LCB-2853

LCB-2853 is an antagonist of thromboxane A2 (TXA2) receptor, with antiplatelet and antithrombotic activities.

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].

[1]. Depin JC, et al. Pharmacodynamics and antithrombotic effects after intravenous administration of the new thromboxane A2 receptor antagonist sodium 4-[[1-[[[(4-chlorophenyl)sulfonyl]amino]methyl]cyclopentyl] methyl]benzeneacetate. Arzneimittelforschung. 1994 Nov;44(11):1203-7. [2]. Lardy C, et al. Antiaggregant and antivasospastic properties of the new thromboxane A2 receptor antagonist sodium 4-[[1-[[[(4-chlorophenyl)sulfonyl]amino]methyl]cyclopentyl] methyl]benzeneacetate. Arzneimittelforschung. 1994 Nov;44(11):1196-202.