Edwards G, Weston A H
Department of Physiological Sciences, University of Manchester, UK.
Pharmacol Ther. 1990;48(2):237-58. doi: 10.1016/0163-7258(90)90082-d.
Potassium channel openers comprise a diverse group of chemical agents which open plasma-lemmal K-channels. They show selectivity for smooth muscle, although K-channels in cardiac and skeletal muscle, neurones and the pancreatic beta-cell are also affected at relatively high concentrations. In addition, at least one endogenous K-channel opener of vascular origin--endothelium-derived hyperpolarizing factor--exists and in man plays a role in modulating blood vessel tone. The type of K-channel involved in the actions of both exogenous and endogenous K-channel openers is still uncertain, although a prime candidate in smooth muscle seems similar to the [ATPi]-modulated K-channel in the pancreatic beta-cell. This review focuses attention on the action of these agents in vascular smooth muscle and on the possible clinical exploitation of their powerful vasorelaxant properties.
钾通道开放剂包括多种能打开质膜钾通道的化学试剂。它们对平滑肌具有选择性,不过在相对高浓度时,心肌、骨骼肌、神经元及胰腺β细胞中的钾通道也会受到影响。此外,至少有一种血管源性内源性钾通道开放剂——内皮衍生超极化因子——存在,且在人体中对调节血管张力起作用。尽管平滑肌中一个主要候选通道似乎类似于胰腺β细胞中的[ATPi]调节钾通道,但外源性和内源性钾通道开放剂作用所涉及的钾通道类型仍不确定。本综述重点关注这些试剂在血管平滑肌中的作用以及对其强大血管舒张特性可能的临床应用。