N-ethylmaleimide inhibits platelet aggregation and potentiates hydrogen peroxide formation induced by thrombin.
The effect of NEM pretreatment on hydrogen peroxide accumulation and aggregation in non stimulated and activated human platelets was studied. It was shown that low concentrations of NEM potentiate hydrogen peroxide formation induced specifically by thrombin. The cooperative effect of NEM with thrombin is dose-dependent and reaches the maximum at 5 microM NEM. Thrombin is particularly effective at low concentrations (0.02-0.1 U). Extracellular Ca2+ significantly increases the NEM effect. Moreover NEM inhibits aggregation both in PRP and in washed platelets, exhibiting the greatest activity in washed platelets stimulated by thrombin.
Institute of Biological Chemistry, University of Genoa, Italy.
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Leoncini
D019796:15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid; D016718:Arachidonic Acid / Q000494:pharmacology; D001792:Blood Platelets / Q000187:drug effects*; D000001:Calcimycin / Q000494:pharmacology; D002118:Calcium / Q000378:metabolism / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D005033:Ethylmaleimide / Q000494:pharmacology*; D006801:Humans; D006861:Hydrogen Peroxide / Q000378:metabolism*; D015539:Platelet Activation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D011450:Prostaglandin Endoperoxides, Synthetic / Q000494:pharmacology; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology; D013917:Thrombin / Q000494:pharmacology*; D013928:Thromboxane A2 / Q000031:analogs & derivatives / Q000494:pharmacology; D014662:Vasoconstrictor Agents / Q000494:pharmacology
D010975:Platelet Aggregation Inhibitors; D011450:Prostaglandin Endoperoxides, Synthetic; D014662:Vasoconstrictor Agents; D016718:Arachidonic Acid; D000001:Calcimycin; D013928:Thromboxane A2; D019796:15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid; D006861:Hydrogen Peroxide; D013917:Thrombin; D013755:Tetradecanoylphorbol Acetate; D005033:Ethylmaleimide; D002118:Calcium