The effect of ligand structure on glutathione-mediated decomposition of propylene amine oxime derivatives

C.A. Roth, T.J. Hoffman, M. Corlija, W.A. Volkert, R.A. Holmes
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引用次数: 5

Abstract

Tetramethylpropyleneamine oxime (TMPAO) was synthesized and complexed to 99mTc. 99mTc-TMPAO samples, when challenged with reduced glutathione (GSH), were shown to have two GSH sensitive components, similar to a mixture of d,l and meso 99mTc-HMPAO. One component had a GSH-induced second-order dissociation rate constant (K2) similar to 99mTc-meso-HMPAO. Despite the presence of a large fraction of this component in these samples, brain uptake and autoradiographic studies with 99mTc-TMPAO were equivalent to 99mTc-d,l-HMPAO suggesting that both the d,l and meso 99mTc-TMPAO isomers are efficiently trapped in brain.

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配体结构对谷胱甘肽介导丙烯胺肟衍生物分解的影响
合成了四甲基丙烯胺肟(TMPAO),并与99mTc络合。99mTc-TMPAO样品,当用还原型谷胱甘肽(GSH)刺激时,显示出两种GSH敏感成分,类似于d,l和中位99mTc-HMPAO的混合物。其中一种组分具有类似于99mTc-meso-HMPAO的gsh诱导的二级解离速率常数(K2)。尽管这些样品中存在很大一部分该成分,但99mTc-TMPAO的脑摄取和放射自显影研究结果与99mTc-d,l- hmpao相当,这表明d,l和中位99mTc-TMPAO异构体都有效地被捕获在大脑中。
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