: A selective inhibitor of thromboxane synthetase |
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| Authors: | Salvador Moncada Stuart Bunting Kevin Mullane Peter Thorogood John R Vane Amiram Raz Philip Needleman |
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| Institution: | Wellcome Research Laboratories Langley Court, Beckenham Kent BR3 3BS England;Department of Pharmacology Washington University Medical School St. Louis, Missouri 63110, U.S.A. |
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| Abstract: | Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes (IC50: 22 μg/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-PHG2. Several imidazole analogues and other substances were tested but only 1-methyl-imidadole was more potent that imidazole iteself. The use of imidazole of inhibit thromboxane formation could help to elucidate the role of thromboxanes in physiology or pathophysiology. |
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