将octreotide中的苯丙氨酸用酪氨酸替换合成[Tyr3]octreotide,对其进行了131I标记.考察了氯胺T标记法中氯胺T和[Tyr3]octreotide的用量对标记率的影响,观察了Graves眼病相关炎症细胞对131I-[Tyr3]octrotide的体外摄取情况.结果表明,对octreotide进行结构修饰后得到的[Tyr3]octreotide可以用于131I标记;氯胺T法对[Tyr3]octreotide进行131I标记时,氯胺T和[Tyr3]octreotide的最佳用量分别为1.6和1.4 μg,最高标记率为85%;T淋巴细胞、活化的成纤维细胞及血管内皮细胞均能够摄取131-[Tyr3]octreotide,而脂肪细胞的摄取则明显较少.以上结果表明,131I-[Tyr3]octreotide能够被Graves眼病发病过程中的炎症细胞摄取,具有用于Graves眼病发病过程中炎症反应程度评估的应用潜力.但由于摄取量还很小,需要进一步深入研究.%Phenylalanine was displaced by tyrosine in octreotide([Tyr3]octreotide) to study the labeling methods of [Tyr3]octreotide with 131Ⅰ, and the difference uptake ability of 131 Ⅰ-[Tyr3]octreotide in various cell lines of Graves ophthalmopathy were observed. The results showed that [Tyr3]octreotide could be labeled with 131Ⅰ by chloramines-T method and the optimal conditiona was 1.6μg chloramines-T and 1.4μg [Tyr3]octreotide. The labeling efficiency was 85％. T lymphocyte, fibroblast, and HUVEC could accumulate 131 Ⅰ-[Tyr3]octreotide largely compared to lipocyte, which indicated that 131Ⅰ-[Tyr3]octreotide could be combined with inflammatory cells in Graves' ophthalmopathy.
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