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Sulmazole is a cardiotonic agent.1,2 It increases cAMP accumulation via antagonism of the adenosine A1 receptor (IC50 = 78.1 µM), inhibition of phosphodiesterase (PDE), and reduction of Gi-mediated inhibition of adenylate cyclase in rat adipocyte membranes.1 Sulmazole also selectively inhibits PDE5 over PDE3 (IC50s = 21 and 150 µM, respectively) in a cell-free assay.2 It restores cardiac output, the force of right ventricular contraction, and heart rate, and decreases right atrial pressure in a dog heart-lung preparation model of pentobarbital-induced depressed cardiac function.3
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1. The new cardiotonic agent sulmazole is an A1 adenosine receptor antagonist and functionally blocks the inhibitory regulator, Gi. Mol. Pharmacol. 33(4), 441-448 (1988).
2. Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: Analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase. J. Med. Chem. 36(10), 1387-1392 (1993).
3. Improvement of cardiac performance by AR-