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一种用于脑成像的新型(99m)锝氮配合物的合成与生物分布

Synthesis and biodistribution of a new (99m)Tc nitrido complex for cerebral imaging.

作者信息

Zhang JunBo, Wang XueBin, Li ChunYun

机构信息

Department of Chemistry, Beijing Normal University, Beijing, 100875, Peoples Republic of China.

出版信息

Nucl Med Biol. 2002 Aug;29(6):665-9. doi: 10.1016/s0969-8051(02)00311-6.

Abstract

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.

摘要

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。

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