Cilostazol #33528

Cilostazol is a potent inhibitor (IC₅₀ = 0.57 μM) of phosphodiesterase 3 (PDE3) and also inhibits the uptake of adenosine into muscle, endothelial cells, erythrocytes, and platelets (1). PDE3 hydrolyses both cAMP and cGMP, and plays a role in regulating cAMP-mediated signaling in a number of cell and tissue types, but is particularly important in regulating heart muscle, vascular smooth muscle, and platelet aggregation (2). Clinical studies demonstrate that Cilostazol is effective against inflammation, insulin resistance, and cardiomyopathy. Cilostazol, in conjunction with anti-platelet medication, reduced risk of restenosis, amputation, and target lesion revascularization following peripheral vascular interventions (3). Treatment of a murine model of obesity-associated left ventricular diastolic dysfunction with Cilostazol and hypertension medication resulted in improved left ventricular function and reduced TGF-β1/SMAD3 and Akt/mTOR signaling (4). Cilostazol is seen as more effective than aspirin in preventing recurrent ischemic stroke and intracranial hemorrhage (5), and as a potential treatment of Raynaud syndrome (6).