Imidazole: a selective inhibitor of thromboxane synthetase

Prostaglandins. 1977 Apr;13(4):611-8. doi: 10.1016/0090-6980(77)90232-5.

Abstract

Imidazole inhibits the enzymic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes (IC50: 22 MICRONG/ML; DETERMINED BY BIOASSAY). The inhibitor is selective, for prostaglandin cyclo-oxygenase is only affected at high doses. Radiochemical data confirms that imidazole blocks the formation of 14C-thromboxane B2 from 14C-PGH2. Several imidazole analogues and other substances were tested but only 1-methyl-imidazole was more potent than imidazole itself. The use of imidazole to inhibit thromboxane formation could help to elucidate the role of thromboxanes in physiology or pathophysiology.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Aorta / enzymology
  • Arachidonic Acids / pharmacology
  • Blood Platelets / enzymology
  • Hydroxy Acids
  • Imidazoles / pharmacology*
  • Male
  • Microsomes / enzymology
  • Muscle, Smooth / enzymology
  • Oxidoreductases / antagonists & inhibitors*
  • Oxidoreductases / biosynthesis
  • Peroxides / metabolism
  • Prostaglandins / metabolism*
  • Pyrans
  • Rabbits
  • Seminal Vesicles / enzymology
  • Sheep

Substances

  • Arachidonic Acids
  • Hydroxy Acids
  • Imidazoles
  • Peroxides
  • Prostaglandins
  • Pyrans
  • Oxidoreductases