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首页> 外文期刊>General Pharmacology >Effects of three different Ca(2+) pump ATPase inhibitors on evoked contractions in rabbit aorta and activities of Ca(2+) pump ATPases in porcine aorta.
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Effects of three different Ca(2+) pump ATPase inhibitors on evoked contractions in rabbit aorta and activities of Ca(2+) pump ATPases in porcine aorta.

机译：三种不同的Ca（2+）泵ATPase抑制剂对兔主动脉诱发的收缩和猪主动脉中Ca（2+）泵ATPase活性的影响。

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摘要

Using vascular smooth muscle, we describe the actions of three pharmacological tools, cyclopiazonic acid (CPA), thapsigargin (TG) and 2,5-di-(tert-butyl)-1,4-benzohydroquinone (tBHQ), which are presumed to act as selective inhibitors of the sarco-endoplasmic reticulum Ca(2+)-ATPases (SERCAs). In porcine aortic smooth muscle microsomes two Ca(2+)-ATPase activities have been described, one vanadate-sensitive and one vanadate-resistant, representing the Ca(2+)-ATPase activities of the plasma membrane and SERCAs, respectively. In agreement, CPA, TG and tBHQ, in the concentration range 0.1 microM to 0.1 mM, dose-dependently inhibit the Ca(2+)-ATPase activity only in the vanadate-resistant microsomes. However, 0.1 mM tBHQ also significantly inhibited the Ca(2+)-ATPase activity of vanadate-sensitive microsomes. In rabbit aortic rings, all three SERCA inhibitors produced a dose-dependant inhibition of contractions evoked by 20 mM caffeine or 1 microM phenylephrine (PE) in a Ca(2+)-free physiological solution. However, in PE-contracted rings, tBHQ (> or =30 microM) also significantly inhibited the ability of cromakalim to induce relaxation. In conclusion, the data suggest that CPA, TG and tBHQ can all act as selective SERCA inhibitors in both porcine and rabbit aortic smooth muscle. However, in contrast to CPA and TG, high concentrations of tBHQ can exhibit some nonspecific effects, which include inhibition of the plasma membrane Ca(2+)-ATPase and possibly K(+) channels regulated by cromakalim.
机译：我们使用血管平滑肌描述了三种药理学工具，即环吡嗪酸（CPA），毒胡萝卜素（TG）和2,5-二-（叔丁基）-1,4-苯并氢醌（tBHQ）的作用充当肌膜内质网Ca（2 +）-ATPases（SERCAs）的选择性抑制剂。在猪主动脉平滑肌微粒体中，已经描述了两种Ca（2 +）-ATPase活性，一种对钒酸盐敏感，对钒酸盐具有抗性，分别代表质膜和SERCA的Ca（2 +）-ATPase活性。在一致的情况下，CPA，TG和tBHQ在0.1 microM到0.1 mM的浓度范围内，仅在抗钒酸盐的微粒体中剂量依赖性地抑制Ca（2 +）-ATPase活性。但是，0.1 mM tBHQ也显着抑制了钒酸盐敏感微粒体的Ca（2 +）-ATPase活性。在兔主动脉环中，所有三种SERCA抑制剂均在无Ca（2+）的生理溶液中产生20 mM咖啡因或1 microM苯肾上腺素（PE）引起的收缩的剂量依赖性抑制。但是，在PE收缩的环中，tBHQ（>或= 30 microM）也显着抑制了克罗马卡林诱导松弛的能力。总之，数据表明CPA，TG和tBHQ均可在猪和兔主动脉平滑肌中充当选择性SERCA抑制剂。但是，与CPA和TG相比，高浓度的tBHQ可能表现出一些非特异性作用，包括抑制质膜Ca（2 +）-ATPase以及可能受克罗马卡林调节的K（​​+）通道。

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