劳卡尼对豚鼠离体心脏制剂微粒体Na⁺、K⁺ -ATP酶的影响。
Influence of lorcainide on microsomal Na+, K(+)-ATPase in guinea-pig isolated heart preparations.
作者信息
Almotrefi A A, Dzimiri N
机构信息
Department of Pharmacology, King Saud University, Riyadh, Saudi Arabia.
出版信息
Br J Pharmacol. 1991 Feb;102(2):530-2. doi: 10.1111/j.1476-5381.1991.tb12205.x.
Abstract
- The effects of lorcainide on the myocardial Mg2(+)-dependent, Na+ and K(+)-activated adenosine triphosphatase (Na+, K(+)-ATPase) were compared in guinea-pig heart preparations with those of ouabain, a specific inhibitor of the enzyme activity. 2. Both ouabain and lorcainide inhibited the microsomal Na+, K(+)-ATPase activity in a concentration-dependent fashion. Their inhibitory effective ranges were 0.05-100 microM and 0.15-125 microM, respectively, and the concentrations for half maximal inhibition (IC50 values) were 2.1 +/- 0.3 and 33.5 +/- 7.3 microM, respectively. 3. In a second series of experiments, the combined effects of the two drugs on the enzyme activity were studied. In these experiments, lorcainide produced a concentration-dependent potentiation of the inhibitory effects of ouabain on Na+, K(+)-ATPase activity. 4. The present study demonstrates that lorcainide is a potent inhibitor of myocardial Na+, K(+)-ATPase.
摘要
- 在豚鼠心脏标本中，比较了劳卡尼对心肌镁离子依赖的、钠钾激活的三磷酸腺苷酶（Na⁺,K⁺-ATP酶）的作用与哇巴因（该酶活性的特异性抑制剂）的作用。2. 哇巴因和劳卡尼均以浓度依赖方式抑制微粒体Na⁺,K⁺-ATP酶活性。它们的抑制有效范围分别为0.05 - 100微摩尔/升和0.15 - 125微摩尔/升，半数最大抑制浓度（IC50值）分别为2.1±0.3和33.5±7.3微摩尔/升。3. 在第二系列实验中，研究了两种药物对酶活性的联合作用。在这些实验中，劳卡尼使哇巴因对Na⁺,K⁺-ATP酶活性的抑制作用呈浓度依赖性增强。4. 本研究表明，劳卡尼是心肌Na⁺,K⁺-ATP酶的强效抑制剂。
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引用本文的文献
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