Stimulation of prostacyclin release from vessel wall by Bay g 6575, an antithrombotic compound.
Ingestion of 1.2 g Bay g 6575 daily for 1 week by six healthy volunteers had no effect on blood-coagulation, fibrinolysis, or platelet aggregation in vitro, but it seemed to inhibit platelet aggregation in vivo (shown by a smaller reduction in the platelet aggregate ratio after venous occlusion). Plasma drawn from five volunteers after ingestion of a single dose of 1.2 g of the drug stimulated prostacyclin release from slices of rat aorta which had been washed until they stopped releasing anti-aggregating substances, whereas plasma from the same individuals before ingestion of the substance did not. Administration of either Bay g 6575 or dipyridamole alone had no effect on platelet aggregation in vitro, but combined administration resulted in a striking and prolonged inhibition of A.D.P.-induced platelet aggregation. It is proposed that the previously described antithrombotic properties of Bay g 6575 in animals are due to stimulation of prostacyclin release from the vessel wall, and that this effect is also demonstrable in man.
D000244:Adenosine Diphosphate / Q000037:antagonists & inhibitors; D000284:Administration, Oral; D000818:Animals; D001011:Aorta / Q000378:metabolism*; D001777:Blood Coagulation / Q000187:drug effects*; D002986:Clinical Trials as Topic; D003470:Culture Media; D004176:Dipyridamole / Q000494:pharmacology; D004311:Double-Blind Method; D004357:Drug Synergism; D011464:Epoprostenol / Q000378:metabolism*; D005342:Fibrinolysis / Q000187:drug effects; D005343:Fibrinolytic Agents / Q000008:administration & dosage / Q000097:blood / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects*; D011453:Prostaglandins / Q000378:metabolism*; D011720:Pyrazoles / Q000008:administration & dosage / Q000097:blood / Q000494:pharmacology*; D051381:Rats; D013268:Stimulation, Chemical
D003470:Culture Media; D005343:Fibrinolytic Agents; D011453:Prostaglandins; D011720:Pyrazoles; D000244:Adenosine Diphosphate; D004176:Dipyridamole; D011464:Epoprostenol