Zhang J, Wang X
Department of Chemistry, Beijing Normal University, People's Republic of China.
Appl Radiat Isot. 2001 Oct;55(4):453-6. doi: 10.1016/s0969-8043(01)00091-4.
In order to seek a new class of brain perfusion imaging agent containing [99mTcN]2+ core, bis(N-cyclobutyl dithiocarbamato) nitrido technetium-99m complex [99mTcN(CBDTC)2] (CBDTC: N-cyclobutyl dithiocarbamato) was synthesized through a simple and efficient method, which can be utilized for the preparation of a radiopharmaceutical through a lyophilized kit formulation. The radiochemical purity of the complex was over 90%, as measured by thin layer chromatography. No decomposition of the complex at room temperature was observed over a period of 6 h. It's partition coefficient indicated that it is a good lipophilic complex. Biodistribution in mice showed that the complex was significantly retained in the brain. The brain uptake (ID %/g) was 3.61, 3.15 and 2.62 and the brain/blood ratio was 1.00, 1.44 and 1.30 at 5, 30 and 60 min post-injection, respectively. These results suggest that this compound could be a potential brain perfusion imaging agent.
为了寻找一类含[99mTcN]2+核心的新型脑灌注显像剂，通过一种简单有效的方法合成了双（N-环丁基二硫代氨基甲酸酯）氮𬭩-99m锝配合物[99mTcN(CBDTC)2]（CBDTC：N-环丁基二硫代氨基甲酸酯），该配合物可通过冻干试剂盒配方用于制备放射性药物。通过薄层色谱法测定，该配合物的放射化学纯度超过90%。在室温下6小时内未观察到该配合物分解。其分配系数表明它是一种良好的亲脂性配合物。在小鼠体内的生物分布表明该配合物在脑中显著滞留。注射后5、30和60分钟时，脑摄取量（ID%/g）分别为3.61、3.15和2.62，脑血比分别为1.00、1.44和1.30。这些结果表明该化合物可能是一种潜在的脑灌注显像剂。
