Zhang JunBo, Wang XueBin, Li ChunYun
Department of Chemistry, Beijing Normal University, Beijing, 100875, Peoples Republic of China.
Nucl Med Biol. 2002 Aug;29(6):665-9. doi: 10.1016/s0969-8051(02)00311-6.
The bis(N-isopentyl dithiocarbamato) nitrido technetium-99m complex [(99m)TcN(IPEDTC)(2)] (IPEDTC: N-isopentyl dithiocarbamato) has been synthesized by the reduction of (99m)TcO(4)(-) into (99m)TcN with stannous chloride in the presence of succinic dihydrazide and propylenediamine tetraacetic acid, followed by the addition of the sodium salt of N-isopentyl dithiocarbamate. The radiochemical purity of the complex was over 90% as measured by thin layer chromatography. In vitro studies showed that the complex possessed good stability under physiological conditions. Its partition coefficient indicated that it was a lipophilic complex. The electrophoresis results showed the complex was neutral. Biodistribution in mice showed that the complex accumulated in brain with high uptake and good retention. The brain uptake (ID%/g) was 2.22, 2.06 and 2.45 and the brain/blood ratio was 1.01, 2.34 and 3.22 at 5, 30 and 60 min post-injection, respectively. These results for the complex suggested that it could be a potential brain perfusion imaging agent.
双（N-异戊基二硫代氨基甲酸盐）氮合锝-99m配合物[（99m）TcN（IPEDTC）₂]（IPEDTC：N-异戊基二硫代氨基甲酸盐）的合成方法为：在琥珀酸二酰肼和丙二胺四乙酸存在下，用氯化亚锡将（99m）TcO₄⁻还原为[（99m）TcN]²⁺，随后加入N-异戊基二硫代氨基甲酸钠盐。通过薄层色谱法测定，该配合物的放射化学纯度超过90%。体外研究表明，该配合物在生理条件下具有良好的稳定性。其分配系数表明它是一种亲脂性配合物。电泳结果显示该配合物呈中性。在小鼠体内的生物分布研究表明，该配合物在脑中具有高摄取和良好的滞留性。注射后5、30和60分钟时，脑摄取量（ID%/g）分别为2.22、2.06和2.45，脑/血比分别为1.01、2.34和3.22。该配合物的这些结果表明它可能是一种潜在脑灌注显像剂。
