| In Vivo |
AM-8123 (100 mg/kg; p.o.) results in sustained improvement in systolic function and decreases both EDV and ESV as measured by echocardiography but not by the invasive pressure-volume conductance catheter at study termination[1]. AM-8123 (0.035, 0.09, 0.9, and 9 mg/kg; i.v.) improves cardiovascular function[1]. AM-8123 exhibits appreciably greater oral bioavailability in rats and dogs relative to pyr-apelin-13. AM-8123 infusion results in an increase in EF, SV, and dP/dt max at submicromolar unbound plasma concentrations with minimal change in HR, indicating that acute infusion of AM-8123 is associated with an improvement in several markers of cardiac function. AM-8123 is a more potent mediator of both ERK and AKT phosphorylation relative to pyr-apelin-13[1]. Animal Model: Lewis rats (2~3 months old)[1] Dosage: 100 mg/kg Administration: P.o. Result: Resulted in sustained improvement in systolic function. Decreased both EDV and ESV as measured by echocardiography but not by the invasive pressure-volume conductance catheter at study termination. Animal Model: Rats[1] Dosage: 0.035, 0.09, 0.9, and 9 mg/kg Administration: I.v. Result: Improved cardiovascular function.
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