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肝脏切片对静脉注射和口服胆道造影剂的摄取。

Liver slice uptake of intravenous and oral biliary contrast media.

作者信息

Müller W E, Stillbauer A E

出版信息

Arch Int Pharmacodyn Ther. 1980 Aug;246(2):187-204.

PMID:7436626
Abstract

Using the liver slice technique, the uptake of five intravenous (including iodipamide, ioglycamide, iotroxamide, and iodoxamide) and one oral (iopodate) biliary contrast media into the rat liver was investigated. For all six compounds a saturable high-affinity and a nonsaturable low-affinity uptake system could be identified. There is no great difference of the liver uptake of the five intravenous compounds, but the oral compound iopodate is taken up by the rat liver to a much higher extent than the intravenous compounds. Since the liver slice uptake of the biliary contrast media was not clearly depending on metabolic energy, the presented results favor intracellular binding more than an active carrier as uptake mechanism. Human serum albumin strongly reduces hepatic uptake of all six compounds. The inhibition of the uptake was directly depending on the degree of serum albumin binding. No evidence for a carrier role of serum albumin within the uptake process could be found. The uptake mechanism of the liver for the biliary contrast media failed to be very specific, since liver slice uptake could be inhibited by iopanoate, bromosulfthalein, ouabain, and taurocholate and by each of the contrast media itself.

摘要

采用肝切片技术,研究了五种静脉注射用(包括碘番酸、碘甘卡明、碘托酰胺和碘多酰胺)和一种口服(碘泊酸盐)胆道造影剂在大鼠肝脏中的摄取情况。对于所有这六种化合物,均可鉴定出一种可饱和的高亲和力摄取系统和一种不饱和的低亲和力摄取系统。五种静脉注射化合物在肝脏中的摄取情况差异不大,但口服化合物碘泊酸盐被大鼠肝脏摄取的程度远高于静脉注射化合物。由于胆道造影剂在肝切片中的摄取并不明显依赖于代谢能量,因此所呈现的结果更支持细胞内结合而非主动载体作为摄取机制。人血清白蛋白可显著降低所有六种化合物的肝脏摄取。摄取的抑制作用直接取决于血清白蛋白的结合程度。在摄取过程中未发现血清白蛋白具有载体作用的证据。肝脏对胆道造影剂的摄取机制并非非常特异,因为肝切片摄取可被碘泛酸、溴磺酞钠、哇巴因和牛磺胆酸盐以及每种造影剂本身所抑制。

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