Synthesis, radiochemistry and biological evaluation of technetium-99m complexes with 1,8-diamine-3,6-dithiaoctane (DDO) ligands

Th Maina, E Chiotellis
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引用次数: 2

Abstract

The synthesis, radiochemical analysis and biological characteristics of some 1,8-diamine-3,6-dithiaoctane derivatives labelled with Tc-99m are reported. Analysis by HPLC shows that most of the 99mTc-chelates are multicomponent. Furthermore, almost all 99mTc-complexes isolated by HPLC are lipophilic and stable in vitro. The biodistributions of the most lipophilic of these complexes were evaluated in mice. The N-morpholinylethyl and N,N'′-bisalicylyl derivatives of 1,8-diamine-3,6-dithiaoctane yielded 99mTc-complexes which exhibit considerable uptake and retention in organs of interest, such as the heart and the brain.

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1,8-二胺-3,6-二硫辛烷(DDO)配体锝-99m配合物的合成、放射化学和生物学评价
本文报道了一些用Tc-99m标记的1,8-二胺-3,6-二硫辛烷衍生物的合成、放射化学分析和生物学特性。HPLC分析表明,大多数99mtc螯合物为多组分。此外,几乎所有的99mtc配合物都具有亲脂性和体外稳定性。这些复合物中最亲脂的生物分布在小鼠中进行了评估。1,8-二胺-3,6-二硫辛烷的N- morpholiny乙基和N,N' ' -双水杨基衍生物产生99mtc复合物,在心脏和大脑等器官中表现出相当大的吸收和保留。
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