Zhang Junbo, Lin Xiao, Ren Jialei, Liu Jing, Wang Xuebin
Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
Appl Radiat Isot. 2010 Jan;68(1):101-4. doi: 10.1016/j.apradiso.2009.08.019. Epub 2009 Sep 6.
In the present study, the N-benzyl dithiocarbamate (BZDTC) was synthesized and radiolabeled with (99m)TcN intermediate to form the bis(N-benzyl dithiocarbamato) nitrido technetium-99m complex [(99m)TcN(BZDTC)(2)]. The radiochemical purity of the complex was over 90% by thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). It was stable over 6h at room temperature. The partition coefficient and electrophoresis results indicated that this complex was lipophilic and neutral. Biodistribution in mice showed that the complex accumulated in the brain with high uptake. The brain uptake (ID%/g) was 1.87, 1.21 and 0.85 and the brain/blood ratio was 0.75, 1.55 and 1.12 at 5, 30 and 60min post-injection, respectively. These results suggest that this complex could be a potential brain perfusion imaging agent.
在本研究中，合成了N-苄基二硫代氨基甲酸盐（BZDTC），并用(99m)TcN中间体进行放射性标记，形成双（N-苄基二硫代氨基甲酰基）氮鎝-99m络合物[(99m)TcN(BZDTC)(2)]。通过薄层色谱法（TLC）和高效液相色谱法（HPLC）测定，该络合物的放射化学纯度超过90%。它在室温下6小时内稳定。分配系数和电泳结果表明该络合物具有亲脂性且呈中性。在小鼠体内的生物分布显示，该络合物在脑中大量摄取并蓄积。注射后5、30和60分钟时，脑摄取量（ID%/g）分别为1.87、1.21和0.85，脑血比分别为0.75、1.55和1.12。这些结果表明该络合物可能是一种潜在的脑灌注显像剂。
