A new stable prostacyclin analogue OP41483 (15-cyclopentyl-.OMEGA.-pentanor-5(E)-carbacyclin).

Abstract

Effects of a new stable prostacyclin analogue OP41483 (15-cyclopentyl-omega-pentanor-5(E)-carbacyclin) on platelet aggregation, plasma thromboxane B2 levels, hemodynamic parameters, and clinical safety were studied. Normal volunteers received intravenous infusions of OP41483 at doses of 2.5 (n = 3), 5.0 (n = 3), 10 (n = 3), and 20 (n = 5) ng/kg/min for one hour. During infusion, ADP (adenosine diphosphate)-induced platelet aggregation decreased significantly, and blood pressure decreased slightly, but plasma thromboxane B2 levels did not change significantly. The intravenous infusion of OP41483 at the dose of 10 ng/kg/min for one hour over three successive days was performed. During the each infusion, platelet aggregation and mean blood pressure decreased significantly.