一种新型含[^(99m)TcN]^(2+)核脑显像剂的初步研究  

A PRELIMINARY STUDY ON A NEW BRAIN IMAGING AGENT CONTAINING [^(99m)TcN]^(2+) CORE

作　　者：张俊波[1] 王学斌[1] 庞楠楠[1] 罗权[1] 董华斌[1] 

机构地区：[1]北京师范大学化学系,北京100875

出　　处：《北京师范大学学报（自然科学版）》2003年第4期507-510,共4页Journal of Beijing Normal University(Natural Science)

基　　金：国家自然科学基金资助项目 (2 0 2 0 10 0 4 ) ;北京师范大学青年科学基金资助项目 ;北京师范大学本科生研究基金资助项目

摘　　要：采用了SnCl2 ·2H2 O为还原剂 ,丁二酰二酰肼 (SDH)为N3- 离子提供体 ,在室温下制备[99mTcN]2 +中间体 ,然后与三水·N 环丁基 二硫代氨基甲酸钠 (CBDTC)发生配体交换反应得到放射化学纯度大于 90 %的99mTcN CBDTC配合物 .该配合物在室温下放置 6h内稳定 ,脂水分配系数结果表明该配合物是一脂溶性较好的物质 .小鼠体内生物分布表明99mTcN CBDTC在脑中有较好的摄取和滞留 ,脑的质量摄取率am ,br在注射后 5 ,30 ,6 0min时分别达到 3.6 1,3.15 ,2 .6 2 %·g- 1,脑与血的质量摄取率am ,br与am ,bl的比分别为 1.0 0 ,1.4 4,1.30 ,有望发展成为一类新型脑灌注显像剂 .The complex 99m TcN-CBDTC (CBDTC:N-cyclobutyl dithiocarbamate trihy-drate) is synthesized through ligand-exchange reaction. The two step procedure involves the initial reaction of 99m TcO -_4 with succinic dihydrazide (SDH) as a donor of nitride nitrogen atom (N 3- ) in the presence of stannous chloride dihydrate as reducing agent and propylenediamine tetracetic acid (PDTA) as complexant, followed by the addition of sodium N-cyclobutyl dithiocarbamate trihydrate. The radiochemical purity (RCP) of the product is over 90% as measured by thin layer chromatography (TLC). It is stable over 6 h at room temperature(25 ℃). Its partition coefficient indicates that it is a good lipophilic complex. The biodistribution results in mice indicate that 99m TcN-CBDTC is significantly retained in brain. The brain uptake ( a_m ) is 3.61, 3.15 and 2.62 %·g -1 and the a_ m ,br / a_ m ,bl is 1.00, 1.44 and 1.30 at 5, 30 and 60 min post-injection respectively. These results suggest the potential usefulness of the complex as a brain perfusion imaging agent.

关 键 词：锝-99m 锝氮核 锝氮-三水·N-环丁基-二硫代氨基甲酸钠配合物 脑灌注显像剂 生物分布 

分 类 号：R817.4[医药卫生—影像医学与核医学] O615.4[医药卫生—放射医学]