Zhang JunBo, Song ZhiXin, Jinfeng Chu, Wang XueBin
Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, PR China.
Appl Radiat Isot. 2009 Sep;67(9):1661-3. doi: 10.1016/j.apradiso.2009.03.119. Epub 2009 Apr 16.
The (99m)TcN(PNP5)(DMCHDTC)(DMCHDTC: 2,3-dimethyl cyclohexyl dithiocarbamate, PNP5:bis(dimethoxypropylphosphinoethyl)ethoxyethylamine) complex was synthesized through a ligand-exchange reaction. The two-step procedure involved 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 tetraacetic acid (PDTA) as complexant, followed by the addition of the PNP5 ligand and the DMCHDTC ligand. The radiochemical purity (RCP) of the product was over 90% as measured by thin layer chromatography (TLC). No decomposition of the complex at room temperature was observed over a period of 6 h. Its partition coefficient indicated that it was a lipophilic complex. The electrophoresis results showed the complex was cationic. The biodistribution results in mice indicated that (99m)TcN(PNP5)(DMCHDTC) was significantly retained into the heart. The heart uptake (ID%/g) was 14.47, 12.23 and 8.76 at 5, 30 and 60 min post-injection, respectively. The heart/liver, heart/lung and heart/blood ratios of the complex were 1.24, 3.62 and 23.05 at 60 min post-injection, suggesting it will be a potential myocardial imaging agent.
[(99m)TcN(PNP5)(DMCHDTC)]⁺（DMCHDTC：2,3 - 二甲基环己基二硫代氨基甲酸盐，PNP5：双（二甲氧基丙基膦基乙基）乙氧基乙胺）配合物通过配体交换反应合成。两步法包括首先使(99m)TcO₄⁻与作为氮化物氮原子（N³⁻）供体的琥珀酸二酰肼（SDH）在二水合氯化亚锡作为还原剂和丙二胺四乙酸（PDTA）作为络合剂的存在下反应，随后加入PNP5配体和DMCHDTC配体。通过薄层色谱法（TLC）测定，产物的放射化学纯度（RCP）超过90%。在6小时内未观察到该配合物在室温下分解。其分配系数表明它是一种亲脂性配合物。电泳结果表明该配合物是阳离子型的。在小鼠体内的生物分布结果表明，[(99m)TcN(PNP5)(DMCHDTC)]⁺在心脏中显著潴留。注射后5、30和60分钟时心脏摄取量（ID%/g）分别为14.47、12.23和8.76。注射后60分钟时该配合物的心脏/肝脏、心脏/肺和心脏/血液比值分别为1.24、3.62和23.05，表明它将是一种潜在的心肌显像剂。
