运输小有机阳离子的老鼠的肝脏。有机阳离子转运体的作用OCT1。

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马特尔F,检查者T, Russ H, Grundemann D,代理我,Koepsell H, Schomig E

运输小有机阳离子的老鼠的肝脏。有机阳离子转运体的作用OCT1。

Naunyn Schmiedebergs拱Aug-Sep杂志。1996;354 (3):320 - 6。

PubMed ID

8878062 (在PubMed

]

文摘

肾脏和肝脏是主要器官循环有机阳离子的失活。最近,一种有机阳离子转运体(OCT1)已经从大鼠肾脏克隆。为了回答这个问题OCT1是否也参与肝吸收有机阳离子有机阳离子的药理特性在肝细胞运输相比,瞬变OCT1表达的特点。大鼠肝细胞的主要文化贪婪地积累小的有机阳离子3 h-1-methyl-4-phenylpyridinium (3 h-mpp +)。在平衡时,肝细胞累积3 h-mpp +五六折。最初的特定3 h-mpp +运输在肝细胞被饱和。half-saturating浓度是13 mumol / l。3 h-mpp +交通敏感奎宁(Ki = 0.79 mumol / l)和cyanine863 (Ki = 0.097 mumol / l)。奎宁和cyanine863是已知的抑制剂的类型我肝阳离子药物运输和肾排泄的有机阳离子,分别。比较3 h-mpp +运输的功能特性与OCT1肝细胞,OCT1不等的表达和特征在哺乳动物细胞系(293细胞)。 Initial rates of 3H-MPP+ transport were saturable, the Km being 13 mumol/l. The rank order of inhibitory potencies of various inhibitors was almost identical in hepatocytes and 293 cells transiently transfected with OCT1. There was a positive correlation between the Ki's for the inhibition of 3H-MPP+ transport in isolated hepatocytes and transfected 293 cells (r = 0.85; P < 0.01; n = 8). The results indicate that OCT1 is functionally expressed not only in the kidney but also in hepatocytes where it is responsible for the transport of small organic cations which, in the past, have been classified as type I substrates.

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药物转运蛋白

药物	转运体	类	生物	药理作用	行动
奎尼丁	溶质载体家庭22个成员1	蛋白质	人类	未知的	抑制剂	细节
奎宁	溶质载体家庭22个成员1	蛋白质	人类	未知的	底物 抑制剂	细节