Development of superior bone scintigraphic agent from a series of up>99m up>Tc-labeled zoledronic acid derivatives
- 作者：Jianguo Lin ; Ling Qiu
- 关键词：Diphosphonic acid ; 99mTc-IPeDP ; Biodistribution ; Pharmacokinetics ; Bone imaging
- 刊名：Applied Radiation and Isotopes
- 出版年：2012
- 期刊代码：6_09698043
- 类别：ce
- 出版时间：May, 2012
- 卷：70
- 期：5
- 页码：848-855
- 文件大小：835 K
摘要
Two novel zoledronic acid (ZL) derivatives, 1-hydroxy-4-(1H-imidazol-1-yl)butane-1,1-diyldiphosphonic acid (IBDP) and 1-hydroxy-5-(1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (IPeDP), were prepared and labeled with the radionuclide technetium-99m in a high labeling yield. In vitro stabilities of these radiolabeled complexes were measured by the radio-HPLC analysis as a function of time, which showed excellent stability with the radiochemical purity of over 95%at 6 h post preparation. Their in vivo biological performances were evaluated and compared with those of up>99m up>Tc-ZL and up>99m up>Tc-MDP (methylenediphosphonic acid). The biodistribution in mice and scintigraphic images of the rabbit showed that the tracer agent up>99m up>Tc-IPeDP had highly selective uptake in the skeletal system and rapid clearance from the blood and soft tissues and an excellent scintigraphic image can be obtained in a shorter time post injection with clear visualization of the skeleton and low soft tissue activity. These preclinical studies suggest that up>99m up>Tc-IPeDP would be a novel superior bone scintigraphic agent.