Carvedilol, a new beta-adrenoceptor antagonist and vasodilator antihypertensive drug, inhibits superoxide release from human neutrophils

Eur J Pharmacol. 1992 Apr 22;214(2-3):277-80. doi: 10.1016/0014-2999(92)90130-v.

Abstract

Carvedilol produced a dose-dependent inhibition of superoxide (O2-) release from human neutrophils (PMNs) (IC50 = 28 microM) and scavenged O2- generated during dihydroxyfumaric acid (DHF) autooxidation (IC50 = 41 microM). Other beta-blockers, such as celiprolol, labetalol and atenolol, or the antioxidant, 'lazaroid', U74500A had no effect on O2- either released from PMNs or generated during DHF autooxidation. Propranolol, at 0.3 mM, inhibited O2- release from PMNs (73%) but failed to scavenge O2- generated from DHF. The novel free radical-scavenging effect of carvedilol may contribute to the cardioprotective activity of the compound.

MeSH terms

  • Adrenergic beta-Antagonists / pharmacology
  • Adult
  • Antihypertensive Agents / pharmacology
  • Carbazoles / pharmacology*
  • Carvedilol
  • Free Radical Scavengers
  • Fumarates / metabolism
  • Humans
  • In Vitro Techniques
  • Lipid Peroxidation / drug effects
  • Neutrophils / drug effects*
  • Neutrophils / metabolism
  • Propanolamines / pharmacology*
  • Superoxides / metabolism*
  • Tetradecanoylphorbol Acetate / pharmacology
  • Vasodilator Agents / pharmacology

Substances

  • Adrenergic beta-Antagonists
  • Antihypertensive Agents
  • Carbazoles
  • Free Radical Scavengers
  • Fumarates
  • Propanolamines
  • Vasodilator Agents
  • Carvedilol
  • Superoxides
  • dihydroxyfumarate
  • Tetradecanoylphorbol Acetate