用99m锝标记的各种卤代亚氨基二乙酸类化合物在狒狒（山魈）模型中用于肝胆闪烁显像的制备及生物动力学评估。

Preparation and biokinetic evaluation of various halogenated iminodiacetic acid-type compounds labeled with technetium-99m for hepatobiliary scintigraphy in the baboon (Papio ursinus) model.

作者信息

Dormehl I C, Grobbelaar C, van Wyk A, Jacobs L, Maree M, Oliver D

机构信息

Institute for Life Sciences, University of Pretoria, South Africa.

出版信息

Am J Physiol Imaging. 1990;5(1):3-7.

PMID:2372410

Abstract

In an evaluation of various 99mTc-labeled halogenated (F, Cl, Br, I) iminodiacetic acid (IDA) derivatives for hepatobiliary scintigraphy, it was found that, in the baboon model, none of these compounds performed as well as did disida. F-IDA was least effective, with the lowest biliary excretion and highest renal participation, but multihalogen substitution as in penta-F-IDA increased the biliary specificity and reduced urinary excretion to the extent that penta-F-IDA scored second to disida and even above I-IDA, with its high molecular weight. Surprising also was the relatively good performance of Cl-IDA compared to Br-IDA and I-IDA.

摘要

在对用于肝胆闪烁显像的各种99mTc标记的卤代（氟、氯、溴、碘）亚氨基二乙酸（IDA）衍生物进行评估时发现，在狒狒模型中，这些化合物的表现均不如二异丙基IDA（disida）。氟代IDA（F-IDA）效果最差，胆汁排泄最低，肾脏摄取最高，但像五氟代IDA（penta-F-IDA）那样的多卤代取代增加了胆汁特异性并减少了尿液排泄，以至于五氟代IDA仅次于二异丙基IDA，甚至超过了分子量较大的碘代IDA（I-IDA）。与溴代IDA和碘代IDA相比，氯代IDA（Cl-IDA）的表现相对较好，这也令人惊讶。