两种~(125)I标记的神经紧张肽类似物的动物体内分布
Biodistribution Properties of Two ~(125)I Labeled Novel Neurotensin Analogues
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摘要: 采用氯胺T法对神经紧张肽类似物NT1和NT2进行125I标记,并观察了125I-NT1和125I-NT2在正常小鼠和荷人结肠癌裸鼠体内的分布。结果显示,125I-NT1和125I-NT2标记率分别为68%和76%,经Sep-Pak-C18反相柱分离后,放化纯度>98%;两种125I标记的NT类似物血液清除较快,部分由肝、肾脏排泄,体内分布基本一致,对肿瘤具有相似的靶向性。这说明两种NT类似物N端Arg和Lys互换对其体内的分布特性没有明显影响。与125I-NT1相比,125I-NT2在体内的清除速度更快,在胃中更稳定,其T/NT也更高,更适于作进一步研究。Abstract: Two novel neurotensin analogues NT1(Arg-Lys-ProTyr-TLe-Leu)and NT2(Lys-Arg-Pro-Tyr-TLe-Leu) are labeled with ~(125)I by Chloramine T method.Biodistribution studies of ~(125)I-NT1 and ~(125)I-NT2 are carried out in ICR mice and Balb/c nude mice bearing HT29 xenografts.The results indicate that ~(125)I-NT1 and ~(125)I-NT2 have similar biodistribution and specific tumor targeting properties.~(125)I-NT2 shows promising proterties and is worth of further investigation.
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