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钙拮抗剂的心脏选择性

Cardioselectivity of calcium antagonists.

作者信息

Godfraind T

机构信息

Laboratoire de Pharmacologie, Université Catholique de Louvain, Bruxelles, Belgium.

出版信息

Cardiovasc Drugs Ther. 1994 May;8 Suppl 2:353-64. doi: 10.1007/BF00877320.

Abstract

Calcium antagonists comprise a diverse group of chemically unrelated agents that interact with voltage-operated calcium channels (L-type) and thereby inhibit smooth muscle and cardiac contractility. Although they interact with the alpha 1 subunit of voltage-operated calcium channels, all calcium antagonists are not identical pharmacological agents. They are not only different from a chemical point of view, but also because some of them exhibit tissue selectivity, being more powerful blockers of the contraction of arteries than of cardiac muscle. The current view that their major therapeutic action is related to vasodilation is an oversimplification, as their action is more complex and may be related to factors other than hemodynamic ones.

摘要

钙拮抗剂包括一组化学结构不相关的药物,它们与电压门控钙通道(L型)相互作用,从而抑制平滑肌和心肌的收缩力。尽管它们与电压门控钙通道的α1亚基相互作用,但所有钙拮抗剂并非药理学特性完全相同的药物。它们不仅在化学角度有所不同,而且还因为其中一些表现出组织选择性,对动脉收缩的阻断作用比对心肌的更强。目前认为它们的主要治疗作用与血管舒张有关的观点过于简单化,因为它们的作用更为复杂,可能与血流动力学因素以外的其他因素有关。

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