The endothelin system and its potential as a therapeutic target in cardiovascular disease

Pharmacol Ther. 1996;72(2):109-48. doi: 10.1016/s0163-7258(96)00101-5.


Endothelin (ET)-1, an endothelium-derived peptide, is the most potent vasoconstrictor agent described to date. ET-1 also has positive inotropic and chronotropic effects in the heart and is a co-mitogen in both cardiac and vascular myocytes. The major elements of the system involved in formation of ET-1 and its isopeptides, as well as the receptors mediating their effects, have been cloned and characterised. Antagonists of the ET receptors are now available, and selective inhibitors of the ET-converting enzymes are being developed. Early studies using receptor antagonists support the involvement of ET-1 in the pathophysiology of several cardiovascular diseases. The relative merits of ET-converting enzyme inhibitors and receptor antagonists for the treatment of cardiovascular disease are discussed.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Cardiovascular Diseases / drug therapy
  • Cardiovascular Diseases / metabolism
  • Cardiovascular Diseases / physiopathology*
  • Cardiovascular Physiological Phenomena
  • Endothelin-1 / biosynthesis
  • Endothelin-1 / genetics
  • Endothelin-1 / physiology*
  • Humans
  • Molecular Sequence Data
  • Receptors, Endothelin / drug effects
  • Receptors, Endothelin / genetics
  • Receptors, Endothelin / metabolism


  • Endothelin-1
  • Receptors, Endothelin