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维拉帕米是一种比钙拮抗剂更好的镁激动剂吗?一种假说?

Is verapamil a better magnesium agonist rather than a calcium antagonist? A hypothesis?

作者信息

Singh R B

机构信息

Medical Hospital and Research Center, Moradabad, India.

出版信息

Med Hypotheses. 1987 Sep;24(1):1-9. doi: 10.1016/0306-9877(87)90041-7.

DOI:10.1016/0306-9877(87)90041-7
PMID:2444862
Abstract

Mg and verapamil have similar effects on the cardiovascular system. Both the agents have been successfully used for the treatment of hypertension and protection of the ischaemic myocardium. The exact mechanism of action of calcium blocking drugs including verapamil is unknown. It is proposed that verapamil stimulates the Mg-carrying transport system and Mg diffusion in the cell so that Mg influx is enhanced. This in turn causes suppression of the slow inward Ca current and fast inward Na current resulting into decreased transport of Ca and Na. Verapamil possibly also influences outward K and Mg currents and alter the shape and duration of the action potential. Since Mg ions maintain the structural and functional integrity of the cardiovascular system, therefore Mg mediated mechanisms of action for verapamil appears to be more logical.

摘要

镁和维拉帕米对心血管系统有相似作用。这两种药物均已成功用于治疗高血压和保护缺血心肌。包括维拉帕米在内的钙通道阻滞剂的确切作用机制尚不清楚。有人提出,维拉帕米可刺激细胞内携带镁的转运系统和镁的扩散,从而增强镁的内流。这进而导致慢内向钙电流和快内向钠电流受到抑制,从而减少钙和钠的转运。维拉帕米可能还会影响外向钾电流和镁电流,并改变动作电位的形状和持续时间。由于镁离子维持心血管系统的结构和功能完整性,因此镁介导的维拉帕米作用机制似乎更合理。

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Is verapamil a better magnesium agonist rather than a calcium antagonist? A hypothesis?维拉帕米是一种比钙拮抗剂更好的镁激动剂吗?一种假说?
Med Hypotheses. 1987 Sep;24(1):1-9. doi: 10.1016/0306-9877(87)90041-7.
2
Evidence of a new, preferentially Mg-carrying, transport system besides the fast Na and the slow Ca channels in the excited myocardial sarcolemma membrane.在受刺激的心肌肌膜上,除了快速钠通道和缓慢钙通道外,存在一种新的、优先携带镁的转运系统的证据。
J Mol Cell Cardiol. 1979 Oct;11(10):1109-27. doi: 10.1016/0022-2828(79)90397-3.
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Functional differentiation of the transmembrane sodium and calcium channels in mammalian cardiac fibers by use of specific inhibitors.利用特异性抑制剂对哺乳动物心脏纤维中跨膜钠通道和钙通道进行功能分化研究
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Calcium channel and prolactin release in rat clonal pituitary cells: effects of verapamil.大鼠垂体克隆细胞中的钙通道与催乳素释放:维拉帕米的作用
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Effects of verapamil on rapid Na channel-dependent action potentials of K+-depolarized ventricular fibers.维拉帕米对钾离子去极化心室纤维快速钠通道依赖性动作电位的影响。
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Inhibition of calcium-dependent action potentials in mammalian myocardium by specific inhibitors of the transmembrane calcium conductivity (verapamil, D 600).通过跨膜钙电导率的特异性抑制剂(维拉帕米、D 600)抑制哺乳动物心肌中钙依赖性动作电位。
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Calcium antagonists: definition and mode of action.钙拮抗剂:定义与作用方式。
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Calcium antagonistic drugs differ in ability to block the slow Na+ channels of young embryonic chick hearts.钙拮抗药物在阻断幼龄胚胎 chick 心脏的慢钠通道的能力上存在差异。 (注:原文中“chick”可能有误,推测可能是“chicken”,即鸡)
Eur J Pharmacol. 1983 Oct 14;94(1-2):9-18. doi: 10.1016/0014-2999(83)90436-3.

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