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一种新型抗心律失常药物劳卡胺与丙吡胺相比,对离体心肌纤维的电生理效应。

Electrophysiological effects of a new antiarrhythmic agent, lorcainide, on the isolated cardiac muscle fiber as compared with disopyramide.

作者信息

Shigenobu K, Atoda H, Asano T, Kasuya Y

出版信息

J Pharmacobiodyn. 1980 Dec;3(12):677-85. doi: 10.1248/bpb1978.3.677.

Abstract

Electrophysiological effects of a new antiarrhythmic agent, lorcainide, were studied in the isolated guinea pig ventricular myocardium and were compared with those of disopyramide; some of the experiments were also made by using the canine ventricular myocardium. Both lorcainide and disopyramide selectively depressed the maximum rate of rise of the action potential with little effect on the resting and overshooting potential. The action potential duration tended to be shortened slightly, and the prolongation of the refractory period produced by these agents was only slight. Both agents did not produce the substantial modification of the slow response produced by isoproterenol in the depolarized muscle at the concentrations enough to depress the maximum rate of rise of the action potential. Both agents also produced the marked depression of the rate of the action potential of the canine ventricular muscle, and the conduction velocity measured in the canine false tendon was markedly decreased by both agents. It was concluded that both lorcainide and disopyramide are typical Class I agents according to the classification proposed by Vaughan Williams and that lorcainide is about 10 times (at least 3 times) more potent than disopyramide in this respect.

摘要

研究了一种新型抗心律失常药物劳卡胺在豚鼠离体心室肌中的电生理效应,并与丙吡胺的效应进行了比较;部分实验还使用了犬心室肌。劳卡胺和丙吡胺均选择性地降低动作电位的最大上升速率,而对静息电位和超射电位影响很小。动作电位时程有轻微缩短的趋势,这些药物产生的不应期延长也很轻微。在足以降低动作电位最大上升速率的浓度下,这两种药物对异丙肾上腺素在去极化肌肉中产生的慢反应均未产生实质性改变。这两种药物还显著降低了犬心室肌的动作电位频率,并且在犬假腱中测量的传导速度也被这两种药物显著降低。结论是,根据沃恩·威廉姆斯提出的分类,劳卡胺和丙吡胺均为典型的Ⅰ类药物,并且在这方面劳卡胺的效力比丙吡胺强约10倍(至少3倍)。

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