Vesnarinone

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.Formal Name: 6-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]-3,4-dihydro-2(1H)-quinolinone. CAS Number: 81840-15-5. Synonyms: OPC 8212. Molecular Formula: C22H25N3O4. Formula Weight: 395.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMSO: 3 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 272 nm. SMILES: COC1=CC=C(C(N2CCN(C3=CC(CCC(N4)=O)=C4C=C3)CC2)=O)C=C1OC. InChi Code: InChI=1S/C22H25N3O4/c1-28-19-7-3-16(14-20(19)29-2)22(27)25-11-9-24(10-12-25)17-5-6-18-15(13-17)4-8-21(26)23-18/h3,5-7,13-14H,4,8-12H2,1-2H3,(H,23,26). InChi Key: ZVNYJIZDIRKMBF-UHFFFAOYSA-N.