Imidazole: a selective inhibitor of thromboxane synthetase.
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.
D000818:Animals; D001011:Aorta / Q000201:enzymology; D001095:Arachidonic Acids / Q000494:pharmacology; D001792:Blood Platelets / Q000201:enzymology; D006880:Hydroxy Acids; D007093:Imidazoles / Q000494:pharmacology*; D008297:Male; D008861:Microsomes / Q000201:enzymology; D009130:Muscle, Smooth / Q000201:enzymology; D010088:Oxidoreductases / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D010545:Peroxides / Q000378:metabolism; D011453:Prostaglandins / Q000378:metabolism*; D011714:Pyrans; D011817:Rabbits; D012669:Seminal Vesicles / Q000201:enzymology; D012756:Sheep
D001095:Arachidonic Acids; D006880:Hydroxy Acids; D007093:Imidazoles; D010545:Peroxides; D011453:Prostaglandins; D011714:Pyrans; D010088:Oxidoreductases