K(ATP) channel therapeutics at the bedside

J Mol Cell Cardiol. 2005 Jul;39(1):99-112. doi: 10.1016/j.yjmcc.2005.04.006.


The family of potassium channel openers regroups drugs that share the property of activating adenosine triphosphate-sensitive potassium (K(ATP)) channels, metabolic sensors responsible for adjusting membrane potential-dependent functions to match cellular energetic demands. K(ATP) channels, widely represented in metabolically-active tissue, are heteromultimers composed of an inwardly rectifying potassium channel pore and a regulatory sulfonylurea receptor subunit, the site of action of potassium channel opening drugs that promote channel activity by antagonizing ATP-induced pore inhibition. The activity of K(ATP) channels is critical in the cardiovascular adaptive response to stress, maintenance of neuronal electrical stability, and hormonal homeostasis. Thereby, K(ATP) channel openers have a unique therapeutic spectrum, ranging from applications in myopreservation and vasodilatation in patients with heart or vascular disease to potential clinical use as bronchodilators, bladder relaxants, islet cell protector, antiepileptics and promoters of hair growth. While the current experience in practice with potassium channel openers remains limited, multitude of ongoing investigations aims at defining the benefit of this emerging family of therapeutics in diverse disease conditions associated with metabolic distress.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • ATP-Binding Cassette Transporters / drug effects
  • ATP-Binding Cassette Transporters / metabolism
  • Adenosine Triphosphate / metabolism
  • Anti-Arrhythmia Agents / pharmacology*
  • Arrhythmias, Cardiac / drug therapy
  • Endocrine System Diseases / drug therapy
  • Humans
  • Hypertension / drug therapy*
  • Lung Diseases / drug therapy
  • Myocardial Ischemia / drug therapy*
  • Peripheral Vascular Diseases / drug therapy*
  • Potassium Channels / drug effects*
  • Potassium Channels / metabolism
  • Potassium Channels, Inwardly Rectifying / drug effects
  • Potassium Channels, Inwardly Rectifying / metabolism
  • Receptors, Drug / drug effects
  • Receptors, Drug / metabolism
  • Skin Diseases / drug therapy
  • Sulfonylurea Receptors
  • Urologic Diseases / drug therapy


  • ATP-Binding Cassette Transporters
  • Anti-Arrhythmia Agents
  • Potassium Channels
  • Potassium Channels, Inwardly Rectifying
  • Receptors, Drug
  • Sulfonylurea Receptors
  • Adenosine Triphosphate