Lanreotide的~(188)Re标记及其生物分布
The Labeling of Lanreotide With ~(188)Re and Its Biodistribution
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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 188Re 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 SepPak C18 reverse phase extraction cartridge. The stability of 188Relanreotide can be improved by adding ascorbic acid in vitro. 188Relanreotide is eliminated rapidly from blood and is excreted through liver, the uptake of lung and intestine is higher than other organs.Key words: 188Re labeling; lanreotide; biodistribution