新型骨显像剂99mTc-EDP的合成与研究

以亚磷酸二乙酯为原料,经多步反应合成了亚乙烯基二膦酸(EDP)配体.通过1HNMR测定进行了结构确认;经99mTc标记后,标记率高于95%.体外稳定性测定表明,6h后放化纯度仍保持在90%以上.小鼠体内分布实验表明,99mTc-EDP与99mTc-MDP(99mTc-亚甲基二膦酸)均具有较强的亲骨性能,99mTc-EDP骨摄取优于99mTc-MDP,并且随着时间的增加,骨与非靶器官摄取的比值都在增加,远远高于99mTc-MDP.进行了狗SPECT全身骨显像实验,2h后获得清晰的图像.

THE SYSTHESIS AND STUDY OF A NEW KIND OF BONE IMAGING AGENT 99mTc-EDP

Ethenylidenebisphosphonate(EDP)is synthesized successfully from the initial compound, diethyl phosphate. Its structure is determined by 1HNMR. The labelling yields of 99mTc-EDP is more than 95% under the selected labelling condition. The stability study of 99mTc-EDP indicates that its radiochemistry purity is more than 90% after 6 h. The study of the biodistribution in mice of 99mTc-EDP demonstrates that 99mTc-EDP and 99mTc-MDP all have a high bone uptake, and the bone uptake of 99mTc-EDP exceeds 99mTc-MDP and it improves with the time going as well as the ratio between of bone and other organ, which also is farthest higher than 99mTc-MDP. The whole body bone imaging in dog by SPECT is studied after injecting 99mTc-EDP. The results indicate very clear scintigraphic images obtained for 99mTc-EDP at 2 h p.i..