Milrinone

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Chemical Structure| 78415-72-2 同义名 : 米利酮 ;Win 47203;WIN 47,203;Milrinone, Primacor, Corotrop, Milrila, Win-47203
CAS号 : 78415-72-2
货号 : A218047
分子式 : C12H9N3O
纯度 : 99%
分子量 : 211.22
MDL号 : MFCD00133539
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(236.72 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
靶点

  • PDE2

    PDE2, IC50:5.2 μM

  • PDE3

    PDE3, IC50:2.1 μM
描述 Cyclic nucleotide phosphodiesterases (PDEs) from the human heart were separated into three isoforms, FI, FII and FIII. Milrinone has been proved to be a potent and selective inhibitor of human cardiac FIII PDE, a "low Km" enzyme for cyclic AMP (cAMP-PDE). The IC50 value for the inhibition of FIII PDE was 0.42 μM, while those of FI and FII PDEs, "high Km" enzymes, were 38 and 19 μM, respectively[3]. The concentration of milrinone that produced 50% relaxation of tracheal spirals constricted by carbachol was 3.6 × 10-5 M; The IC50 for milrinone for lung parenchymal strips contracted by histamine was 3.2 × 10-5 M; Milrinone relaxed pulmonary artery rings constricted by norepinephrine with an IC50 of 3.8 × 10-6 M[4]. Milrinone caused a concentration-dependent increase in the cAMP level in rabbit and human platelets with similar potency. Furthermore, milrinone inhibited human platelet aggregation with an IC50 of 2 μM. It was a very potent cardiotonic agent, which concentration-dependently increased left ventricular developed pressure (LVDP) and contractility as well as cAMP in rabbit coronary smooth muscle cells[5]. In rabbit heart, partial inhibition of PDE4 by milrinone contributed to greater increases in cardiomyocyte cAMP and calcium levels[6]. In mongrel dogs underwent pulmonary artery catheterization, Milrinone led to significant increases in right ventricular function as well as significant improvements in pulmonary vascular resistance, pulmonary blood flow, and left ventricular filling[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
NCT02606253 Heart Failure Phase 4 Active, not recruiting October 31, 2018 United States, Tennessee ... 展开 >> Vanderbilt University Medical Center Nashville, Tennessee, United States, 37204 收起 <<
NCT02884011 - Completed - United States, Illinois ... 展开 >> Rush Univeristy Medical Center Chicago, Illinois, United States, 60612 收起 <<
NCT02261506 Bacteremia Not Applicable Completed - Canada, Alberta ... 展开 >> Foothills Hospital Calgary, Alberta, Canada University of Alberta Hospital Edmonton, Alberta, Canada Canada, British Columbia Royal Columbian Hospital Vancouver, British Columbia, Canada St. Paul's Hospital Vancouver, British Columbia, Canada Canada, Manitoba St. Boniface Hospital Winnipeg, Manitoba, Canada Canada, Nova Scotia Queen Elizabeth II Hospital Halifax, Nova Scotia, Canada Canada, Ontario Kingston General Hospital Kingston, Ontario, Canada London Health Sciences Centre London, Ontario, Canada The Ottawa Hospital Ottawa, Ontario, Canada Sunnybrook Health Sciences Centre Toronto, Ontario, Canada, M4N3M5 Mount Sinai Hospital Toronto, Ontario, Canada St. Michael's Hospital Toronto, Ontario, Canada Toronto Western Hospital Toronto, Ontario, Canada Canada, Quebec CHUM Montreal, Quebec, Canada Université de Sherbrooke Sherbrooke, Quebec, Canada Canada Centre hospitalier affilié universitaire de Québec Quebec, Canada CSSS de Trois-Rivières Quebec, Canada 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.73mL

0.95mL

0.47mL

23.67mL

4.73mL

2.37mL

47.34mL

9.47mL

4.73mL
参考文献

[1]Cone J, Wang S, et al. Comparison of the effects of cilostazol and milrinone on intracellular cAMP levels and cellular function in platelets and cardiac cells. J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504.

[2]Shipley JB, Tolman D, et al. Milrinone: basic and clinical pharmacology and acute and chronic management. Am J Med Sci. 1996 Jun;311(6):286-91.

[3]Ito M, Tanaka T, Saitoh M, Masuoka H, Nakano T, Hidaka H. Selective inhibition of cyclic AMP phosphodiesterase from various human tissues by milrinone, a potent cardiac bipyridine. Biochem Pharmacol. 1988 May 15;37(10):2041-4. doi: 10.1016/0006-2952(88)90554-0. PMID: 2837222.

[4]Rossing TH, Drazen JM. Effects of milrinone on contractile responses of guinea pig trachea, lung parenchyma and pulmonary artery. J Pharmacol Exp Ther. 1986 Sep;238(3):874-9. PMID: 3746666.

[5]Cone J, Wang S, Tandon N, Fong M, Sun B, Sakurai K, Yoshitake M, Kambayashi J, Liu Y. Comparison of the effects of cilostazol and milrinone on intracellular cAMP levels and cellular function in platelets and cardiac cells. J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504. doi: 10.1097/00005344-199910000-00004. PMID: 10511123.

[6]Shakur Y, Fong M, Hensley J, Cone J, Movsesian MA, Kambayashi J, Yoshitake M, Liu Y. Comparison of the effects of cilostazol and milrinone on cAMP-PDE activity, intracellular cAMP and calcium in the heart. Cardiovasc Drugs Ther. 2002 Sep;16(5):417-27. doi: 10.1023/a:1022186402442. PMID: 12652111.

[7]Chen EP, Bittner HB, Davis RD Jr, Van Trigt P 3rd. Milrinone improves pulmonary hemodynamics and right ventricular function in chronic pulmonary hypertension. Ann Thorac Surg. 1997 Mar;63(3):814-21. doi: 10.1016/s0003-4975(97)00011-8. PMID: 9066407.