Atopaxar (30-100 mg/kg; p.o.) causes a dose-dependent prolongation of the time to occlusion of the femoral artery in photochemically-induced thrombosis (PIT) guinea pigs model. Atopaxar does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg. Animal Model: Guinea pigs, PIT model Dosage: Oral administration Administration: 10 mg/kg, 30 mg/kg, 100 mg/kg Result: Prolonged the time to occlusion by 1.8-fold and 2.4-fold at 30 mg/kg and 100 mg/kg, respectively, compared with controls.
体外研究
Atopaxar inhibits haTRAP (high-affinity thrombin receptor activating peptide) binding to PAR-1 on human platelet membranes in a concentration-dependent manner, with an IC 50 of 0.019 μM. Atopaxar inhibits human platelet aggregation induced by thrombin or TRAP in a concentration-dependent manner. Atopaxar does not inhibit PRP (platelet-rich plasma) aggregation induced by ADP, U46619, collagen, and PAR-4ap, up to a concentration of 20 μM.
编辑结构
