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99Tcm-MAG2-Ade肿瘤显像剂的合成及其生物活性研究
引用本文:赵云岭,张春丽,齐传民,游桂荣,付占立,郭凤琴,王荣福.99Tcm-MAG2-Ade肿瘤显像剂的合成及其生物活性研究[J].核化学与放射化学,2005,27(2):82-86.
作者姓名:赵云岭  张春丽  齐传民  游桂荣  付占立  郭凤琴  王荣福
作者单位:北京师范大学,化学系,北京,100875;北京大学,第一医院,核医学科,北京,100034
基金项目:国家自然科学基金资助项目(20171008和20371009);北京师范大学青年科学基金(理科)资助项目(107179)
摘    要:为了制备肿瘤显像剂^99Tc^m标记肽,合成并表征了新的碱基修饰的小肽配体9-N-(S-三苯甲基巯基乙酰)二甘氨酰氨基乙基]腺嘌呤(Tr—MAG2-Ade)。通过直接标记法得到了水溶性配合物^99Tc^m-MAGz—Ade,并对其体外稳定性进行了检测。在荷瘤小鼠体内的生物分布结果表明,^99Tc^m-MAGz—Ade在肿瘤中有较高的摄取,肿瘤与肌肉的摄取比为5.7,肿瘤与血液的摄取比为1.55。血液清除较快,有望用于非腹部肿瘤的显像。

关 键 词:肿瘤显像剂    碱基  生物分布
文章编号:0253-9950(2005)02-0082-05
修稿时间:2005年2月25日

Synthesis and Biodistribution of 99Tcm-MAG2-Ade as A Tumor Imaging Agent
ZHAO Yun-ling,ZHANG Chun-li,QI Chuan-min,YOU Gui-rong,FU Zhan-li,GUO Feng-ping,WANG Rong-fu.Synthesis and Biodistribution of 99Tcm-MAG2-Ade as A Tumor Imaging Agent[J].Journal of Nuclear and Radiochemistry,2005,27(2):82-86.
Authors:ZHAO Yun-ling  ZHANG Chun-li  QI Chuan-min  YOU Gui-rong  FU Zhan-li  GUO Feng-ping  WANG Rong-fu
Affiliation:ZHAO Yun-ling , ZHANG Chun-li, QI Chuan-min, YOU Gui-rong, FU Zhan-li, GUO Feng-qing, WANG Rong-fuDepartment of Chemistry, Beijing Normal University, Beijing 100875, China Department of Nuclear Medicine, Peking University, First Hospital, Beijing 100034, China
Abstract:A new peptide ligand containing adenine 9-N-(S-tritylmercaptoacetyl) diglycylaminoethyl] adenine (Tr-MAG2-Ade) is synthesized and characterized by IR, 1H NMR, 13C NMR, MS and elemental analysis. The complex 99Tcm-MAG2-Ade is prepared by directly labeling method. The partition coefficient and stability in vitro indicated that the complex is hydrophilic and stable over a period of 6 h at room temperature. The biodistribution of 99Tcm-MAG2-Ade in mice bearing S180 tumor shows that a tumor-specific accumulation and quick blood clearance. The uptake ratios of tumor to muscle and blood at 3 hours post injection are 5.70 and 1.55, respectively. The complex 99Tcm-MAG2-Ade appears to be a potential tumor imaging agent.
Keywords:tumor imaging agent  peptide  biological base  biodistribution
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