中性亲脂性Tc-99m N3S2螯合物的合成、表征及生物分布研究

P.R. Singh , M. Corlija , D.E. Troutner , A.R. Ketring , W.A. Volkert
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引用次数: 1

摘要

已知二胺二硫醇(DADT)在水溶液中与99mTc形成中性亲脂配合物,在水溶液中它们很容易以高收率形成并表现出优异的稳定性。合成了一种新的三胺二硫醇(TADT)配体,对其进行了表征,并证明其形成了中性亲脂性的99mtc螯合物。大鼠体内99mTc螯合物的生物分布表明,静脉注射99mTc螯合物后,其在脑或心脏的摄取较低,但摄取的活性在较长时间内保持不变。该螯合物的体内和体外特性表明,对该TADT配体进行化学修饰可能产生形成具有合适诊断特性的99mTc螯合物的配体系统。
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Synthesis, characterization and biodistribution studies of a neutral-lipophilic Tc-99m N3S2 chelate

Diaminedithiols (DADT) are known to form neutral-lipophilic complexes with 99mTc in aqueous solutions, where they are readily formed in high yields and demonstrate excellent stability. A new triaminedithiol (TADT) ligand was synthesized, characterized and shown to form a neutral-lipophilic 99mTc-chelate. The biodistribution of this 99mTc chelate in rats showed that its uptake in brain or heart following i.v. injection of the 99mTc chelate was low, but activity taken up was retained over a long period of time. The in vivo and in vitro properties of this chelate indicate the possibility that chemical modification of this TADT ligand may produce ligand systems that form 99mTc chelates with suitable diagnostic properties.

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