动脉中钙拮抗剂作用的调节。

Blood vessels Pub Date : 1990-01-01 DOI:10.1159/000158809
T Godfraind, N Morel, M Wibo
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引用次数: 16

摘要

本文综述了实验证据,表明二氢吡啶钙拮抗剂的特定结合位点参与抑制刺激依赖性钙进入动脉细胞,从而抑制收缩反应。二氢吡啶结合位点的表观亲和力与高亲和力和低亲和力状态的比例有关,这种亲和力由膜电位调节,但也可能取决于其他因素,如G蛋白。在钙拮抗剂中,可以确定一组表现出电压依赖性的药物。它们明显的药理学效力高度依赖于静息膜电位和去极化刺激的持续时间。
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Modulation of the action of calcium antagonists in arteries.

This paper is a review of the experimental evidence showing that specific binding sites for dihydropyridine Ca antagonists are involved in inhibition of stimulus-dependent Ca entry into arterial cells and thereby in inhibition of the contractile response. The apparent affinity of the dihydropyridine binding site is related to the proportion of a high- and a low-affinity state which is regulated by membrane potential but could also be dependent upon other factors such as G proteins. Among Ca antagonists, a subgroup of agents exhibiting voltage dependence may be identified. Their apparent pharmacological potency is highly dependent on resting membrane potential and on the duration of the depolarizing stimulus.

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