Cilostazol-d₄is intended for use as an internal standard for the quantification of cilostazol by GC- or LC-MS. Cilostazol is a phosphodiesterase 3A (PDE3A) inhibitor (IC₅₀= 0.2 µM for the platelet enzyme).¹It is selective for PDE3A over PDE1, -2, -4, and 5 (IC₅₀s = >5 µM for all). Cilostazol inhibits collagen- or ADP-induced aggregation of isolated rabbit platelets (IC₅₀s = 29 and 31 µM, respectively).²In vivo, cilostazol (30 mg/kg) reduces thrombus formation by 84% in a mouse model of pulmonary thromboembolism. It reduces cardiac fibrosis and prevents the development of diastolic dysfunction and cardiac hypertrophy induced by a high-fat diet and angiotensin II in mice.³Formulations containing cilostazol have been used in the treatment of the symptoms of intermittent claudication in peripheral vascular disease.

1.SchrÖr, K.The pharmacology of cilostazolDiabetes Obes. Metab.4 (Suppl 2)S14-S19(2002) 2.Koga, Y., Kihara, Y., Okada, M., et al.2(1H)-Quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activitiesBioorg. Med. Chem. Lett.8(12)1471-1476(1998) 3.Reddy, S.S., Agarwal, H., and Barthwal, M.K.Cilostazol ameliorates heart failure with preserved ejection fraction and diastolic dysfunction in obese and non-obese hypertensive miceJ. Mol. Cell. Cardiol.12346-57(2018)