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成功合成了一种二肽分子-叔丁基氧二肽胺磷酸对碘苯酚酯;采用封管法进行了二肽的~(131)(?)标记,标记率可达85%;采用细胞结合实验对配合物体外生物活性进行了评价,标记抗原保持了原来的亲和力,在标记等操作过程中未受到明显损伤;并对配合物进行了稳定性、亲脂性、急性毒性的考察。结果表明,配合物亲脂性高、毒性低、结构和性能比较稳定,三天后的脱碘率约为12%;成功建立了肿瘤动物模型,得到了配合物在正常小鼠和肿瘤大白兔体内的分布结果。
The dipeptide molecule tert-butyloxy dipeptide amine p-iodophenol phosphate was successfully synthesized. The ~ (131) (?) Labeling of dipeptide was carried out by sealing tube method with the labeling rate up to 85% The in vitro biological activity of the complex was evaluated. The labeled antigen retained its original affinity and was not significantly damaged during the labeling. The stability, lipophilicity and acute toxicity of the complex were investigated. The results showed that the complex has high lipophilicity, low toxicity and relatively stable structure and performance, and the deiodination rate is about 12% after three days. The tumor animal model was successfully established and the complex was obtained in normal mice and tumor rabbits Distribution results.