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Amrinone

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Chemical Structure| 60719-84-8 同义名 : Inamrinone;WIN 40,680
CAS号 : 60719-84-8
货号 : A110103
分子式 : C10H9N3O
纯度 : 99%
分子量 : 187.198
MDL号 : MFCD00083228
存储条件:

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 16 mg/mL(85.47 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Amrinone is a type 3 pyridine phosphodiesterase inhibitor used in the treatment of congestive heart failure. Amrinone increases cyclic adenosine monophosphate by preventing its breakdown[3]. Amrinone is administered subcutaneously to rats at a dose of 10 mg/kg/day for 14 days, significant reduction of neointimal thickness was noted. Amrinone produced a dose-dependent inhibition of ADP-induced rat platelet aggregation in vitro as well as ex vivo in rats. The proliferation of human aortic smooth muscle cells in culture stimulated with FBS or PDGF was also inhibited by amrinone[4]. Amrinone produced positive inotropic and lusitropic effects in both conscious and anesthetized dogs with autonomic nervous system blockade[5]. Amrinone caused enhancement of right ventricular contractility and afterload reduction[6]. Augmentation of myocardial contraction by amrinone in patients with chronic coronary artery disease and severe baseline left ventricular dysfunction predicts improvement in left ventricular ejection fraction after coronary artery bypass graft surgery[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02174029 - Completed - Canada, British Columbia ... 展开 >> Royal Columbian Hospital New Westminster, British Columbia, Canada, V3L 3W7 收起 <<
NCT00060840 - Completed - -
NCT00060840 Congestive Heart Failure Phase 2 Completed - United States, New Jersey ... 展开 >> Newark Beth Isreal Medical Center Newark, New Jersey, United States, 07112 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Ohio University of Cincinnati Cincinnati, Ohio, United States, 45219 Cleveland Clinic Foundation Cleveland, Ohio, United States, 44195 United States, Pennsylvania Allegheny General Hospital Pittsburgh, Pennsylvania, United States, 15212 United States, Texas Baylor University Medical Center Dallas, Texas, United States, 75226 University of Texas/St. Paul Medical Center Dallas, Texas, United States, 75390 Texas Heart Institute Houston, Texas, United States, 20345 Germany Herz-und Diabeteszentrum Nordrhein-Westfalen Gergstrab, Bad Oeynhausen, Germany, 32545 Deutsches Herfzzentrum Berlin Augustenburger Platz, Berlin, Germany, 13353 United Kingdom Harefield Hospital Harefield, Middlesex, United Kingdom, UB96JH 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.34mL

1.07mL

0.53mL

26.71mL

5.34mL

2.67mL

53.42mL

10.68mL

5.34mL

参考文献

[1]Asif M. Phosphodiesterase-III Inhibitors Amrinone and Milrinone on Epilepsy and Cardiovascular Activities. N Am J Med Sci. 2012 Oct;4(10):499-502.

[2]Xiong W, Ferrier GR, Howlett SE. Diminished inotropic response to amrinone in ventricular myocytes from myopathic hamsters is linked to depression of high-gain Ca2+-induced Ca2+ release. J Pharmacol Exp Ther. 2004 Aug;310(2):761-73.

[3]Ichioka S, Nakatsuka T, Ohura N, Sato Y, Harii K. Clinical use of amrinone (a selective phosphodiesterase III inhibitor) in reconstructive surgery. Plast Reconstr Surg. 2001 Dec;108(7):1931-7

[4]Hachisu M, Nomura M, Fujishima K. [Effects of amrinone, an inhibitor of c-AMP-specific phosphodiesterases, on neointimal hyperplasia after balloon injury in rats]. Nihon Yakurigaku Zasshi. 1998 Oct;112(4):267-74. Japanese

[5]Pagel PS, Hettrick DA, Warltier DC. Amrinone enhances myocardial contractility and improves left ventricular diastolic function in conscious and anesthetized chronically instrumented dogs. Anesthesiology. 1993 Oct;79(4):753-65

[6]Ochiai Y, Morita S, Tanoue Y, Kawachi Y, Tominaga R, Yasui H. Effects of amrinone, a phosphodiesterase inhibitor, on right ventricular/arterial coupling immediately after cardiac operations. J Thorac Cardiovasc Surg. 1998 Jul;116(1):139-47

[7]Perez-Baliño NA, Masoli OH, Meretta AH, Rodriguez A, Cragnolino DE, Perrone S, Boullon F, Mele E, Palacios I, Brown KA. Amrinone stimulation test: ability to predict improvement in left ventricular ejection fraction after coronary bypass surgery in patients with poor baseline left ventricular function. J Am Coll Cardiol. 1996 Nov 15;28(6):1488-92