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一种用于脑成像的新型99mTc氮化物配合物的合成与生物分布

Synthesis and biodistribution of a new 99mTc nitrido complex for brain imaging.

作者信息

Zhang J, Wang X, Lu G, Tang Z

机构信息

Department of Chemistry, Beijing Normal University, People's Republic of China.

出版信息

Appl Radiat Isot. 2001 May;54(5):745-8. doi: 10.1016/s0969-8043(00)00322-5.

DOI:10.1016/s0969-8043(00)00322-5
PMID:11258522
Abstract

Bis(N-isobutyl-dithiocarbamato) nitrido technetium-99m complex [99mTcN(IBDTC)2] (IBDTC: N-isobutyl dithiocarbamato) was synthesized by the reduction of 99mTcO4- into [99mTc = N]2+ with stannous chloride in the presence of succinic dihydrazide and propylenediamine tetraacetic acid, followed by the addition of sodium N-isobutyl dithiocarbamate dihydrate. The radiochemical purity of the complex was over 90% as measured by thin layer chromatography. It was stable over 6h at room temperature. Its partition coefficient indicated that it is a good lipophilic complex. Biodistribution in mice demonstrated that the complex accumulated in the brain with high uptake and good retention. The brain uptake (ID%/g) was 6.22, 5.45 and 3.88 and the brain/blood ratio was 1.51, 2.24, 1.84 at 5, 30 and 60 min post-injection, respectively. These results suggest potential usefulness of the complex as a brain perfusion imaging agent.

摘要

双(N-异丁基二硫代氨基甲酸盐)氮基锝-99m配合物[99mTcN(IBDTC)2](IBDTC:N-异丁基二硫代氨基甲酸盐)是通过在琥珀酸二酰肼和丙二胺四乙酸存在下,用氯化亚锡将99mTcO4-还原为[99mTc = N]2+,然后加入N-异丁基二硫代氨基甲酸钠二水合物合成的。通过薄层色谱法测定,该配合物的放射化学纯度超过90%。它在室温下6小时内稳定。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6.22、5.45和3.88,脑/血比分别为1.51、2.24和1.84。这些结果表明该配合物作为脑灌注显像剂具有潜在的应用价值。

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