The regulation and pharmacology of endothelial nitric oxide synthase

Annu Rev Pharmacol Toxicol. 2006;46:235-76. doi: 10.1146/annurev.pharmtox.44.101802.121844.


Nitric oxide (NO) is a small, diffusible, lipophilic free radical gas that mediates significant and diverse signaling functions in nearly every organ system in the body. The endothelial isoform of nitric oxide synthase (eNOS) is a key source of NO found in the cardiovascular system. This review summarizes the pharmacology of NO and the cellular regulation of endothelial NOS (eNOS). The molecular intricacies of the chemistry of NO and the enzymology of NOSs are discussed, followed by a review of the biological activities of NO. This information is then used to develop a more global picture of the pharmacological control of NO synthesis by NOSs in both physiologic conditions and pathophysiologic states.

Publication types

  • Review

MeSH terms

  • Animals
  • Enzyme Inhibitors / pharmacology*
  • Gene Expression Regulation, Developmental / physiology
  • Humans
  • Isoenzymes / antagonists & inhibitors
  • Isoenzymes / metabolism
  • Nitric Oxide / metabolism
  • Nitric Oxide / physiology*
  • Nitric Oxide Synthase Type III / antagonists & inhibitors*
  • Nitric Oxide Synthase Type III / metabolism*


  • Enzyme Inhibitors
  • Isoenzymes
  • Nitric Oxide
  • Nitric Oxide Synthase Type III