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[钾通道功能的药理学调节可能性]

[Possibilities of the pharmacologic regulation of potassium channel function].

作者信息

Kasparov S A

出版信息

Farmakol Toksikol. 1989 May-Jun;52(3):88-93.

PMID:2676590
Abstract

Potassium channels of excitable membranes are a heterogeneous group of channels among which one can distinguish potential-dependent, Ca2+-dependent, receptor-dependent and others. The substances contributing to the activation of these channels decrease excitability of membranes and the substances suppressing the activity of potassium channels increase it. A number of agents (narcotic analgetics, ligands of sigma-opiate receptors, GABA -mimetics, M-cholinergic agent) might modulate the activity of potassium channels indirectly through the corresponding receptors. Also, some drugs used in medical practice exert the immediate effect on these channels. Among them there are myotropic hypotensive drugs diazoxide, pinacidyl, BRL 34915 and minoxydyl, antidiabetic agents -- the derivatives of sulfon urea (butamide). The transfer of potassium ions through membranes is probably one of the fundamental mechanisms of the action of pharmacological agents.

摘要

可兴奋膜的钾通道是一组异质性通道,其中可区分出电位依赖性、钙依赖性、受体依赖性等类型。促成这些通道激活的物质会降低膜的兴奋性,而抑制钾通道活性的物质则会增加膜的兴奋性。许多药物(麻醉性镇痛药、σ-阿片受体配体、GABA模拟物、M胆碱能药物)可能通过相应受体间接调节钾通道的活性。此外,一些医学实践中使用的药物对这些通道有直接作用。其中有血管平滑肌舒张性降压药二氮嗪、匹那地尔、BRL 34915和米诺地尔,抗糖尿病药物——磺脲类衍生物(丁磺酰胺)。钾离子通过膜的转运可能是药物作用的基本机制之一。

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