117mSn-DTPMP的制备及其生物性质研究

Preparation and biodistribution of 117mSn-DTPMP

  • 摘要: 合成了具有亲骨性的氨基膦酸配体-DTPMP(二乙基三胺基五亚甲基膦酸),制备了117mSn(Ⅳ)-DTPMP,对配合物的稳定性、亲脂性作了研究,考察了它在小鼠体内的分布。将其生物性质与已有文献报道的117mSn(Ⅳ)-DTPA作了比较。结果表明117mSn(Ⅳ)-DTPMP的制备方法简单,配合物稳定性好,亲水,在小鼠体内的生物行为表明117mSn(Ⅳ)-DTPMP的靶向摄取率即骨摄取率较高,高于国外文献报道的117mSn(Ⅳ)-DTPA,是一种极具潜力的新型放射性药物。

     

    Abstract: Abstract: In this work, DTPMP Triethyleneteraamine hexa(methylene phosphonic acid) is synthesized and labelled with 117m Tin (t1/2 14d;γ159KeV,86%). The preparation conditions, stability and lipophilicity of 117mSn(IV)-DTPMP were investigated. Biodistribution of Sn-117m4+ DTPMP in mice was studied. It was found that the quantity of DTPMP and pH value of the prepararion solution had vital effects on the labeling yield of 117mSn(IV)-DTPMP. It was also found that 117mSn(IV)-DTPMP was hydrophilic and stable at room temperature and 37℃ in open air. 117m Sn-117m4+ DTPMP showed unexpectedly high bone uptake and bone-to-blood ratio in the mice. It is higher than that of 117m Sn-117m4+ DTPA. This made it potentially useful as an reagent for skeletal scintigraphy and radiotherapy of bone tumors.

     

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