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9,11-Epoxyiminoprosta-5,13-dienoic acid is a thromboxane A2 antagonist in human platelets

Abstract

THROMBOXANE A2 (TXA2), an important arachidonic acid metabolite, aggregates platelets1–6, constricts coronary smooth muscle1,7,8, and is formed during mechanical or anaphylactic organ challenge9–11. There are selective thromboxane A2 synthetase inhibitors12–16 but there are no known, selective TXA2-receptor antagonists. We report here that 9,11-epoxy-imino-prosta-5,13-dienoic acid17 (9,11-EIP) antagonises TXA2-mediated platelet aggregation without inhibiting thromboxane synthetase or fatty acid cyclo-oxygenase. This finding should allow further exploration of the nature of TXA2 receptors in human platelets.

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FITZPATRICK, F., BUNDY, G., GORMAN, R. et al. 9,11-Epoxyiminoprosta-5,13-dienoic acid is a thromboxane A2 antagonist in human platelets. Nature 275, 764–766 (1978). https://doi.org/10.1038/275764a0

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