, 10-Tetraaminomethylenephosphonate）, and then DOTMP was labelled with 177 Lu. 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 radioactivityuptake was mainly in bone and less in other organs and tissues. The results of SPECT ima- ging of Japanese white rabbit showed that the radioactivity was accumulated in bladder. 177Lu_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 that 177 Lu-DOTMP has good bone targeting and is worthy of fur- ther study.