Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China.
Molecules. 2011 Jul 25;16(8):6165-78. doi: 10.3390/molecules16086165.
A series of novel zoledronic acid (ZL) derivatives 1-hydroxy-3-(2-methyl-1H-imidazol-1-yl)propane-1,1-diyldiphosphonic acid (MIPrDP), 1-hydroxy-4-(2-methyl-1H-imidazol-1-yl)butane-1,1-diyldiphosphonic acid (MIBDP), and 1-hydroxy-5-(2-methyl-1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (MIPeDP) were prepared and successfully labeled with (99m)Tc in high labeling yields. The in vitro stability and in vivo biodistribution of (99m)Tc-MIPrDP, (99m)Tc-MIBDP and (99m)Tc-MIPeDP were investigated and compared. The biodistribution studies indicate that the radiotracer (99m)Tc-MIPrDP has highly selective uptake in the skeletal system and rapid clearance from soft tissues. The present findings indicate that (99m)Tc-MIPrDP holds great potential for use in bone imaging.
一系列新型唑来膦酸（ZL）衍生物 1-羟基-3-（2-甲基-1H-咪唑-1-基）丙烷-1,1-二膦酸（MIPrDP）、1-羟基-4-（2-甲基-1H-咪唑-1-基）丁烷-1,1-二膦酸（MIBDP）和 1-羟基-5-（2-甲基-1H-咪唑-1-基）戊烷-1,1-二膦酸（MIPeDP）被制备并成功标记高标记产率的 (99m)Tc。研究并比较了 (99m)Tc-MIPrDP、(99m)Tc-MIBDP 和 (99m)Tc-MIPeDP 的体外稳定性和体内生物分布。生物分布研究表明，放射性示踪剂 (99m)Tc-MIPrDP 在骨骼系统中有高度选择性摄取，并且从软组织中快速清除。目前的研究结果表明，(99m)Tc-MIPrDP 在骨成像中有很大的应用潜力。
