Kimura M, Kimura I, Maekawa M
Jpn J Pharmacol. 1978 Oct;28(5):681-92. doi: 10.1254/jjp.28.681.
The cumulative log dose-response curve (DRC) isometrically produced by CaCl2 on depolarized uteri of rats in Ca2+-free KCl Ringer's solution (pH 7.8) showed a plateau-shaped type, when responses were plotted as a percent of the maximal tension of 50 micrometer acetylcholine, whereas those produced by BaCl2 or SrCl2 were a simple sigmoid type with the maximal response near the height of the plateau induced by Ca2+. The plateau phase of Ca2+ was inhibited competitively by Mg2+ (0.5--50 mM) and non-competitively by Mn2+ (30 micrometer--1 mM), whereas the maximal contraction of Ca2+ was not inhibited by either ion. Dantrolene (0.1 mM) inhibited both the plateau and the maximal contraction of Ca 2+ and retained the plateau-shaped type. EGTA (2mM) potentiated the plateau to the maximal response level and changed the DRC induced by Ca2+ to the simple sigmoid type. From these results, the plateau of DRC induced by Ca2+ seems to be mainly due to actions of external Ca2+ on the calcium binding of internal surface of cell membrane, suggesting that the internal surface is the site of the bivalent cations tested.
在无钙的氯化钾林格氏液(pH 7.8)中,氯化钙对等长收缩的去极化大鼠子宫产生的累积对数剂量-反应曲线(DRC)呈平台型,此时反应以50微米乙酰胆碱最大张力的百分比表示;而氯化钡或氯化锶产生的曲线为简单的S型,最大反应接近钙离子诱导的平台高度。钙离子的平台期受到镁离子(0.5 - 50 mM)的竞争性抑制和锰离子(30微米 - 1 mM)的非竞争性抑制,而钙离子的最大收缩不受这两种离子的抑制。丹曲林(0.1 mM)抑制钙离子的平台期和最大收缩,并保持平台型。乙二醇双四乙酸(EGTA,2 mM)将平台增强至最大反应水平,并将钙离子诱导的DRC转变为简单的S型。从这些结果来看,钙离子诱导的DRC的平台期似乎主要是由于细胞外钙离子对细胞膜内表面钙结合的作用,这表明内表面是所测试二价阳离子的作用位点。