VESNARINONE Chemical Properties

Melting point:

238.1-239.5° (Tominaga); mp 238.1-239.8° (Shimizu)

Boiling point:

519.41°C (rough estimate)

Density 

1.2414 (rough estimate)

refractive index 

1.6500 (estimate)

storage temp. 

Store at -20°C

solubility 

DMSO:9.84(Max Conc. mg/mL);24.88(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.26(Max Conc. mM)
DMF:3.0(Max Conc. mg/mL);7.59(Max Conc. mM)

form 

A crystalline solid

pka

2.86(at 25℃)

color 

White to off-white

VESNARINONE Usage And Synthesis

Description

Vesnarinone is a new orally-active positive inotropic agent introduced for the treatment of congestive heart failure. It exerts a positive inotropic effect on the heart and has a peripheral vasodilatory effect. Vesnarinone is claimed not to affect heart rate or aggravate arrhythmia.

Description

Vesnarinone is an inhibitor of phosphodiesterase 3 (PDE3; IC₅₀s = 10.7 and 13.2 μM for PDE3A and PDE3B, respectively). It also inhibits ether-a-go-go-related gene 1 (ERG1) channels (IC₅₀ = 1.1 μM in HEK293T cells expressing human ERG1). Vesnarinone (3-300 μM) increases contractile tension in isolated ventricular muscles of dog, cat, rabbit, and guinea pig in a dose-dependent manner. 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.

Originator

Otsuka (Japan)

Uses

Cardiotonic.

Definition

ChEBI: Arkin (TN) is an organic molecular entity.

brand name

Arkin (Otsuka America);Arkin-Z.

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