一种新型脑灌注显像剂^(99m)TcN-CPDTC的制备及生物分布  

Preparation and Biodistribution of the ~ (99m)TcN-CPDTC Complex as a New Potential Brain Perfusion Imaging Agent

作　　者：张俊波[1] 王学斌[1] 

机构地区：[1]北京师范大学化学系,北京100875

出　　处：《高等学校化学学报》2001年第7期1095-1097,共3页Chemical Journal of Chinese Universities

基　　金：北京市科委重点基金 (批准号 :95 330 430 0 )

摘　　要：The complex 99m TcN CPDTC(CPDTC: N cyclopropyl dithiocarbamate trihydrate) 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 nitrido ligand(N 3- ) in the presence of stannous chloride dihydrate as reducing agent and propylenediamine tetraacetic acid(PDTA) as complex agent, followed by the addition of sodium N cyclopropyl 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. Its partition coefficient indicates it is a good lipophilic complex. The biodistribution results in mice indicate that 99m TcN CPDTC is significantly retained into the brain. The brain uptake(%, ID/g) is 4.64, 3 54 and 2.59 and the brain/blood ratio is 1.08, 1.27 and 1.28 at 5, 30 and 60 min post injection respectively. These results suggest potential usefulness of the complex as a brain perfusion imaging agent.The complex 99m TcN CPDTC(CPDTC: N cyclopropyl dithiocarbamate trihydrate) 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 nitrido ligand(N 3- ) in the presence of stannous chloride dihydrate as reducing agent and propylenediamine tetraacetic acid(PDTA) as complex agent, followed by the addition of sodium N cyclopropyl 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. Its partition coefficient indicates it is a good lipophilic complex. The biodistribution results in mice indicate that 99m TcN CPDTC is significantly retained into the brain. The brain uptake(%, ID/g) is 4.64, 3 54 and 2.59 and the brain/blood ratio is 1.08, 1.27 and 1.28 at 5, 30 and 60 min post injection respectively. These results suggest potential usefulness of the complex as a brain perfusion imaging agent.

关 键 词：锝-99m 锝氮配合物 放射性药物 生物分布 脑灌注显像剂 放射性标记物 

分 类 号：R817.41[医药卫生—影像医学与核医学]