Synonym
Milrinone, Primacor, Corotrop, Milrila, Win-47203
IUPAC/Chemical Name
6-methyl-2-oxo-5-pyridin-4-yl-1H-pyridine-3-carbonitrile
InChi Key
PZRHRDRVRGEVNW-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H9N3O/c1-8-11(9-2-4-14-5-3-9)6-10(7-13)12(16)15-8/h2-6H,1H3,(H,15,16)
SMILES Code
N#CC1=CC(C2=CC=NC=C2)=C(C)NC1=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
Milrinone is a PDE3 inhibitor, and also an inotrope and vasodilator.
In vitro activity:
This study examined functional regulation of TP receptors by serine phosphorylation and effects of IP receptor stimulation and protein kinase A (PKA) activity on TP receptor sensitivity in myocytes from neonatal porcine resistance pulmonary arteries after 72 h hypoxia in vitro. Milrinone normalized TP receptor sensitivity in hypoxic myocytes by restoring PKA-mediated regulatory TP receptor phosphorylation
Reference: Br J Pharmacol. 2011 Jul;163(6):1223-36. https://pubmed.ncbi.nlm.nih.gov/21385177/
In vivo activity:
In CHF rats, intravenous infusion of milrinone reduced both pulmonary and systemic arterial blood pressure. In contrast, inhalation of milrinone predominantly dilated pulmonary blood vessels, resulting in a reduced pulmonary-to-systemic vascular resistance ratio. Repeated milrinone inhalations in 20-min intervals caused a stable reduction of pulmonary artery pressure.
Reference: Anesthesiology. 2007 Jan;106(1):124-31. https://pubmed.ncbi.nlm.nih.gov/17197854/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMF |
0.3 |
1.42 |
|
| DMSO |
28.4 |
134.48 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
211.22
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Santhosh KT, Elkhateeb O, Nolette N, Outbih O, Halayko AJ, Dakshinamurti S. Milrinone attenuates thromboxane receptor-mediated hyperresponsiveness in hypoxic pulmonary arterial myocytes. Br J Pharmacol. 2011 Jul;163(6):1223-36. doi: 10.1111/j.1476-5381.2011.01306.x. PMID: 21385177; PMCID: PMC3144536.
2. 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.
3. Hentschel T, Yin N, Riad A, Habbazettl H, Weimann J, Koster A, Tschope C, Kuppe H, Kuebler WM. Inhalation of the phosphodiesterase-3 inhibitor milrinone attenuates pulmonary hypertension in a rat model of congestive heart failure. Anesthesiology. 2007 Jan;106(1):124-31. doi: 10.1097/00000542-200701000-00021. PMID: 17197854.
4. 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.
In vitro protocol:
1. Santhosh KT, Elkhateeb O, Nolette N, Outbih O, Halayko AJ, Dakshinamurti S. Milrinone attenuates thromboxane receptor-mediated hyperresponsiveness in hypoxic pulmonary arterial myocytes. Br J Pharmacol. 2011 Jul;163(6):1223-36. doi: 10.1111/j.1476-5381.2011.01306.x. PMID: 21385177; PMCID: PMC3144536.
2. 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.
In vivo protocol:
1. Hentschel T, Yin N, Riad A, Habbazettl H, Weimann J, Koster A, Tschope C, Kuppe H, Kuebler WM. Inhalation of the phosphodiesterase-3 inhibitor milrinone attenuates pulmonary hypertension in a rat model of congestive heart failure. Anesthesiology. 2007 Jan;106(1):124-31. doi: 10.1097/00000542-200701000-00021. PMID: 17197854.
2. 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.
1: Burkhardt BE, Rücker G, Stiller B. Prophylactic milrinone for the prevention of low cardiac output syndrome and mortality in children undergoing surgery for congenital heart disease. Cochrane Database Syst Rev. 2015 Mar 25;3:CD009515. doi: 10.1002/14651858.CD009515.pub2. Review. PubMed PMID: 25806562.
2: Majure DT, Greco T, Greco M, Ponschab M, Biondi-Zoccai G, Zangrillo A, Landoni G. Meta-analysis of randomized trials of effect of milrinone on mortality in cardiac surgery: an update. J Cardiothorac Vasc Anesth. 2013 Apr;27(2):220-9. doi: 10.1053/j.jvca.2012.08.005. Epub 2012 Oct 10. Review. PubMed PMID: 23063100.
