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我们从肝脏中关于布美他尼以及多特异性胆汁酸/药物转运体的概念中学到了什么。

What we have learned about bumetanide and the concept of multispecific bile acid/drug transporters from the liver.

作者信息

Petzinger E, Blumrich M, Brühl B, Eckhardt U, Föllmann W, Honscha W, Horz J A, Müller N, Nickau L, Ottallah-Kolac M, Platte H D, Schenk A, Schuh K, Schulz K, Schulz S

机构信息

Institute of Pharmacology and Toxicology, Justus Liebig University Giessen, Germany.

出版信息

J Hepatol. 1996;24 Suppl 1:42-6.

PMID:8926368
Abstract

Bumetanide is a weak organic acid which is transported into hepatocytes by a transport system that is related neither to the cloned sodium-dependent taurocholate cotransporting polypeptide Ntcp nor to the cloned organic anion transporting polypeptide oatp. Bumetanide is known to be transported in the kidney by a multispecific organic anion transporter which is the pAH-transporter from the proximal tubule cell. In the liver, bumetanide uptake competes with bile acid uptake, indicating a functionally related multispecific transporter for bile acids and drugs in hepatocytes. This multispecific bile acid transporter MBAT has not been cloned yet. When basolateral membranes were photoaffinity labeled with [3H]bumetanide, several bumetanide binding proteins were separated and identified after protein sequencing from two-dimensional electrophoresis gels.

摘要

布美他尼是一种弱酸,它通过一种转运系统进入肝细胞,该转运系统既与克隆的钠依赖性牛磺胆酸盐共转运多肽Ntcp无关,也与克隆的有机阴离子转运多肽oatp无关。已知布美他尼在肾脏中由一种多特异性有机阴离子转运体转运,该转运体是近端肾小管细胞的对氨基马尿酸转运体。在肝脏中,布美他尼的摄取与胆汁酸的摄取相互竞争,这表明肝细胞中存在一种功能相关的胆汁酸和药物多特异性转运体。这种多特异性胆汁酸转运体MBAT尚未被克隆。当用[3H]布美他尼对基底外侧膜进行光亲和标记时,从二维电泳凝胶上进行蛋白质测序后,分离并鉴定了几种布美他尼结合蛋白。

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J Hepatol. 1996;24 Suppl 1:42-6.
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Br J Pharmacol. 2015 Sep;172(18):4469-4480. doi: 10.1111/bph.13231. Epub 2015 Aug 4.
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Hepatic glutathione and glutathione S-conjugate transport mechanisms.肝脏谷胱甘肽和谷胱甘肽S-共轭物转运机制。
Yale J Biol Med. 1997 Jul-Aug;70(4):287-300.