Use-dependent block of cardiac late Na+ current by ranolazine

Heart Rhythm

Volumn 6, Issue 11, 2009, Pages 1625-1631

  Rajamani, Sridharan ^a   El Bizri, Nesrine ^a   Shryock, John C ^a   Makielski, Jonathan C ^b   Belardinelli, Luiz ^a  

^a GILEAD SCIENCES   (United States)

^b UNIVERSITY OF WISCONSIN SCHOOL OF MEDICINE AND PUBLIC HEALTH   (United States)

Author keywords

Angina; Late sodium; Ranolazine; Sodium channel; Tachycardia

Indexed keywords

PROTEIN SCN5A; RANOLAZINE; SODIUM CHANNEL; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG POTENCY; DRUG PROTEIN BINDING; EMBRYO; HEART ELECTROPHYSIOLOGY; HUMAN; HUMAN CELL; HYPERPOLARIZATION; IC 50; PRIORITY JOURNAL; QT PROLONGATION; SITE DIRECTED MUTAGENESIS; SODIUM CURRENT; STEADY STATE; WILD TYPE;

ACETANILIDES; ACTION POTENTIALS; ENZYME INHIBITORS; HUMANS; PIPERAZINES; SODIUM CHANNELS; TACHYCARDIA;

EID: 70449119097     PISSN: 15475271     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.hrthm.2009.07.042     Document Type: Article

References (25)

1. Rajamani S., Shryock J.C., and Belardinelli L. Block of tetrodotoxin-sensitive, Na(V)1.7 and tetrodotoxin-resistant, Na(V)1.8, Na(+) channels by ranolazine. Channels (Austin) 2 6 (2008) 449-460
2. Wang G.K., Calderon J., and Wang S.Y. State- and use-dependent block of muscle Nav1.4 and neuronal Nav1.7 voltage-gated Na+ channel isoforms by ranolazine 73 (2008) 940-948
3. Dudel J., Peper K., Rudel R., et al. Effect of tetrodotoxin on membrane currents in mammalian cardiac fibres. Nature 213 (1967) 296-297
4. Maltsev V.A., Sabbah H.N., Higgins R.S., et al. Novel, ultraslow inactivating sodium current in human ventricular cardiomyocytes. Circulation 98 (1998) 2545-2552
5. Nagatomo T., January C.T., and Makielski J.C. Preferential block of late sodium current in the LQT3 DeltaKPQ mutant by the class I(C) antiarrhythmic flecainide. Mol Pharm 57 (2000) 101-107
6. Dumaine R., and Kirsch G.E. Mechanism of lidocaine block of late current in long Q-T mutant Na+ channels. Am J Physiol 274 (1998) H477-H487
7. Wang D.W., Yazawa K., Makita N., et al. Pharmacological targeting of long QT mutant sodium channels. J Clin Invest 99 (1997) 1714-1720
8. Antzelevitch C., Belardinelli L., Zygmunt A.C., et al. Electrophysiological effects of ranolazine, a novel antianginal agent with antiarrhythmic properties. Circulation 110 (2004) 904-910
9. Undrovinas A.I., Belardinelli L., Undrovinas N.A., et al. Ranolazine improves abnormal repolarization and contraction in left ventricular myocytes of dogs with heart failure by inhibiting late sodium current. J Cardiovasc Electrophysiol 17 Suppl 1 (2006) S169-S177
10. Scirica B.M., Morrow D.A., Hod H., et al. Effect of ranolazine, an antianginal agent with novel electrophysiological properties, on the incidence of arrhythmias in patients with non ST-segment elevation acute coronary syndrome: results from the Metabolic Efficiency With Ranolazine for Less Ischemia in Non ST-Elevation Acute Coronary Syndrome Thrombolysis in Myocardial Infarction 36 (MERLIN-TIMI 36) randomized controlled trial. Circulation 116 (2007) 1647-1652
11. Zaza A., Belardinelli L., and Shryock J.C. Pathophysiology and pharmacology of the cardiac "late sodium current.". Pharmacol Ther 119 (2008) 326-339
12. Vassalle M., Bocchi L., and Du F. A slowly inactivating sodium current (INa2) in the plateau range in canine cardiac Purkinje single cells. Exp Physiol 92 (2007) 161-173
13. Makita N., Shirai N., Nagashima M., et al. A de novo missense mutation of human cardiac Na+ channel exhibiting novel molecular mechanisms of long QT syndrome. FEBS Lett 423 (1998) 5-9
14. Oginosawa Y., Nagatomo T., Abe H., et al. Intrinsic mechanism of the enhanced rate-dependent QT shortening in the R1623Q mutant of the LQT3 syndrome. Cardiovasc Res 65 (2005) 138-147
15. Hondeghem L.M., and Katzung B.G. Antiarrhythmic agents: the modulated receptor mechanism of action of sodium and calcium channel-blocking drugs. Ann Rev Pharmacol Toxicol 24 (1984) 387-423
16. Hille B. Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reaction. J Gen Physiol 69 (1977) 497-515
17. Belardinelli L., Shryock J.C., and Fraser H. Inhibition of the late sodium current as a potential cardioprotective principle: effects of the late sodium current inhibitor ranolazine. Heart 92 Suppl 4 (2006) iv6-iv14
18. Bennett P.B., Yazawa K., Makita N., et al. Molecular mechanism for an inherited cardiac arrhythmia. Nature 376 (1995) 683-685
19. + current in human ventricular cardiomyocytes. Cardiovasc Res 69 (2006) 116-127
20. Valdivia C.R., Chu W.W., Pu J., et al. Increased late sodium current in myocytes from a canine heart failure model and from failing human heart. J Mol Cell Cardiol 38 (2005) 475-483
21. Moss A.J., Zareba W., Schwarz K.Q., et al. Ranolazine shortens repolarization in patients with sustained inward sodium current due to type-3 long-QT syndrome. J Cardiovasc Electrophysiol 12 (2008) 1289-1293
22. Berecki G., Zegers J.G., Bhuiyan Z.A., et al. Long-QT syndrome-related sodium channel mutations probed by the dynamic action potential clamp technique. J Physiol 570 (2006) 237-250
23. Dumaine R., Towbin J.A., Brugada P., et al. Ionic mechanisms responsible for the electrocardiographic phenotype of the Brugada syndrome are temperature dependent. Circ Res 85 (1999) 803-809
24. Nagatomo T., Fan Z., Ye B., et al. Temperature dependence of early and late currents in human cardiac wild-type and long Q-T DeltaKPQ Na+ channels. Am J Physiol 275 (1998) H2016-H2024
25. Rivolta I., Abriel H., Tateyama M., et al. Inherited Brugada and long QT-3 syndrome mutations of a single residue of the cardiac sodium channel confer distinct channel and clinical phenotypes. J Biol Chem 276 (2001) 30623-30630