N_2S_2或N_3S型配体的合成、^(99)Tc^m标记及生物分布研究  

SYNTHESIS OF LABELED PEPTIDE COMPLEXES WITH TECHNETIUM-99m AND BIODISTRIBUTION IN MICE

作　　者：张华北[1] 郭雪峰[1] 齐传民[1] 李波[1] 冯淑娟[1] 金未[1] 杨凌春[1] 刘伯里[1] 戴梅[1] 

机构地区：[1]北京师范大学化学系,北京100875

出　　处：《核化学与放射化学》2002年第4期198-203,226,共7页Journal of Nuclear and Radiochemistry

基　　金：国家自然科学基金资助项目 ( 2 980 10 0 2 ;2 0 1710 0 8)

摘　　要：以MAG3为基本分子骨架 ,根据构效关系 ,分别引入合适的天然氨基酸 ,设计合成了 4种N2 S2 或N3S型小分子多肽新配体 ,并通过了IR ,1HNMR ,13CNMR ,MS谱学鉴定和元素分析表征。采用葡庚糖酸钙(GH)交换法对 4个配体进行了99Tcm 标记 ,研究了配合物在小鼠体内的生物分布特征。结果表明 ,99Tcm MVGG肾摄取较高 ,滞留时间较长 ,血清除快 ,且肾与其它组织的活度比值高 ,具备成为肾功能显像剂的条件 ;99Tcm MPGG肾初始摄取较高 ,R(肾 /血 )活度比值高 ,但肾清除较快 ,R(肾 /肝 )活度比值较低 ;99Tcm MVTC和99Tcm MPTC心肌初始摄取均较高 。Four new N 2S 2 or N 3S small peptide chelators are synthesized based on renal function imaging agent 99Tc m-MAG 3 as fundamental structure by introducing natural amino acids according to reasonable structure-activity relationships. All the new compounds are identified on the basis of the spectroscopic data, such as IR, 1H NMR, 13C NMR, MS and elemental analysis. All the chelators are labeled with technetium-99m and further tested for the biological activity in mice. The biodistribution results in mice indicate that 99Tc m-MVGG has high kidney uptake, good retention, quick blood clearance and high activity ratios of kidney to other tissues, suggesting that it would be a new potential renal function imaging agent; 99Tc m-MPGG has better kidney accumulation and higher activity ratios of kidney to blood; 99Tc m-MVTC and 99Tc m-MPTC have higher heart accumulation.

关 键 词：N3S型配体 合成 肾功能显像剂 多肽 生物分布 ^99Tc^m-MVGG N2S2型配体 锝99 放射性标记 

分 类 号：R817.47[医药卫生—影像医学与核医学]