Qiu Ling, Cheng Wen, Lin Jianguo, Zhang Shu, Luo Shineng
Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, 214063, China.
J Labelled Comp Radiopharm. 2013 Sep;56(11):573-80. doi: 10.1002/jlcr.3065. Epub 2013 Sep 16.
In order to develop a superior bone imaging agent, a new radiotracer (99m)Tc-1-hydroxy-5-(2-butyl-1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (BIPeDP) was designed and prepared with good radiochemical yield and stability. The biodistribution in mice shows that (99m)Tc-BIPeDP has high specificity in the skeleton with the maximum uptake of 17.30 ± 0.14 injected dose per gram at 60 min. Kinetics of blood clearance shows that the distribution half-life (T1/2α) and elimination half-life (T1/2β) of (99m)Tc-BIPeDP are 3.7 and 49.7 min, respectively. An excellent image can be obtained at 1-h post-injection with the single photon emission computed tomography bone scanning, which is clearer and quicker than (99m)Tc-zoledronic acid, (99m)Tc-1-hydroxy-5-(1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid, and (99m)Tc-methylenediphosphonic acid All results indicate that (99m)Tc-BIPeDP holds great potential as a novel promising bone imaging agent.
为了开发一种更优的骨显像剂，设计并制备了一种新的放射性示踪剂（99m）Tc-1-羟基-5-（2-丁基-1H-咪唑-1-基）戊烷-1,1-二膦酸（BIPeDP），其具有良好的放射化学产率和稳定性。在小鼠体内的生物分布表明，（99m）Tc-BIPeDP在骨骼中具有高特异性，在60分钟时每克的最大摄取量为17.30±0.14注射剂量。血液清除动力学表明，（99m）Tc-BIPeDP的分布半衰期（T1/2α）和消除半衰期（T1/2β）分别为3.7分钟和49.7分钟。注射后1小时通过单光子发射计算机断层扫描骨扫描可获得优异的图像，比（99m）Tc-唑来膦酸、（99m）Tc-1-羟基-5-（1H-咪唑-1-基）戊烷-1,1-二膦酸和（99m）Tc-亚甲基二膦酸更清晰、更快。所有结果表明，（99m）Tc-BIPeDP作为一种新型有前景的骨显像剂具有巨大潜力。
