LCB-2853

LCB-2853 is an antagonist of thromboxane A2 (TXA2) receptor, with antiplatelet and antithrombotic activities. In Vivo: In dog coronary stenosis, LCB 2853 shows a very high efficacy with ED₅₀ of 7.2 μg/kg. In rat venous thrombosis induced by combination of venous injury and blood stasis, perfused LCB 2853 decreases the weight of thrombi in a dose related manner with ED₅₀ of 220 μg/kg/min^[1]. In vivo, both against platelet aggregation and vasoconstriction, LCB 2853 shows an ED₅₀ lower than 1 mg/kg i.v. in rat AA-induced thrombocytopenia or U 46619-induced hypertension (ED₅₀ = 0.25 and 0.16 mg/kg) as well as in AA-induced sudden death in the mouse (ED₅₀ = 0.44 mg/kg). The U 46619-induced bronchoconstriction is blocked after i.v. administration of LCB 2853 (ED₅₀ = 18.4 μg/kg)^[2].