Oral antiplatelet agent 1 (2.5-80 mg/kg; p.o.; single dosage) decreases thrombus weight in FeCl3 thrombosis model rats[1].
Oral antiplatelet agent 1 (2.5-40 mg/kg; p.o.; single dosage) prolongs the bleeding time in tail-bleeding model rats[1].
Oral antiplatelet agent 1 exhibits great stability in both rat and human liver microsomes with the low clearance values and long half-life [human: T1/2=208.3 min, Clint=10.1 mL/(min g protein); rats: T1/2=89.1 min, Clint=10.6 mL/(min g protein)][1].
Oral antiplatelet agent 1 (5 mg/kg; p.o.; single dosage) exhibits excellent pharmacokinetic properties with relatively low clearance, high plasma exposure and good oral bioavailability in rats[1].
| Animal Model: | Male Wistar rats (250-300 g, n = 10; FeCl3 thrombosis model)[1] |
| Dosage: | 2.5, 5, 10, 20, 40 and 80 mg/kg |
| Administration: | p.o.; single dosage |
| Result: | Decreased thrombus weight in a dose-dependent manner with an ED50 of 27 mg/kg compared to that of 7 mg/kg for Clopidogrel (HY-15283). |
| Animal Model: | Male rats (250-300 g, n = 10; tail-bleeding model)[1] |
| Dosage: | 2.5, 5, 10, 20 and 40 mg/kg |
| Administration: | p.o.; single dosage |
| Result: | Prolonged the bleeding time in a dose-dependent manner. |
| Animal Model: | Male Sprague-Dawley rats (200-220g)[1] |
| Dosage: | 5 mg/kg |
| Administration: | p.o.; single dosage |
| Result: | Pharmacokinetic Parameters of Oral antiplatelet agent 1 (compound 58l) in male Sprague-Dawley rats[1].
| Cmax (ng/mL) | T1/2 (h) | Tmax (h) | AUC0-∞ (ng·h/mL) | MRT (h) | | p.o. 5 mg/kg | 1661 ± 642 | 2.91 ± 1.09 | 0.25 | 4120 ± 2127 | 3.64 ± 0.18 |
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