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克罗卡林对犬动脉平滑肌张力和⁸⁶Rb外流的多种作用。

The diverse effects of cromakalim on tension and 86Rb efflux in canine arterial smooth muscle.

作者信息

Masuzawa K, Matsuda T, Asano M

机构信息

Department of Pharmacology, Nagoya City University Medical School, Japan.

出版信息

Br J Pharmacol. 1991 May;103(1):1033-40. doi: 10.1111/j.1476-5381.1991.tb12296.x.

Abstract
  1. To characterize further the K+ channels opened by cromakalim in arterial smooth muscle, the effects of cromakalim on tension and 86Rb efflux were compared in endothelium-denuded strips of coronary, mesenteric and middle cerebral (MC) arteries of the dog. 2. Cromakalim relaxed strips precontracted with 20.9 mM K+. The maximum relaxation induced by cromakalim varied in the arteries used; 94% in the coronary artery, 60% in the mesenteric artery and only 38% in the MC artery. Cromakalim failed to relax arterial strips precontracted with 65.9 mM K+. 3. When the effects of cromakalim on 86Rb efflux were determined in 20.9 mM K(+)-contracted strips, cromakalim-induced relaxations were accompanied by a large increase in 86Rb efflux in the coronary artery, by a small increase in the mesenteric artery but by an apparent decrease in the MC artery. 4. When 10(-7) M nifedipine was added to 20.9 mM K(+)-contracted strips, to inactivate Ca2(+)-activated K+ (KCa) channels, cromakalim produced a greater increase (measured from the point at which cromakalim was administered) in 86Rb efflux than in the absence of nifedipine, suggesting that the effects of cromakalim on 86Rb efflux from the 20.9 mM K(+)-contracted strips may be the resultant of two opposing effects: an increased 86Rb efflux perhaps due to the opening of ATP-sensitive K+ (KATP) channels, and a decreased efflux due to the closing of KCa channels. 5. After the inactivation of Kca channels in 20.9mM K+-contracted strips, the cromakalim-induced increase in 86Rb efflux measured as area under the curve was eight times greater in the coronary artery than in the MC artery. The increase in 86Rb efflux in the mesenteric artery was intermediate between these extremes. 6. Cromakalim also increased the 86Rb efflux from 65.9 mm K+-contracted strips. This increase was not augmented by the addition of nifedipine. Under these conditions, a similar variation in efflux response (as area under the curve) for cromakalim was noted in the arteries used. 7. The relaxant responses of each artery to cromakalim were competitively antagonized by glibenclamide, a blocker of KATP channels. The cromakalim-induced increase in 86Rb efflux was also inhibited by glibenclamide. 8. These results suggest that cromakalim-opened K+ channels in the three arteries may differ in terms of their frequency of occurrence in the plasmalemma, their permeability to 86Rb and their ability to modulate tension development. On the other hand, the activities of Kca and voltage-sensitive K+ channels, estimated from the effects of nifedipine, were similar in the three arteries.
摘要
  1. 为了进一步表征在动脉平滑肌中由克罗卡林开放的钾通道,在犬的冠状动脉、肠系膜动脉和大脑中动脉(MC)的去内皮条带上比较了克罗卡林对张力和⁸⁶Rb外流的影响。2. 克罗卡林使预先用20.9 mM钾收缩的条带松弛。克罗卡林诱导的最大松弛在所用动脉中有所不同;在冠状动脉中为94%,在肠系膜动脉中为60%,而在MC动脉中仅为38%。克罗卡林未能使预先用65.9 mM钾收缩的动脉条带松弛。3. 当在20.9 mM钾收缩的条带上测定克罗卡林对⁸⁶Rb外流的影响时,克罗卡林诱导的松弛伴随着冠状动脉中⁸⁶Rb外流的大幅增加,肠系膜动脉中有小幅增加,但MC动脉中则明显减少。4. 当将10⁻⁷ M硝苯地平添加到20.9 mM钾收缩的条带上以灭活钙激活钾(KCa)通道时,与不存在硝苯地平相比,克罗卡林使⁸⁶Rb外流产生更大的增加(从给予克罗卡林的时间点开始测量),这表明克罗卡林对20.9 mM钾收缩条带中⁸⁶Rb外流的影响可能是两种相反作用的结果:可能由于ATP敏感性钾(KATP)通道开放导致⁸⁶Rb外流增加,以及由于KCa通道关闭导致外流减少。5. 在20.9 mM钾收缩条带中KCa通道失活后,以曲线下面积测量的克罗卡林诱导的⁸⁶Rb外流增加在冠状动脉中比在MC动脉中高八倍。肠系膜动脉中⁸⁶Rb外流的增加介于这两个极端之间。6. 克罗卡林还增加了65.9 mM钾收缩条带中的⁸⁶Rb外流。添加硝苯地平并未增强这种增加。在这些条件下,在所使用的动脉中观察到克罗卡林外流反应(作为曲线下面积)有类似变化。7. 每条动脉对克罗卡林的松弛反应都被格列本脲(一种KATP通道阻滞剂)竞争性拮抗。格列本脲也抑制了克罗卡林诱导的⁸⁶Rb外流增加。8. 这些结果表明,在这三条动脉中由克罗卡林开放的钾通道在质膜中的出现频率、对⁸⁶Rb的通透性以及调节张力发展的能力方面可能有所不同。另一方面,根据硝苯地平的作用估计,KCa和电压敏感性钾通道在这三条动脉中的活性相似。

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