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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/01/30 18:16:50」(JST)

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Vesnarinone (INN) is a cardiotonic agent. A mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. Vesnarinone improves ventricular performance most in patients with the worst degree of heart failure.

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1. 収縮能障害による心不全における強心剤 inotropic agents in heart failure due to systolic dysfunction
2. 心臓手術施行患者の術後合併症 postoperative complications among patients undergoing cardiac surgery
3. 心臓リモデリング：臨床的評価および治療 cardiac remodeling clinical assessment and therapy

English Journal

Visualization and dynamics of multidimensional health-related quality-of-life-adjusted overall survival: a new analytic approach.

Andrei AC, Grady KL.Author information Bluhm Carrdiovascular Institute, Northwestern University, 676 N St Clair St., Suite 1700, Chicago, IL, USA, aandrei@nmh.org.AbstractBACKGROUND: Vesnarinone Trial (VesT) was a three-armed, placebo-controlled, randomized clinical trial designed to study the effects of 30 mg or 60 mg/day vesnarinone. Certain contradictory results involving patient health-related quality-of-life (HRQOL) and overall survival (OS) have made a definitive and unified conclusion difficult.
Quality of life research : an international journal of quality of life aspects of treatment, care and rehabilitation.Qual Life Res.2014 Jan 7. [Epub ahead of print]
BACKGROUND: Vesnarinone Trial (VesT) was a three-armed, placebo-controlled, randomized clinical trial designed to study the effects of 30 mg or 60 mg/day vesnarinone. Certain contradictory results involving patient health-related quality-of-life (HRQOL) and overall survival (OS) have made a definiti
PMID 24395525

Vesnarinone suppresses TNFα mRNA expression by inhibiting valosin-containing protein.

Hotta K, Nashimoto A, Yasumura E, Suzuki M, Azuma M, Iizumi Y, Shima D, Nabeshima R, Hiramoto M, Okada A, Sakata-Sogawa K, Tokunaga M, Ito T, Ando H, Sakamoto S, Kabe Y, Aizawa S, Imai T, Yamaguchi Y, Watanabe H, Handa H.Author information Graduate School of Bioscience and Biotechnology, Tokyo Institute of Technology, Yokohama, Kanagawa, Japan.AbstractVesnarinone is a synthetic quinolinone derivative used in the treatment of cardiac failure and cancer. It is also known to cause agranulocytosis as a side effect, which restricts its use, although the mechanism underlying agranulocytosis is not well understood. Here, we show that vesnarinone binds to valosin-containing protein (VCP), which interacts with polyubiquitinated proteins and is essential for the degradation of IκBα to activate nuclear factor (NF)κB. We show that vesnarinone impairs the degradation of IκBα, and that the impairment of the degradation of IκBα is the result of the inhibition of the interaction between VCP and the 26S proteasome by vesnarinone. These results suggest that vesnarinone suppresses NFκB activation by inhibiting the VCP-dependent degradation of polyubiquitinated IκBα, resulting in the suppression of tumor necrosis factor-α mRNA expression.
Molecular pharmacology.Mol Pharmacol.2013 May;83(5):930-8. doi: 10.1124/mol.112.081935. Epub 2013 Feb 7.
Vesnarinone is a synthetic quinolinone derivative used in the treatment of cardiac failure and cancer. It is also known to cause agranulocytosis as a side effect, which restricts its use, although the mechanism underlying agranulocytosis is not well understood. Here, we show that vesnarinone binds t
PMID 23393163

New predictive models of heart failure mortality using time-series measurements and ensemble models.

Subramanian D, Subramanian V, Deswal A, Mann DL.Author information Department of Computer Science, Rice University, Houston, TX 77005, USA. devika@rice.eduAbstractBACKGROUND: Morbidity and mortality rates associated with heart failure remain high. A wide variety of demographic and clinical factors as well as biomarkers are associated with increased mortality rates. Despite this, most multivariate predictive models for heart failure mortality have predictive accuracies characterized by a C-statistic (area under the receiver operating curve) of ≈0.74.
Circulation. Heart failure.Circ Heart Fail.2011 Jul;4(4):456-62. doi: 10.1161/CIRCHEARTFAILURE.110.958496. Epub 2011 May 11.
BACKGROUND: Morbidity and mortality rates associated with heart failure remain high. A wide variety of demographic and clinical factors as well as biomarkers are associated with increased mortality rates. Despite this, most multivariate predictive models for heart failure mortality have predictive a
PMID 21562057

Japanese Journal

Vesnarinone downregulates CXCR4 expression via upregulation of Kruppel-like factor 2 in oral cancer cells

Uchida Daisuke,Onoue Tomitaro,Begum Nasima-Mila,Kuribayashi Nobuyuki,Tomizuka Yoshifumi,Tamatani Tetsuya,Nagai Hirokazu,Miyamoto Youji
MOLECULAR CANCER 8, 2009
NAID 120004710201

ケモカインレセプターCXCR4を標的とした口腔癌に対するリンパ節転移抑制療法の開発

富塚佳史
四国歯学会雑誌 20(1), 155-175, 2007-06
… Consequently, vesnarinone, a newly identified chemotherapeutic agent, trascriptionally downregulated CXCR4. … Vesnarinone inhibited the cell migration induced by SDF-1 and lymph node metastasis of cells in the orthotopic inoculation model. … By using several deletion constructs against CXCR4 promoters, the minimal vesnarinone-responsive element in the CXCR4 promoter region at -300 to -167 relative to the transcription start site was identified. …
NAID 110006561013

「ベスナリノン」

Vesnarinone
Systematic (IUPAC) name
	6-[4-(3,4-dimethoxybenzoyl)piperazin-1-yl]-3,4-dihydro-1H-quinolin-2-one
Clinical data
AHFS/Drugs.com	International Drug Names
Legal status	℞ Prescription only
Routes	Oral
Identifiers
CAS number	81840-15-5
ATC code	None
PubChem	CID 5663
UNII	5COW40EV8M
ChEMBL	CHEMBL17423
Chemical data
Formula	C22H25N3O4
Mol. mass	395.45 g/mol
	SMILES COC1=C(C=C(C=C1)C(=O)N2CCN(CC2)C3=CC4=C(C=C3)NC(=O)CC4)OC;
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英: vesnarinone
商: アーキンZ
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vesnarinone