配体结构对谷胱甘肽介导的丙胺肟衍生物分解的影响。

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

作者信息

Roth C A, Hoffman T J, Corlija M, Volkert W A, Holmes R A

机构信息

Research and Nuclear Medicine Services, Harry S. Truman Memorial Veterans Hospital, Columbia, MO 65211.

出版信息

Int J Rad Appl Instrum B. 1992 Oct;19(7):783-90. doi: 10.1016/0883-2897(92)90140-t.

DOI:10.1016/0883-2897(92)90140-t

PMID:1399700

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.

摘要

合成了四甲基丙二胺肟（TMPAO）并使其与99mTc络合。当用还原型谷胱甘肽（GSH）处理99mTc-TMPAO样品时，显示出有两个对GSH敏感的成分，类似于d，l和内消旋99mTc-HMPAO的混合物。其中一个成分的GSH诱导二级解离速率常数（K2）与99mTc-内消旋-HMPAO相似。尽管这些样品中存在很大一部分该成分，但用99mTc-TMPAO进行的脑摄取和放射自显影研究与99mTc-d，l-HMPAO相当，这表明d，l和内消旋99mTc-TMPAO异构体都能有效地滞留在脑中。