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利尿剂对蟾蜍膀胱上皮细胞中环3',5'-AMP依赖性蛋白激酶的抑制作用。

Inhibition by diuretics of cyclic 3',5'-AMP-dependent protein kinase from toad bladder epithelium.

作者信息

Ferguson D R, Twite B R

出版信息

Br J Pharmacol. 1973 Oct;49(2):288-92. doi: 10.1111/j.1476-5381.1973.tb08374.x.

Abstract
  1. A cAMP-dependent protein kinase enzyme has been isolated from toad bladder epithelium.2. This enzyme catalyses the phosphorylation of histones; a reaction stimulated by 0.1 muM cAMP.3. Activity of this enzyme in the presence of 0.1 muM cAMP was significantly inhibited by 100 muM mercuderamide, bumetanide and frusemide. A small, though statistically insignificant inhibition was seen with the same concentrations of hydrochlorothiazide and ethacrynic acid.4. The half maximal inhibition was achieved with mercuderamide, 5 muM, and with frusemide and bumetanide 600 muM.
摘要
  1. 已从蟾蜍膀胱上皮中分离出一种环磷酸腺苷(cAMP)依赖性蛋白激酶。

  2. 这种酶催化组蛋白的磷酸化;该反应受0.1μM cAMP刺激。

  3. 在0.1μM cAMP存在的情况下,该酶的活性被100μM汞撤米特、布美他尼和呋塞米显著抑制。相同浓度的氢氯噻嗪和依他尼酸也有轻微抑制作用,不过在统计学上无显著意义。

  4. 汞撤米特5μM、呋塞米和布美他尼600μM可达到半数最大抑制。

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How diuretics work.利尿剂的作用机制。
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引用本文的文献

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Furosemide--pharmacology and cellular mode of action.呋塞米——药理学与细胞作用模式
Naunyn Schmiedebergs Arch Pharmacol. 1974;281(3):295-300. doi: 10.1007/BF00500598.
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Active sodium transport by the isolated toad bladder.离体蟾蜍膀胱的主动钠转运
J Gen Physiol. 1958 Mar 20;41(4):657-68. doi: 10.1085/jgp.41.4.657.
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