CVT-2759 is a potent inhibitor of A 1 -ADOR , with the IC 50 values of 0.18 μM and 9.5 μM to reduce the binding of [3H]CPX in the absence and presence of 1 mM GTP. CVT-2759 plays an important role in slowing AV nodal conduction and thereby ventricular rate without causing AV block, bradycardia, atrial arrhythmias, or vasodilation.