Heart rate reduction via selective 'funny' channel blockers

Curr Opin Pharmacol. 2007 Apr;7(2):208-13. doi: 10.1016/j.coph.2006.09.005. Epub 2007 Jan 30.

Abstract

The 'funny' current, first described in cardiac pacemaker cells almost 30 years ago, is a key player in the generation of pacemaker activity and the autonomic modulation of heart rate. Because of these specific functions, a search for molecules able to interfere selectively with the 'funny' current was undertaken soon after its discovery, with the aim of developing tools for the pharmacological control of heart rate. This search has succeeded in generating a new class of drugs, the heart rate-reducing agents, which act through specific blockade of f-channels; one of these drugs, ivabradine, is presently marketed against stable angina. Because of their many functions in heart and other tissues, pharmacological utilization of "funny" channel properties is an exciting new frontier open to further developments.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Angina Pectoris / drug therapy
  • Animals
  • Anti-Arrhythmia Agents / adverse effects
  • Anti-Arrhythmia Agents / pharmacology*
  • Benzazepines / adverse effects
  • Benzazepines / pharmacology
  • Coronary Artery Disease / drug therapy
  • Drug Delivery Systems
  • Heart Rate / drug effects*
  • Humans
  • Ion Channel Gating / drug effects*
  • Ion Channels / antagonists & inhibitors*
  • Ivabradine
  • Sinoatrial Node / drug effects

Substances

  • Anti-Arrhythmia Agents
  • Benzazepines
  • Ion Channels
  • Ivabradine