Endothelial dysfunction: a strategic target in the treatment of hypertension?

Pflugers Arch. 2010 May;459(6):995-1004. doi: 10.1007/s00424-010-0786-4. Epub 2010 Feb 2.


Endothelial dysfunction is a common feature of hypertension, and it results from the imbalanced release of endothelium-derived relaxing factors (EDRFs; in particular, nitric oxide) and endothelium-derived contracting factors (EDCFs; angiotensin II, endothelins, uridine adenosine tetraphosphate, and cyclooxygenase-derived EDCFs). Thus, drugs that increase EDRFs (using direct nitric oxide releasing compounds, tetrahydrobiopterin, or L-arginine supplementation) or decrease EDCF release or actions (using cyclooxygenase inhibitor or thromboxane A2/prostanoid receptor antagonists) would prevent the dysfunction. Many conventional antihypertensive drugs, including angiotensin-converting enzyme inhibitors, calcium channel blockers, and third-generation beta-blockers, possess the ability to reverse endothelial dysfunction. Their use is attractive, as they can address arterial blood pressure and vascular tone simultaneously. The severity of endothelial dysfunction correlates with the development of coronary artery disease and predicts future cardiovascular events. Thus, endothelial dysfunction needs to be considered as a strategic target in the treatment of hypertension.

Publication types

  • Review

MeSH terms

  • Angiotensin II / physiology
  • Animals
  • Antihypertensive Agents / therapeutic use*
  • Calcium / administration & dosage
  • Calcium / adverse effects
  • Dinucleoside Phosphates / pharmacology
  • Endothelin-1 / physiology
  • Endothelium, Vascular / physiopathology*
  • Endothelium-Dependent Relaxing Factors
  • Humans
  • Hypertension / drug therapy*
  • Hypertension / physiopathology*
  • Prostaglandin-Endoperoxide Synthases / metabolism
  • Reactive Oxygen Species / metabolism
  • Receptor, Endothelin A / physiology
  • Receptor, Endothelin B / physiology
  • Receptors, Thromboxane / physiology
  • Vasoconstrictor Agents / therapeutic use


  • Antihypertensive Agents
  • Dinucleoside Phosphates
  • Endothelin-1
  • Endothelium-Dependent Relaxing Factors
  • Reactive Oxygen Species
  • Receptor, Endothelin A
  • Receptor, Endothelin B
  • Receptors, Thromboxane
  • Vasoconstrictor Agents
  • uridine adenosine tetraphosphate
  • Angiotensin II
  • Prostaglandin-Endoperoxide Synthases
  • Calcium