Bay U 3405 inhibits cerebral vasospasm induced by authentic thromboxane A2.
Platelet activation results in the formation of various vasoactive mediators such as thromboxane A2 and serotonin. We investigated the effects of Bay U 3405 [(3R)-3- (4-fluorophenyl-sulfonamido)-1,2,3,4,-tetrahydro-9-carbazolepro panoic acid] on vasocontractions of isolated bovine cerebral arteries induced by U 46.619, a stable thromboxane/prostaglandin-endoperoxide analogue, and authentic thromboxane A2 released from thrombin-stimulated human platelets. Bay U 3405 (0.001-10 mumol/l) potently inhibited the contraction induced by U 46.619 and demonstrated a reduction of the thromboxane-mediated component of platelet-induced contractile response at higher concentrations (0.1-10 mumol).
Braun
M
M
Institut für Pharmakologie, Heinrich-Heine-Universität Düsseldorf, FRG.
Schrör
K
K
D019796:15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid; D000818:Animals; D001792:Blood Platelets / Q000502:physiology; D002227:Carbazoles / Q000494:pharmacology / Q000627:therapeutic use*; D002417:Cattle; D002536:Cerebral Arteries / Q000187:drug effects; D006801:Humans; D002546:Ischemic Attack, Transient / Q000139:chemically induced / Q000517:prevention & control*; D011450:Prostaglandin Endoperoxides, Synthetic / Q000494:pharmacology; D012701:Serotonin / Q000097:blood; D013449:Sulfonamides / Q000494:pharmacology / Q000627:therapeutic use*; D013928:Thromboxane A2; D013931:Thromboxanes / Q000037:antagonists & inhibitors*; D014661:Vasoconstriction / Q000187:drug effects
D002227:Carbazoles; D011450:Prostaglandin Endoperoxides, Synthetic; D013449:Sulfonamides; D013931:Thromboxanes; D012701:Serotonin; D013928:Thromboxane A2; D019796:15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid; C063119:ramatroban