117Snm188Re、153Sm)-EDTMP的制备及在小鼠体内的生物分布比较

    Preparation and Biodistribution of 117Snm188Re, 153Sm)-EDTMP in Mice

    • 摘要: 本工作通过合成得到配体EDTMP,制备出标记率较高的117Snm(188Re、153Sm)配合物。对3种配合物的体外稳定性、亲脂性进行了考察;对其生物分布作了初步探索,评价了188Re-EDTMP、117Snm-EDTMP作为骨肿瘤治疗药物的可能性。结果表明,3种配合物都易于被骨摄取,但188Re-EDTMP的体内稳定性较差,容易被洗脱,需要进一步改善;与已用于临床应用的153Sm-EDTMP相比,117Snm-EDTMP的小鼠体内分布与其趋势比较一致,在靶组织(脑骨和四肢骨)上的浓集率较高,显示出可用于骨系统疾病治疗的可能性,有进一步研究的价值。

       

      Abstract: In this work, EDTMP is synthesized and radiolabeled with 117Snm, 153Sm, and 188Re separately. The preparation conditions, stability in vitro and lipophilicity of 117Snm (188Re, 153Sm)-EDTMP were investigated. Biodistribution of 117Snm (188Re, 153Sm)-EDTMP in mice were studied. It is found that 117Snm (188Re, 153Sm)-EDTMP are hydrophilic and stable at room temperature and 37℃ in open air. Three kinds of compounds show high bone uptake and bone-to-blood ratio in mice. but 188Re-EDTMP is not stable enough in vivo. 117Snm-EDTMP showes good biological properties, similar to those of 153Sm-EDTMP, including higher uptake in skeleton, lower residue in soft tissues and rapid blood clearance. The result shows that 117Snm-EDTMP is a potential reagent for skeletal scintigraphy and radiotherapy of bone tumors.

       

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