Cilostazol

Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC₅₀ of 0.2 μM^[1][2]. IC50 & Target: IC50: 0.2 μM ( PDE 3A)^[1] In Vitro: Cilostazol selectively inhibits cGMP-inhibited phosphodiesterase (PDE 3) and is a potent inhibitor of platelet aggregation induced by various agonists^[2].
Cilostazol inhibits stress-induced human platelet aggregation (SIPA) dose-dependently, with an IC₅₀ of 15 μM for SIPA, and with a similar IC₅₀ of 12.5 μM for ADP-induced platelet aggregation^[2].
Cilostazol directly and effectively inhibits the activation of HSC but not of Kupffer cells^[3].
In Vivo: Cilostazol (clinically used doses; p.o.; for 2 weeks) could alleviate CCl4 -induced hepatic fibrogenesis in vivo, presumably due to its direct effect to suppress HSC activation^[3].
Cilostazol (intraperitoneal injection; 10 mg/kg; 7 consecutive days after ischemia) attenuates neurological dysfunctions, brain atrophy and infarct volume, and inhibits astrocyte proliferation/glial scar formation and accelerated the angiogenesis in the ischemic boundary zone 7 and 28 days after ischemia^[4].