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| | Ranolazine dihydrochloride Basic information |
| | Ranolazine dihydrochloride Chemical Properties |
| Melting point | 222-229.5 °C(lit.) | | storage temp. | Desiccate at RT | | solubility | H2O: 10 mg/mL, soluble | | form | solid | | color | off-white | | Water Solubility | H2O: soluble ≥10mg/mL | | Merck | 14,8111 | | Stability: | Hygroscopic | | CAS DataBase Reference | 95635-56-6(CAS DataBase Reference) |
| Safety Statements | 22-24/25 | | WGK Germany | 3 | | RTECS | TK7845370 | | HS Code | 29335990 |
| | Ranolazine dihydrochloride Usage And Synthesis |
| Description | Ranolazine is a piperazine derivative with cardioprotective activity. It reduces the late sodium current (INa) in mouse myocytes expressing the long QT syndrome 3 mutant sodium channel DKPQ, ventricular myocytes isolated from a canine model of heart failure, guinea pig ventricular myocytes exposed to hydrogen peroxide or anemone toxin-II, and HEK293 cells expressing human Nav1.5 channels (IC50s = 5.9-15 μM) as well as the late potassium current (IKr) in canine ventricular myocytes and HEK293 cells (IC50s = 11.5 and 14.4 μM, respectively). Ranolazine also inhibits radioligand binding to α1-, β1-, and β2-adrenergic receptors (Kis = 8.2-19.5, 1.4-8.6, and 0.5-14.8 μM, respectively). In vivo, ranolazine (480 μg/kg per min) reduces clofilium-induced prolongation of the QTc interval and Torsade de Pointes (TdP) in rabbits. Ranolazine also reduces interstitial collagen deposition as well as atrial natriuretic peptide (ANP; Item Nos. 24539 | 24276), connective tissue growth factor (CTGF), brain natriuretic peptide (BNP; ), and matrix metalloproteinase-2 (MMP-2) mRNA levels, and prevents left ventricular dilation in a mouse model of cardiotoxicity induced by doxorubicin . | | Chemical Properties | White Crystalline Powder | | Uses | treatment of angina and congestive heart failure | | Uses | Ranolazine Dihydrochloride is an anti-ischemic agent which modulates myocardial metabolism. Antianginal. | | Biological Activity | Antianginal agent with antiarrhythmic properties that acts as a partial fatty acid oxidation inhibitor. Activates pyruvate dehydrogenase in ischemic myocytes to promote glucose oxidation, switching substrate utilization from fatty acids to glucose. Also shown to inhibit late I Na and I Kr currents. | | Biochem/physiol Actions | Ranolazine is a derivative of anti-ischemic piperazine and acts as sodium (Na+)-current inhibitor. It has the potential to treat diastolic heart failure and helps in ameliorating myocardial diastolic function. | | storage | Desiccate at RT | | References | [1] J C SHRYOCK L B. Inhibition of late sodium current to reduce electrical and mechanical dysfunction of ischaemic myocardium[J]. British Journal of Pharmacology, 2009, 153 6: 1128-1132. DOI: 10.1038/sj.bjp.0707522
[2] RICHARD L VERRIER. Mechanisms of ranolazine’s dual protection against atrial and ventricular fibrillation.[J]. Europace, 2013, 15 3: 317-324. DOI: 10.1093/europace/eus380
[3] WEI-QUN WANG. Antitorsadogenic effects of ({+/-})-N-(2,6-dimethyl-phenyl)-(4[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazine (ranolazine) in anesthetized rabbits.[J]. Journal of Pharmacology and Experimental Therapeutics, 2008, 325 3: 875-881. DOI: 10.1124/jpet.108.137729
[4] CARLO G. TOCCHETTI. Ranolazine protects from doxorubicin-induced oxidative stress and cardiac dysfunction[J]. European Journal of Heart Failure, 2014, 16 4: 358-366. DOI: 10.1002/ejhf.50 |
| | Ranolazine dihydrochloride Preparation Products And Raw materials |
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