有机阴离子
化学
有机阴离子转运多肽
有机阳离子转运蛋白
有机阴离子转运蛋白1
钠
两亲性
奎尼丁
药物化学
生物化学
离子
运输机
有机化学
药理学
生物
基因
聚合物
共聚物
作者
Jessica E. van Montfoort,Bruno Hagenbuch,Karin Fattinger,Majon Muller,Geny Groothuis,Dirk K. F. Meijer,Peter J. Meier
出处
期刊:PubMed
日期:1999-10-01
卷期号:291 (1): 147-52
被引量:29
摘要
Hepatic uptake of albumin-bound amphipathic organic cations has been suggested to be mediated by multispecific bile salt and organic anion transport systems. Therefore, we investigated whether the recently cloned rat organic anion transporting polypeptides 1 and 2 as well as the human organic anion transporting polypeptide might be involved in the hepatocellular uptake of bulky type II organic cations. In cRNA-injected Xenopus laevis oocytes, all three carriers mediated uptake of the known type II model compounds N-(4, 4-azo-n-pentyl)-21-deoxy-ajmalinium and rocuronium, whereas the newly synthesized type II model compounds N-methyl-quinine and N-methyl-quinidine were transported only by the human organic anion transporting polypeptide. This carrier-mediated uptake of N-methyl-quinine and N-methyl-quinidine was sodium-independent and saturable with apparent K(m) values of approximately 5 and approximately 26 microM, respectively. In contrast to bulky type II organic cations, more hydrophilic type I organic cations such as tributylmethylammonium and choline were not transported by any of the organic anion transporting polypeptides. These findings demonstrate that organic anion transporting polypeptides can also mediate hepatocellular uptake of type II organic cations, whereas uptake of small and more water-soluble type I cations is mediated by different transport systems such as the organic cation transporters.
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