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克罗卡林对蛙离体心肌细胞钾膜电导的作用。

Action of cromakalim on potassium membrane conductance in isolated heart myocytes of frog.

作者信息

Pilsudski R, Rougier O, Tourneur Y

机构信息

Laboratoire de Physiologie des Eléments Excitables, CNRS UA244, Université Claude Bernard, Villeurbanne, France.

出版信息

Br J Pharmacol. 1990 Jul;100(3):581-7. doi: 10.1111/j.1476-5381.1990.tb15850.x.

Abstract
  1. The effects of cromakalim on membrane currents were studied at 20 degrees C in frog atrial and ventricular cells in patch clamp recording using the whole cell configuration. 2. When cromakalim (1 microM) was applied in the external medium, a time-independent current was activated in a few minutes. Cromakalim induced a weak increase of inward membrane currents recorded during hyperpolarization and a large increase of outward membrane currents recorded during depolarization. 3. The current voltage relationship of the cromakalim-induced current reversed near EK and rectified in the outward direction. 4. The cromakalim-activated current was inhibited by external application of cesium (20 mM), barium (1.8 mM), tolbutamide (1 mM) and glibenclamide (1 microM). 5. The effects of cromakalim were insensitive to a cytosolic increase in adenosine 5'-triphosphate (ATP, 3-5 mM). Cromakalim had no effects when applied in the cell. 6. Our results confirm that cromakalim activates an IK(ATP)-like conductance and suggest that the effects of the drug are due to an action on the external side of the membrane and are independent of the ATP cell content.
摘要
  1. 在20摄氏度下,采用全细胞模式,运用膜片钳记录技术,研究了克罗卡林对蛙心房和心室细胞的膜电流的影响。2. 当在外部介质中加入克罗卡林(1微摩尔)时,几分钟内就会激活一种与时间无关的电流。克罗卡林使超极化期间记录到的内向膜电流略有增加,而使去极化期间记录到的外向膜电流大幅增加。3. 克罗卡林诱导的电流的电流电压关系在接近EK处反转,并在向外方向上整流。4. 外部施加铯(20毫摩尔)、钡(1.8毫摩尔)、甲苯磺丁脲(1毫摩尔)和格列本脲(1微摩尔)可抑制克罗卡林激活的电流。5. 克罗卡林的作用对细胞内三磷酸腺苷(ATP,3 - 5毫摩尔)的增加不敏感。在细胞内施加克罗卡林无作用。6. 我们的结果证实,克罗卡林激活了一种类似IK(ATP)的电导,并表明该药物的作用是由于其对膜外侧的作用,且与细胞内ATP含量无关。

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本文引用的文献

1
ATP-regulated K+ channels in cardiac muscle.心肌中的ATP调节钾通道。
Nature. 1983;305(5930):147-8. doi: 10.1038/305147a0.
4
Dissociation of actions of BRL 34915 in the rat portal vein.
Eur J Pharmacol. 1987 Sep 23;141(3):485-8. doi: 10.1016/0014-2999(87)90570-x.

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