81840-15-5 Usage
Description
VESNARINONE, also known as Arkin or Arkin-Z, is a novel orally-active positive inotropic agent specifically introduced for the treatment of congestive heart failure. It possesses the unique ability to exert a positive inotropic effect on the heart, enhancing its contractility, while also providing a peripheral vasodilatory effect. Notably, VESNARINONE is distinguished by its lack of impact on heart rate and its non-aggravating nature towards arrhythmia, making it a promising pharmaceutical candidate for heart failure management.
VESNARINONE functions as an inhibitor of phosphodiesterase 3 (PDE3), with IC50 values of 10.7 and 13.2 μM for PDE3A and PDE3B, respectively. Additionally, it inhibits ether-a-go-go-related gene 1 (ERG1) channels, with an IC50 of 1.1 μM in HEK293T cells expressing human ERG1. These actions contribute to its efficacy in increasing contractile tension in isolated ventricular muscles across various species, including dogs, cats, rabbits, and guinea pigs, in a dose-dependent manner.
In different animal models of heart failure, VESNARINONE has demonstrated its cardiotonic properties. In dog models with tricuspid insufficiency and pulmonary stenosis-induced congestive heart failure, oral and intravenous administration of VESNARINONE increases right ventricular pressure without affecting heart rate. Similarly, in a guinea pig model of aortic stenosis-induced congestive heart failure, it enhances contractility and coronary flow while simultaneously decreasing heart rate.
Used in Pharmaceutical Industry:
VESNARINONE is used as a cardiotonic agent for the treatment of congestive heart failure. Its unique mechanism of action, which includes positive inotropic effects and peripheral vasodilation without influencing heart rate or exacerbating arrhythmia, makes it a valuable asset in managing heart failure conditions. Formulations containing VESNARINONE, such as those available under the brand names Arkin and Arkin-Z, have been specifically developed and utilized for this purpose, offering an effective therapeutic option for patients suffering from congestive heart failure.
Check Digit Verification of cas no
The CAS Registry Mumber 81840-15-5 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 8,1,8,4 and 0 respectively; the second part has 2 digits, 1 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 81840-15:
(7*8)+(6*1)+(5*8)+(4*4)+(3*0)+(2*1)+(1*5)=125
125 % 10 = 5
So 81840-15-5 is a valid CAS Registry Number.
InChI:InChI=1/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)
81840-15-5Relevant articles and documents
Pd-Catalyzed Site-Selective Borylation of Simple Arenes via Thianthrenation?
Chen, Xiao-Yue,Huang, Yu-Hao,Zhou, Jian,Wang, Peng
, p. 1269 - 1272 (2020/08/13)
Site-selective borylation of simple arenes was realized in one pot via an electrophilic thianthrenation/Pd-catalyzed borylation sequence. The key to achieve this operatically simple process is the use of Pd catalysis, which could tolerate the solvent and acidic conditions used in the thianthrenation step. This protocol features mild conditions, broad functional group tolerance, and simple manipulations, and is suitable for late-stage functionalization of a wide range of pharmaceuticals and complex bioactive molecules.
Studies on positive inotropic agents. I. Synthesis of 3,4-dihydro-6-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]- 2(1 H)-quinolinone and related compounds
Tominaga,Yo,Ogawa,Yamashita,Yabuuchi,Nakagawa
, p. 2100 - 2110 (2007/10/02)
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