~(117)Sn~m标记HEDTMP的研究

    PREPARATION AND CHARACTERISTICS OF ~(117)Sn~m-HEDTMP

    • 摘要: 合成了亲骨性的氨基膦类化合物HEDTMP(羟乙基乙二胺三甲撑膦酸 ) ,研究了117Snm(Ⅳ )标记HEDTMP的条件、标记物的稳定性、亲脂性及在小鼠体内的分布。结果表明 ,117Snm(Ⅳ )与HEDTMP在常温下反应 5min即可形成标记率大于 95 %的配合物 ;酸度和配体量对溶液外观有较大的影响 ,但不影响标记率 ;117Snm(Ⅳ ) HEDTMP的稳定性较好 ,属亲水性配合物。小鼠体内分布实验表明 ,配合物主要为骨骼摄取 ,其它组织的摄取趋于本底

       

      Abstract: HEDTMPN-(2-hydroxyethyl)ethylenediamine-1,1,2-tri(methylenephosphonic acid is synthesized and labeled with 117Sn m(Ⅳ).The labeling conditions,stability,lipophiljcity and biodistribution of 117Sn m-HEDTMP in mice are investigated. The results show that the labeling yield of HEDTMP with 117Sn m(Ⅳ) is higher than 95% in 5 min after reaction at room temperature. Acidity and ligand dosage exert great influence to exterior of reaction solution, but labeling yield is still high. The 117Sn m-HEDTMP is very stable at room temperature and 37 ℃ and is hydrophilic. The biodistribution experiments of 117Sn m-HEDTMP in mice show that uptake of the membra bone is higher at 4 h after injection, the uptake of other tissues is low.

       

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