Lanreotide的~(188)Re标记及其生物分布

The Labeling of Lanreotide With ~(188)Re and Its Biodistribution

  • 摘要: 以氯化亚锡为还原剂、酒石酸钠为转换络合剂,用188Re直接标记了Lanreotide;并观察了标记物在动物体内的分布。结果表明,标记反应的最佳条件是:10μgLanreotide、1.5mg酒石酸钠、1.0mg氯化亚锡和100μL(74MBq)188ReO4-溶液,调反应液pH2~3、60℃下反应40min,标记率为88%~94%;标记物经Sep-PakC18柱纯化,放化纯度大于95%;标记物的体外稳定性较差,但加入一定量的Vc可以提高其稳定性;动物实验表明,188Re-lanreotide在肠和肺中的摄取量较高、血液清除速度较快,并经肝脏代谢。

     

    Abstract: Somatostatin analogue peptide (lanreotide) is labeled directly with 188Re via using tartrate as a transchelate agent and stannous chloride as a reducing agent, and the animal test is evaluated. The results show that the labeling yield is 88%~94% under the optimal labeling condition, the radiochemical purity is more than 95% after purification of SepPak C18 reverse phase extraction cartridge. The stability of 188Relanreotide can be improved by adding ascorbic acid in vitro. 188Relanreotide is eliminated rapidly from blood and is excreted through liver, the uptake of lung and intestine is higher than other organs.Key words: 188Re labeling; lanreotide; biodistribution

     

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