Imidazole: a selective inhibitor of thromboxane synthetase

  • Prostaglandins. 1977 Apr;13(4):611-8. doi: 10.1016/0090-6980(77)90232-5.
S Moncada ,  S Bunting ,  K Mullane ,  P Thorogood ,  J R Vane ,  A Raz ,  P Needleman
PMID: 558637 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.

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