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首页> 外文期刊>Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine >Development of superior bone scintigraphic agent from a series of 99mTc-labeled zoledronic acid derivatives
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Development of superior bone scintigraphic agent from a series of 99mTc-labeled zoledronic acid derivatives

机译：从一系列99mTc标记的唑来膦酸衍生物开发优异的骨闪烁剂

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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 6h post preparation. Their in vivo biological performances were evaluated and compared with those of 99mTc-ZL and 99mTc-MDP (methylenediphosphonic acid). The biodistribution in mice and scintigraphic images of the rabbit showed that the tracer agent 99mTc-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 99mTc-IPeDP would be a novel superior bone scintigraphic agent.
机译：两种新型唑来膦酸（ZL）衍生物，1-羟基-4-（1H-咪唑-1-基）丁烷-1,1-二基二膦酸（IBDP）和1-羟基-5-（1H-咪唑-1-基）制备了戊烷-1,1-二基二膦酸（IPeDP），并用放射性核素99m进行了标记，产率很高。这些放射性标记的复合物的体外稳定性通过放射性HPLC分析作为时间的函数进行测量，显示出优异的稳定性，制备后6小时的放射化学纯度超过95％。对它们的体内生物学性能进行了评估，并与99mTc-ZL和99mTc-MDP（亚甲基二膦酸）进行了比较。示踪剂99mTc-IPeDP在小鼠体内的生物分布和兔子的闪烁显像图像表明，示踪剂99mTc-IPeDP在骨骼系统中具有高度选择性的吸收，并且可以从血液和软组织中快速清除，并且在注射后的较短时间内可以获得出色的闪烁显像骨骼清晰可见，软组织活动低。这些临床前研究表明，99mTc-IPeDP将是一种新型的优秀骨闪烁显像剂。

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