Lack of antiplatelet activity of the new coumarin derivative 8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxy- carboxylmethoxycoumarin under in vivo conditions in man.
Antiplatelet properties of AD 6 (8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxy-carboxyl- methoxycoumarin) have been studied in vitro and in vivo. The drug showed a marked inhibitory effect on platelet aggregation, beta-thromboglobulin (beta TG) release and thromboxane B2 (TxB2) production in vitro. However, such effects were seen only in the presence of high concentrations of the drug (10(-3) and 10(-4) mol/l) and completely disappeared at lower concentrations. No effect was seen in vivo following oral administration of 300 mg of the drug in a small group of volunteers. It can be concluded that in vitro properties of the drug cannot be surmised without due caution to indicate its potential clinical use.
D000244:Adenosine Diphosphate / Q000494:pharmacology; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000494:pharmacology; D001792:Blood Platelets / Q000187:drug effects*; D002866:Chromonar / Q000031:analogs & derivatives / Q000494:pharmacology*; D003094:Collagen / Q000494:pharmacology; D003374:Coumarins / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D010974:Platelet Aggregation / Q000187:drug effects; D001620:beta-Thromboglobulin / Q000378:metabolism
D001095:Arachidonic Acids; D003374:Coumarins; D001620:beta-Thromboglobulin; D016718:Arachidonic Acid; D000244:Adenosine Diphosphate; D003094:Collagen; C025945:cloricromen; D002866:Chromonar