Digoxigenin monodigitoxoside is a Na+/K+-ATPase inhibitor and cardiac glycoside metabolite of digoxin . It has a binding affinity of 0.829 and an inhibitory potency of 1.07 relative to [3H]ouabain in a competitive binding assay using purified lamb Na+/K+-ATPase and for its ATPase activity, respectively. Digoxigenin monodigitoxoside is selective for the α3β1 isoform over α1β1 and α2β1 (Kds = 31.8, 65, and 35 nM, respectively). Digoxigenin monodigitoxoside produces a more potent inotropic response in perfused guinea pig hearts than digoxin with 60 and 46% increases in inotropy, respectively.

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