Potassium channels in vascular smooth muscle: a pathophysiological and pharmacological perspective

Fundam Clin Pharmacol. 2019 Oct;33(5):504-523. doi: 10.1111/fcp.12461. Epub 2019 Apr 1.

Abstract

Potassium (K+ ) ion channel activity is an important determinant of vascular tone by regulating cell membrane potential (MP). Activation of K+ channels leads to membrane hyperpolarization and subsequently vasodilatation, while inhibition of the channels causes membrane depolarization and then vasoconstriction. So far five distinct types of K+ channels have been identified in vascular smooth muscle cells (VSMCs): Ca+2 -activated K+ channels (BKC a ), voltage-dependent K+ channels (KV ), ATP-sensitive K+ channels (KATP ), inward rectifier K+ channels (Kir ), and tandem two-pore K+ channels (K2 P). The activity and expression of vascular K+ channels are changed during major vascular diseases such as hypertension, pulmonary hypertension, hypercholesterolemia, atherosclerosis, and diabetes mellitus. The defective function of K+ channels is commonly associated with impaired vascular responses and is likely to become as a result of changes in K+ channels during vascular diseases. Increased K+ channel function and expression may also help to compensate for increased abnormal vascular tone. There are many pharmacological and genotypic studies which were carried out on the subtypes of K+ channels expressed in variable amounts in different vascular beds. Modulation of K+ channel activity by molecular approaches and selective drug development may be a novel treatment modality for vascular dysfunction in the future. This review presents the basic properties, physiological functions, pathophysiological, and pharmacological roles of the five major classes of K+ channels that have been determined in VSMCs.

Keywords: hypertension; potassium channels; vascular diseases; vascular smooth muscle cells.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Development / methods
  • Humans
  • Muscle, Smooth, Vascular / metabolism*
  • Potassium / metabolism
  • Potassium Channels / metabolism*

Substances

  • Potassium Channels
  • Potassium