Evolution of β-blockers: from anti-anginal drugs to ligand-directed signalling

Trends Pharmacol Sci. 2011 Apr;32(4):227-34. doi: 10.1016/j.tips.2011.02.010. Epub 2011 Mar 21.

Abstract

Sir James Black developed β-blockers, one of the most useful groups of drugs in use today. Not only are they being used for their original purpose to treat angina and cardiac arrhythmias, but they are also effective therapeutics for hypertension, cardiac failure, glaucoma, migraine and anxiety. Recent studies suggest that they might also prove useful in diseases as diverse as osteoporosis, cancer and malaria. They have also provided some of the most useful tools for pharmacological research that have underpinned the development of concepts such as receptor subtype selectivity, agonism and inverse agonism, and ligand-directed signalling bias. This article examines how β-blockers have evolved and indicates how they might be used in the future.

Publication types

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

MeSH terms

  • Adrenergic beta-Agonists / pharmacology
  • Adrenergic beta-Antagonists / pharmacology
  • Adrenergic beta-Antagonists / therapeutic use*
  • Angina Pectoris / drug therapy
  • Angina Pectoris / physiopathology
  • Animals
  • Arrhythmias, Cardiac / drug therapy
  • Arrhythmias, Cardiac / physiopathology
  • Drug Inverse Agonism
  • Humans
  • Ligands
  • Pharmacology / methods*
  • Receptors, Adrenergic, beta / drug effects*
  • Receptors, Adrenergic, beta / metabolism
  • Signal Transduction

Substances

  • Adrenergic beta-Agonists
  • Adrenergic beta-Antagonists
  • Ligands
  • Receptors, Adrenergic, beta