3: Kato M, Hirayama A. [Combination therapy; dobutamine and milrinone]. Nihon Rinsho. 2011 Nov;69 Suppl 9:428-33. Review. Japanese. PubMed PMID: 22724242.
4: Meyer S, Gortner L, Brown K, Abdul-Khaliq H. The role of milrinone in children with cardiovascular compromise: review of the literature. Wien Med Wochenschr. 2011 Apr;161(7-8):184-91. doi: 10.1007/s10354-011-0869-7. Epub 2011 Mar 7. Review. PubMed PMID: 21360291.
5: Bassler D, Kreutzer K, McNamara P, Kirpalani H. Milrinone for persistent pulmonary hypertension of the newborn. Cochrane Database Syst Rev. 2010 Nov 10;(11):CD007802. doi: 10.1002/14651858.CD007802.pub2. Review. PubMed PMID: 21069698.
6: Jennings DL, Thompson ML. Use of combination therapy with a beta-blocker and milrinone in patients with advanced heart failure. Ann Pharmacother. 2009 Nov;43(11):1872-6. doi: 10.1345/aph.1M357. Epub 2009 Sep 29. Review. PubMed PMID: 19789358.
7: Denault AY, Lamarche Y, Couture P, Haddad F, Lambert J, Tardif JC, Perrault LP. Inhaled milrinone: a new alternative in cardiac surgery? Semin Cardiothorac Vasc Anesth. 2006 Dec;10(4):346-60. Review. PubMed PMID: 17200091.
8: Levy JH, Bailey JM, Deeb GM. Intravenous milrinone in cardiac surgery. Ann Thorac Surg. 2002 Jan;73(1):325-30. Review. PubMed PMID: 11834047.
9: Ricksten S. [The pulmonary vasodilatory effect of inhaled prostacyclin and milrinone in heart]. Rev Esp Anestesiol Reanim. 2001 Dec;48(10):460-1. Review. Spanish. PubMed PMID: 11792300.
10: Sherry KM, Locke TJ. Use of milrinone in cardiac surgical patients. Cardiovasc Drugs Ther. 1993 Aug;7(4):671-5. Review. PubMed PMID: 8241010.
11: Feneck RO. Milrinone and postoperative pulmonary hypertension. J Cardiothorac Vasc Anesth. 1993 Apr;7(2 Suppl 1):21-3. Review. PubMed PMID: 8471746.
12: Copp MV, Hill AJ, Feneck RO. Overview of the effects of intravenous milrinone in acute heart failure following surgery. Eur J Anaesthesiol Suppl. 1992;5:35-41. Review. PubMed PMID: 1600968.
13: Kittleson MD. The efficacy and safety of milrinone for treating heart failure in dogs. Vet Clin North Am Small Anim Pract. 1991 Sep;21(5):905-18. Review. PubMed PMID: 1949499.
14: DiBianco R. Clinical results with oral milrinone in heart failure. Eur Heart J. 1989 Aug;10 Suppl C:44-52. Review. PubMed PMID: 2680497.
15: Colucci WS. Myocardial and vascular actions of milrinone. Eur Heart J. 1989 Aug;10 Suppl C:32-8. Review. PubMed PMID: 2680495.
16: Farah AE, Frangakis CJ. Studies on the mechanism of action of the bipyridine milrinone on the heart. Basic Res Cardiol. 1989;84 Suppl 1:85-103. Review. PubMed PMID: 2554875.
17: Young RA, Ward A. Milrinone. A preliminary review of its pharmacological properties and therapeutic use. Drugs. 1988 Aug;36(2):158-92. Review. PubMed PMID: 3053125.
18: Blais DM. Nesiritide compared with milrinone for cardiac surgery. Ann Pharmacother. 2007 Mar;41(3):502-4. Epub 2007 Feb 27. Review. PubMed PMID: 17327288.
19: Bayram M, De Luca L, Massie MB, Gheorghiade M. Reassessment of dobutamine, dopamine, and milrinone in the management of acute heart failure syndromes. Am J Cardiol. 2005 Sep 19;96(6A):47G-58G. Review. PubMed PMID: 16181823.
20: Boger JE, DeLuca SL, Watkins DF, Vershave KK, Thomley AM. Infusion therapy with milrinone in the home care setting for patients who have advanced heart failure. J Intraven Nurs. 1997 May-Jun;20(3):148-54. Review. PubMed PMID: 9214927.
