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-carbazolepropanoic 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 mu-mol/1) 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 mu-mol).