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从分离的肌浆网释放钙离子的抑制剂。I. 钙离子通道阻滞剂。

Inhibitors of Ca2+ release from the isolated sarcoplasmic reticulum. I. Ca2+ channel blockers.

作者信息

Antoniu B, Kim D H, Morii M, Ikemoto N

出版信息

Biochim Biophys Acta. 1985 Jun 11;816(1):9-17. doi: 10.1016/0005-2736(85)90387-6.

DOI:10.1016/0005-2736(85)90387-6
PMID:2408667
Abstract

The effects of Ruthenium red and tetracaine, which inhibit Ca2+-induced Ca2+ release from the isolated sarcoplasmic reticulum (e.g., Ohnishi, S.T. (1979) J. Biochem. (Tokyo) 86, 1147-1150), on several types of Ca2+ release in vitro were investigated. Ca2+ release was triggered by several methods: (1) addition of quercetin or caffeine, (2) Ca2+ jump, and (3) replacement of potassium gluconate with choline chloride to produce membrane depolarization. The time-course of Ca2+ release was monitored using stopped-flow spectrophotometry and arsenazo III as a Ca2+ indicator. Ruthenium red inhibited all of these types of Ca2+ release with the same concentration for half-inhibition C1/2 = 0.08-0.10 microM. Similarly, tetracaine inhibited these types of Ca2+ release with C1/2 = 0.07-0.11 mM. Procaine also inhibits both types of Ca2+ release induced by method 2 and 3 with C1/2 = 0.67-1.00 mM. These results suggest that Ruthenium red, tetracaine and procaine interfere with a common mechanism of the different types of Ca2+ release. On the basis of several pieces of evidence we propose that Ruthenium red and tetracaine block the Ca2+ channel of sarcoplasmic reticulum.

摘要

钌红和丁卡因可抑制从分离的肌浆网中由Ca2+诱导的Ca2+释放(例如,大西,S.T.(1979年)《生物化学杂志》(东京)86卷,1147 - 1150页),本研究调查了它们对几种体外Ca2+释放类型的影响。Ca2+释放通过几种方法触发:(1)添加槲皮素或咖啡因,(2)Ca2+跃变,以及(3)用氯化胆碱替代葡萄糖酸钾以产生膜去极化。使用停流分光光度法并以偶氮胂III作为Ca2+指示剂监测Ca2+释放的时间进程。钌红以相同浓度抑制所有这些类型的Ca2+释放,半数抑制浓度C1/2 = 0.08 - 0.10微摩尔。同样,丁卡因以C1/2 = 0.07 - 0.11毫摩尔抑制这些类型的Ca2+释放。普鲁卡因也以C1/2 = 0.67 - 1.00毫摩尔抑制由方法2和3诱导的两种类型的Ca2+释放。这些结果表明钌红、丁卡因和普鲁卡因干扰不同类型Ca2+释放的共同机制。基于若干证据,我们提出钌红和丁卡因阻断肌浆网的Ca2+通道。

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