AD6 (8-monochloro-3-beta-diethylamino-ethyl-4-methyl-7-ethoxycarbonyl-meth oxy coumarin) inhibits the release of arachidonic acid in human platelets stimulated by thrombin.
The coumarin derivative AD6 is known to inhibit platelet aggregation and release and it possesses vasodilatory properties on coronary arteries of laboratory animals. Furthermore, the inhibition of the production of TxB2 from endogenous substrates after stimulation of human platelets with collagen has been demonstrated. The present report demonstrates that AD6 inhibits the production of labeled arachidonic acid and diglycerides from phospholipids of platelets stimulated with thrombin. This effect is dose-dependent and is already evident at a concentration of the drug (25 microM) which is unable to prevent the aggregation. Apparently, AD6 inhibits the release of arachidonic acid from phosphatidylinositol and choline phosphoglycerides which are the main sources of the substrate for the synthesis of prostaglandins and thromboxanes.
D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000037:antagonists & inhibitors / Q000378:metabolism*; D001241:Aspirin / Q000494:pharmacology; D001792:Blood Platelets / Q000187:drug effects* / Q000378:metabolism; D002866:Chromonar / Q000031:analogs & derivatives / Q000494:pharmacology*; D003374:Coumarins / Q000494:pharmacology*; D004075:Diglycerides / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D006801:Humans; D010743:Phospholipids / Q000378:metabolism; D010974:Platelet Aggregation / Q000187:drug effects*; D011868:Radioisotopes; D013917:Thrombin / Q000494:pharmacology*; D013929:Thromboxane B2 / Q000378:metabolism
D001095:Arachidonic Acids; D003374:Coumarins; D004075:Diglycerides; D010743:Phospholipids; D011868:Radioisotopes; D016718:Arachidonic Acid; D013929:Thromboxane B2; C025945:cloricromen; D013917:Thrombin; D002866:Chromonar; D001241:Aspirin