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Imidazole: a selective inhibitor of thromboxane synthetase.

Prostaglandins (1977-04-01)
S Moncada, S Bunting, K Mullane, P Thorogood, J R Vane, A Raz, P Needleman
PMID558637
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.

MATERIALS
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Sigma-Aldrich
Imidazole, ACS reagent, ≥99% (titration)