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二氢吡啶类钙激动剂和拮抗剂所青睐的不同钙通道门控行为模式。

Different modes of Ca channel gating behaviour favoured by dihydropyridine Ca agonists and antagonists.

作者信息

Hess P, Lansman J B, Tsien R W

出版信息

Nature. 1984;311(5986):538-44. doi: 10.1038/311538a0.

DOI:10.1038/311538a0
PMID:6207437
Abstract

Single cardiac transmembranous Ca channels have three modes of gating behaviour in the absence of drugs, expressed as current records with brief openings (mode 1), with no openings because of channel unavailability (mode 0 or null mode) and with long-lasting openings and very brief closings that appear only rarely (mode 2). The dihydropyridine Ca agonist Bay K 8644 enhances Ca channel current by promoting mode 2, while the Ca antagonists nitrendipine and nimodipine inhibit the current by favouring mode 0.

摘要

在无药物作用时,单个心脏跨膜钙通道有三种门控行为模式,表现为电流记录中出现短暂开放(模式1)、因通道不可用而无开放(模式0或零模式)以及出现仅偶尔发生的持久开放和非常短暂关闭(模式2)。二氢吡啶类钙激动剂Bay K 8644通过促进模式2来增强钙通道电流,而钙拮抗剂尼群地平和尼莫地平则通过促进模式0来抑制电流。

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Different modes of Ca channel gating behaviour favoured by dihydropyridine Ca agonists and antagonists.二氢吡啶类钙激动剂和拮抗剂所青睐的不同钙通道门控行为模式。
Nature. 1984;311(5986):538-44. doi: 10.1038/311538a0.
2
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Effects of a novel calcium channel agonist dihydropyridine analogue, Bay k 8644, on pig coronary artery: biphasic mechanical response and paradoxical potentiation of contraction by diltiazem and nimodipine.新型钙通道激动剂二氢吡啶类似物Bay k 8644对猪冠状动脉的作用:双相机械反应以及地尔硫䓬和尼莫地平对收缩的反常增强作用
J Cardiovasc Pharmacol. 1985 Mar-Apr;7(2):377-89. doi: 10.1097/00005344-198503000-00025.

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