Description
An orally bioavailable, non-nucleoside partial adenosine receptor agonist; binds selectively to human A1 and A2B (EC50s = 0.66 and 1.1 nM, respectively) over A2A and A3 receptors (EC50s = 1,413 and 240 nM, respectively) expressed in CHO cells; decreases electrical field-stimulated norepinephrine release from isolated perfused hearts from SHR but not from control rats at 0.6 µM; protects against stress-induced increases in heart rate in SHR but not control rats at 0.15 mg/kg for 5 days prior to stress induction; decreases cardiac infarct size from 28.7 to 22% in a LAD-induced ischemia mouse model at 0.1 mg/kg; increases LVEF in a microembolization-induced heart failure dog model at 7.5 mg twice daily