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甲磺酸萘莫司他对兔皮质集合管中钠和钾转运特性的影响。

Effect of nafamostat mesilate on Na+ and K+ transport properties in the rabbit cortical collecting duct.

作者信息

Muto S, Imai M, Asano Y

机构信息

Department of Nephrology, Jichi Medical School, Tochigi, Japan.

出版信息

Br J Pharmacol. 1993 Jul;109(3):673-8. doi: 10.1111/j.1476-5381.1993.tb13626.x.

Abstract
  1. To determine the mechanism(s) of hyperkalemia caused by nafamostat mesilate (NM), a serine-protease inhibitor, we investigated the effects of the drug on Na+ and K+ transport properties of the collecting duct (CD) cell in the isolated and perfused cortical collecting duct from rabbit kidneys. 2. NM at 10(-4) M in the lumen, hyperpolarized the apical membrane in parallel with increases in transepithelial resistance (RT) and fractional apical membrane resistance (fRA). 3. These effects were completely inhibited by pretreatment with 50 microM luminal amiloride, whereas they were not affected by luminal addition of 2 mM Ba2+. 4. NM at 10(-4) M in the bath slightly but significantly depolarized the basolateral membrane without any changes in RT or fRA, although NM at 10(-5) M in the bath had no effect on the electrical parameters. 5. It is concluded that NM mainly acts on the apical membrane of the CD cell and inhibits the amiloride-sensitive Na+ conductance in the apical membrane.
摘要
  1. 为了确定丝氨酸蛋白酶抑制剂甲磺酸萘莫司他(NM)引起高钾血症的机制,我们研究了该药物对兔肾分离灌注皮质集合管(CD)细胞钠钾转运特性的影响。2. 管腔内10⁻⁴ M的NM使顶膜超极化,同时跨上皮电阻(RT)和顶膜分数电阻(fRA)增加。3. 用50 μM管腔氨氯地平预处理可完全抑制这些作用,而管腔内添加2 mM Ba²⁺则对其无影响。4. 浴槽中10⁻⁴ M的NM使基底外侧膜轻微但显著去极化,RT或fRA无任何变化,尽管浴槽中10⁻⁵ M的NM对电参数无影响。5. 得出结论,NM主要作用于CD细胞的顶膜,抑制顶膜中氨氯地平敏感的钠电导。

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