Interaction of bretylium tosylate with guinea-pig myocardial Na(+)-K(+)-ATPase.
Interaction of bretylium tosylate with guinea-pig myocardial Na(+)-K(+)-ATPase.
复制标题
甲苯磺酸溴节铵与豚鼠心肌 Na( )-K( )-ATP 酶的相互作用。
DOI：
10.1016/0306-3623(91)90233-v
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发表时间：
1991
期刊：
影响因子：
--
通讯作者：
A. Almotrefi
中科院分区：
文献类型：
--
作者：
N. Dzimiri;A. Almotrefi
1. 布雷利姆对心肌Mg（2+）依赖性、Na (+)-K (+)- atp酶的影响（ec3.6）。1.3)与瓦巴因在豚鼠心脏制剂中的活性比较。2. 瓦巴因和布雷特利姆对微粒体Na (+)-K (+)- atp酶活性的抑制分别在0.01-100和1.0-4000 μ m范围内呈浓度依赖性。溴代溴的IC50值为2.45+/-0.17 mM，溴代溴的IC50值为1.93+/-0.27 mM。3. 在另一组实验中，分别与2.5微米或5.0微米的瓦巴因联合使用布雷氏菌对酶活性的影响进行了测试。4. 两种药物的联合作用导致单个药物的总抑制活性的净降低，布雷氏菌浓度越高，这种降低越明显。这一趋势似乎表明两种药物在抑制Na (+)-K (+)- atp酶活性方面存在竞争性相互作用模式。5. 结果表明，布雷利姆是心肌Na (+)-K (+)-ATP酶对瓦阿巴因抑制的ATP水解的有效抑制剂。这些作用可能与它的一些心脏作用有关。
1. The effects of bretylium on myocardial Mg (2+)-dependent, Na (+)-K (+)-ATPase (EC 3.6. 1.3) activity were compared with those of ouabain in guinea-pig heart preparations. 2. Both ouabain and bretylium inhibited microsomal Na (+)-K (+)-ATPase activity in a concentration-dependent fashion in the range of 0.01-100 and 1.0-4000 microM, respectively. The IC50 values were 1.93+/-0.27 microM for ouabain and 2.45+/-0.17 mM for bretylium. 3. In another set of experiments, the effects of bretylium on the enzyme activity were tested in combination with 2.5 or 5.0 microM ouabain. 4. The combined effects of the two drugs resulted in a net reduction in the total inhibitory activities of the individual drugs, which became more marked the higher the bretylium concentration. This trend seems to suggest a competitive mode of interaction of the two drugs in their inhibitory actions on Na (+)-K (+)-ATPase activity. 5. The results demonstrate therefore that bretylium is a potent inhibitor of ouabain-inhibited ATP hydrolysis by myocardial Na (+)-K (+)-ATPase. These actions may be pertinent with regard to some of its cardiac actions.
抗心律失常药物的致心律失常作用。
DOI：
10.1016/0002-9149(87)90196-2
发表时间：
1987
期刊：
The American journal of cardiology
影响因子：
--
作者：
Rosen,MR;Wit,AL
通讯作者：
Wit,AL