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99Tcm-MAG3-Lys-mPEG的制备及其在小鼠体内的分布
引用本文:付成锋,杨顺龙,王毅,刘新起,褚泰伟,胡少文,王祥云. 99Tcm-MAG3-Lys-mPEG的制备及其在小鼠体内的分布[J]. 同位素, 2005, 18(3): 142-147
作者姓名:付成锋  杨顺龙  王毅  刘新起  褚泰伟  胡少文  王祥云
作者单位:北京大学,化学与分子工程学院,应用化学系,北京,100871
基金项目:国家自然科学基金资助课题(B0109)
摘    要:以mPEG-5000、Fmoe-Lysine和MAG3为原料,经过五步反应合成了载体MAG3-Lys-mPEG;对其进行^99Tc^m标记后,进一步研究了标记物的体外稳定性及其在小鼠体内的生物分布。结果表明,^99Tc^m-MAG3-Lys-mPEG的标记率〉98%;标记物在体外有很好的稳定性,在生理盐水中放置24h时,放化纯度〉91%;在血清中温浴16.5h时放化纯度仍〉92%;标记物在小鼠体内的血液清除较快,在肾脏中的摄取最高,标记物主要经肾脏通过尿液排出体外。mPEG有可能用作反义核酸的有效载体。

关 键 词:^99Tc^m mPEG MAG3-Lys-mPEG 生物分布
文章编号:1000-7512(2005)03-0142-06
收稿时间:2004-08-31
修稿时间:2005-07-10

Preparation and Biodistribution of 99Tcm-MAG3-Lys-mPEG
FU Cheng-feng,YANG Shun-long,WANG Yi,LIU Xin-qi,CHU Tai-wei,HU Shao-wen,WANG Xiang-yun. Preparation and Biodistribution of 99Tcm-MAG3-Lys-mPEG[J]. Isotopes, 2005, 18(3): 142-147
Authors:FU Cheng-feng  YANG Shun-long  WANG Yi  LIU Xin-qi  CHU Tai-wei  HU Shao-wen  WANG Xiang-yun
Affiliation:Department of Applied Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China
Abstract:Starting with mPEG-5000,Fmoc-Lysine,and mercaptoacetyltriglycine(MAG_3),the carrier MAG_3-Lys-mPEG is synthesized through five steps,which carrier is labeled by ~(99)Tc~m with labeling efficiency >98%.~(99)Tc~m-MAG_3-Lys-mPEG shows high stability in vitro.The radiochemical purity keeps up >91% and >92% after incubation in saline for 24 h and in bovine serum for 16.5 h,respectively.The biodistribution in mice indicates that ~(99)Tc~m-MAG_3-Lys-mPEG is quickly cleared from blood,and excreted mainly through the urinary systemr.There is the highest uptake in kidneys.It is expected that mPEG may be used as an effective ASODN carrier.
Keywords:^99Tc^m   mPEG   MAGa-Lys-mPEG   biodistribution
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