HA4788 Cilostazol, CAS 73963-72-1

Cilostazol Description

Cilostazol is a quinolinone derivative first developed as an anti-thrombotic agent, inhibiting ADP-dependent platelet aggregation. It regulates cell proliferation, stimulates cyclic adenosine monophosphate (cAMP) level, and induces cyclic AMP-dependent protein kinase. This is mediated by selective and specific inhibition of cyclic nucleotide phosphodiesterase  (IC50 = 200 nM). Because of its effects on platelets, cilostazol is useful in various conditions, including peripheral artery disease, stroke, and post-stent stenosis. It is metabolized to products that also affect platelet aggregation by cytochrome P450 (CYP) isoforms CYP3A4, CYP3A5, and CYP1B1.

Cilostazol is an antiplatelet drug and a vasodilator. It works by stopping blood cells called platelets from sticking together.

Cilostazol Specifications

Cilostazol Applications

• Used to treat chronic arterial disease and intermittent claudication
• Used to reduce Madin–Darby cell line (MDCK) proliferation through c-Myc down-regulation
• Used for secondary stroke prevention

Reference:

1. Suri, A., et al.: J. Clin. Pharmacol., 38, 144 (1998), Park, S.-W., et al.: Am. J. Cardiol., 84, 511 (1999), Tsuchikane, E., et al.: Circulation, 100, 21 (1999).
2. Koga, Y., Kihara, Y., Okada, M., et al. 2(1H)-Quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities. Bioorganic & Medicinal Chemistry Letters 8(12), 1471-1476 (1998).
3. Taniguchi K, Ohtani H, Ikemoto T, Miki A, Hori S, Sawada Y (October 2007). “Possible case of potentiation of the antiplatelet effect of cilostazol by grapefruit juice”. Journal of Clinical Pharmacy and Therapeutics. 32 (5): 457–9. doi:10.1111/j.1365-2710.2007.00844.x. PMID 17875111
4. Au, T.B., Golledge, J., Walker, P.J., et al. Peripheral arterial disease – diagnosis and management in general practice. Aust.Fam.Physician 42(6), 397-400 (2013).