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| | VESNARINONE Basic information |
| Product Name: | VESNARINONE | | Synonyms: | VESNARINONE;Arkin;Piteranometozine;OPC 8212;6-[4-(3,4-Dimethoxybenzoyl)-1-piperazinyl]-3,4-dihydro-2(1H)-quinolinone;2(1H)-Quinolinone, 6-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]-3,4-dihydro-;0PC-8212;3，4-Dihydro-6-[4-(3，4-dimethoxybenzoyl)-1-piperazinyl]-2(1H)-quinolinone | | CAS: | 81840-15-5 | | MF: | C22H25N3O4 | | MW: | 395.45 | | EINECS: | | | Product Categories: | | | Mol File: | 81840-15-5.mol |  |
| | 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℃) |
| | 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. |
| | VESNARINONE Preparation Products And Raw materials |
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