Vesnarinone (OPC-8212)

A PDE3 inhibitor and ERG1 channel blocker

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库存: 现货

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5mg

￥2175.00

1740.00

- +
10mg

￥3262.00

2610.00

- +
50mg

￥9712.00

7770.00

- +
100mg

￥14962.00

11970.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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Background

Vesnarinone is an inhibitor of phosphodiesterase 3 (PDE3; IC₅₀s = 10.7 and 13.2 μM for PDE3A and PDE3B, respectively).¹ It also inhibits ether-a-go-go-related gene 1 (ERG1) channels (IC₅₀ = 1.1 μM in HEK293T cells expressing human ERG1).² Vesnarinone (3-300 μM) increases contractile tension in isolated ventricular muscles of dog, cat, rabbit, and guinea pig in a dose-dependent manner.³ Oral and i.v. administration of vesnarinone increases right ventricular pressure with no effect on heart rate in dog models of tricuspid insufficiency- and pulmonary stenosis-induced congestive heart failure. It also increases contractility and coronary flow while decreasing heart rate in a guinea pig model of aortic stenosis-induced congestive heart failure. Formulations containing vesnarinone have been used for the treatment of congestive heart failure.⁴

1.Nikpour, M., Sadeghian, H., Saberi, M.R., et al.Design, synthesis and biological evaluation of 6-(benzyloxy)-4-methylquinolin-2(1H)-one derivatives as PDE3 inhibitorsBioorg. Med. Chem.18(2)855-862(2010) 2.Katayama, Y., Fujita, A., Ohe, T., et al.Inhibitory effects of vesnarinone on cloned cardiac delayed rectifier K+ channels expressed in a mammalian cell lineJ. Pharmacol. Exp. Ther.294(1)339-346(2000) 3.Feldman, A.M.Pharmacologic properties and clinical evaluation of the new inotropic agent OPC-8212 (vesnarinone)Cardiovasc. Drug Rev.11(1)1-11(1993) 4.Reis, S.E., Holubkov, R., Young, J.B., et al.Estrogen is associated with improved survival in aging women with congestive heart failure: Analysis of the vesnarinone studiesJ. Am. Coll. Cardiol.36(2)529-533(2000)