Effect of BAY U 3405, a new thromboxane antagonist, on arachidonic acid induced thromboembolism.
The model of AA-induced sudden death employed in these investigations seems to be appropriate for studying the efficacy of TXA2-antagonists. The actions of TXA2 on platelets, respiratory and vascular tissue are considered as key events resulting in the death of the animals. The results obtained in this study, using BAY U 3405 as a selective TXA2 receptor antagonist, clearly show that TXA2 mediated processes are effectively abolished by this type of drug. Since TXA2 is implicated in the pathophysiology of many diseases, potent TXA2 antagonists appear to be useful for treatment of these disorders. BAY U 3405 seems to fulfil these requirements. The threshold dose is 1 to 3 mg/kg p.o. In addition, there is a rapid onset and long duration of action at 10 mg/kg p.o. under the experimental conditions used.
Seuter
F
F
Institute of Pharmacology, BAYER AG, Wuppertal, FRG.
Perzborn
E
E
Fiedler
V B
VB
D000818:Animals; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000037:antagonists & inhibitors* / Q000633:toxicity; D016084:Bronchoconstriction / Q000187:drug effects; D002227:Carbazoles / Q000494:pharmacology*; D003645:Death, Sudden; D004305:Dose-Response Relationship, Drug; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects*; D011817:Rabbits; D013449:Sulfonamides / Q000494:pharmacology*; D015996:Survival Rate; D013923:Thromboembolism / Q000139:chemically induced / Q000517:prevention & control*; D013928:Thromboxane A2 / Q000502:physiology; D013931:Thromboxanes / Q000037:antagonists & inhibitors*
D001095:Arachidonic Acids; D002227:Carbazoles; D013449:Sulfonamides; D013931:Thromboxanes; D016718:Arachidonic Acid; D013928:Thromboxane A2; C063119:ramatroban