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

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

用锝-99m标记的各种卤化亚氨基二乙酸型化合物在狒狒(Papio ursinus)肝胆显像中的制备及生物动力学评价。
在评估各种99mtc标记的卤化(F, Cl, Br, I)亚氨基二乙酸(IDA)衍生物用于肝胆闪烁成像时,发现在狒狒模型中,这些化合物的表现都不如disida。F-IDA效果最差,胆道排泄最低,肾脏参与程度最高,但多卤素替代在五氟- ida中增加了胆道特异性,减少了尿排泄,以至于五氟- ida因其高分子量而排名第二,甚至高于I-IDA。令人惊讶的是,与Br-IDA和I-IDA相比,Cl-IDA的性能相对较好。
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