Biochem/physiol Actions
Atopaxar (E5555) is an orally active, potent and selective thrombin receptor (protease-activated receptor; PAR1) antagonist (IC50 = 19 nM/E5555 vs. 490 nM/TRAP against 10 nM haTRAP for PAR-1 binding on human platelet membranes) that inhibits platelet aggregation induced by thrombin or TRAP T (human platelet IC50 = 64/31 nM against 1 u/mL Thrombin/5 μM TRAP; guinea pig IC50 = 13/97 nM against 2 u/mL Thrombin/20 μM TRAP), but not ADP, U46619, collagen, PAR-4ap or PAF. Atopaxar exhibits antithrombotic efficacy in guinea pigs and rats in vivo (10, 30, 100 mg/kg p.o.).
Orally active, potent and selective thrombin receptor (protease-activated receptor; PAR1) antagonist with antithrombotic efficacy in vivo.