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BAY K 8644对火鸡肌胃肌球蛋白轻链激酶活性的抑制作用。

Inhibition of turkey gizzard myosin light chain kinase activity by BAY K 8644.

作者信息

Movsesian M A, Adelstein R S

出版信息

Eur J Pharmacol. 1984 Aug 3;103(1-2):161-3. doi: 10.1016/0014-2999(84)90204-8.

Abstract

BAY K 8644, a dihydropyridine with positive inotropic effects in smooth muscle, was found to inhibit calmodulin-dependent turkey gizzard myosin light chain kinase activity with an IC50 of 80 microM. In contrast, when myosin light chain kinase was rendered calmodulin-independent by limited proteolysis, drug inhibition was markedly diminished. BAY K 8644 inhibition was additive with that of the negative-inotropic dihydropyridine felodipine. These results indicate that the inotropic effects of dihydropyridines in smooth muscle are unrelated to their calmodulin-antagonistic properties.

摘要

BAY K 8644是一种对平滑肌具有正性肌力作用的二氢吡啶,它能抑制钙调蛋白依赖性火鸡砂囊肌球蛋白轻链激酶的活性,IC50为80微摩尔。相比之下,当通过有限的蛋白水解使肌球蛋白轻链激酶变得不依赖钙调蛋白时,药物抑制作用明显减弱。BAY K 8644的抑制作用与负性肌力二氢吡啶非洛地平的抑制作用具有相加性。这些结果表明,二氢吡啶在平滑肌中的正性肌力作用与其钙调蛋白拮抗特性无关。

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