doi: 10.1016/0090-6980(77)90232-5.
Imidazole: a selective inhibitor of thromboxane synthetase
- PMID: 558637
- DOI: 10.1016/0090-6980(77)90232-5
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Imidazole: a selective inhibitor of thromboxane synthetase
Prostaglandins.
1977 Apr.
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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