Mexiletine block of wild-type and inactivation-deficient human skeletal muscle hNav1.4 Na+ channels0

Journal of Physiology

Volumn 554, Issue 3, 2004, Pages 621-633

  Wang, Ging Kuo ^a   Russell, Corinna ^a   Wang, Sho Ya ^b  

^a HARVARD MEDICAL SCHOOL   (United States)

^b STATE UNIVERSITY OF NEW YORK   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIARRHYTHMIC AGENT; MEXILETINE; SODIUM CHANNEL; SODIUM CHANNEL BLOCKING AGENT; SODIUM ION; TOSYLCHLORAMIDE SODIUM; SODIUM CHANNEL NAV1.4;

ARTICLE; BETA CHAIN; CELL LINE; CELL STIMULATION; CHANNEL GATING; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG EFFICACY; HEART VENTRICLE ARRHYTHMIA; HUMAN; HUMAN CELL; HYPOTHESIS; IC 50; IN VIVO STUDY; LONG QT SYNDROME; MYOTONIA; NEUROPATHIC PAIN; PATHOPHYSIOLOGY; PRIORITY JOURNAL; PROTEIN EXPRESSION; SKELETAL MUSCLE; SODIUM CURRENT; THOMSEN DISEASE; WILD TYPE; CONCENTRATION RESPONSE; DEPOLARIZATION; DRUG MECHANISM; EMBRYO; HEK293 CELL LINE; HUMAN TISSUE; IC50; PHARMACOLOGICAL BLOCKING; SITE DIRECTED MUTAGENESIS; STEADY STATE;

ANTI-ARRHYTHMIA AGENTS; BINDING, COMPETITIVE; CELL LINE; CHLORAMINES; ELECTRIC CONDUCTIVITY; HOMEOSTASIS; HUMANS; MEXILETINE; MUSCLE PROTEINS; MUSCLE, SKELETAL; MUTATION; MYOCARDIUM; PATCH-CLAMP TECHNIQUES; RECEPTORS, CELL SURFACE; SODIUM CHANNEL BLOCKERS; SODIUM CHANNELS; TOSYL COMPOUNDS;

EID: 1242341914     PISSN: 00223751     EISSN: None     Source Type: Journal    
DOI: 10.1113/jphysiol.2003.054973     Document Type: Article

References (27)

1. Cahalan MD (1978). Local anesthetic block of sodium channels in normal and pronase- treated squid giant axons. Biophys J 23, 285-311.
2. Cannon SC (2002). An expanding view of the molecular basis of familial periodic paralysis. Neuromuscular Disorders 12, 533-543.
3. Cannon SC & Strittmatter SM (1993). Functional expression of sodium channel mutations identified in families with periodic paralysis. Neuron 10, 317-326.
4. Catterall WA & Mackie K (2001). Local anesthetics. In Goodman and Gilman's the Pharmacological Basis of Therapeutics, ed.Hardman, JG, Limbird, LE, Molinoff, PB, Ruddon, RW & Gilman, AG, pp. 367-384. Macmillan Publishing Co., New York.
5. Chabal C, Jacobson L, Mariano A, Chaney E & Britell CW (1992). The use of oral mexiletine for the treatment of pain after peripheral nerve injury. Anesthesiology 76, 513-517.
6. De Luca A, Natuzzi F, Desaphy JF, Loni G, Lentini G, Franchini C, Tortorella V & Camerino DC (2000). Molecular determinants of mexiletine structure for potent and use-dependent block of skeletal muscle sodium channels. Mol Pharmacol 57, 268-277.
7. Hamill OP, Marty E, Neher ME, Sakmann B & Sigworth FJ (1981). Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches. Pflugers Arch 391, 85-100.
8. Hille B (1977). Local anesthetics: hydrophilic and hydrophobic pathways for the drug receptor reaction. J General Physiol 69, 497-515.
9. Hille B (2001). Classical mechanisms of block. In Ion Channels of Excitable Membranes, pp. 503-536. Sinauer Associate Inc., Sunderland, MA, USA.
10. Hondeghem LM & Katzung BG (1977). Time- and voltage-dependent interactions of antiarrhythmic drugs with cardiac sodium channels. Biochim Biophys Acta 472, 373-398.
11. Jackson CE, Barohn RJ & Ptacek LJ (1994). Paramyotonia congenita: abnormal short exercise test, and improvement after mexiletine therapy. Muscle Nerve 17, 763-768.
12. Ju YK, Saint DA & Gage PW (1996). Hypoxia increases persistent sodium current in rat ventricular myocytes. J Physiol 497, 337-347.
13. Lehmann-Horn F & Jurkat-Rott K (1999). Voltage-gated ion channels and hereditary disease. Physiol Rev 79, 1317-1372.
14. Maltsev VA, Sabbah HN & Undrovinas AI (2001). Late sodium current is a novel target for amiodarone: studies in failing human myocardium. J Mol Cell Cardiol 33, 923-932.
15. Nan C, Wang S-Y, Strichartz GR & Wang GK (2000). Block of human heart hH1 sodium channels by the enantiomers of bupivacaine. Anesthesiology 93, 1022-1033.
16. O'Leary ME & Chahine M (2002). Cocaine binds to a common site on open and inactivated human heart (Nav1.5) sodium channel. J Physiol 541, 701-716.
17. + channels by local anesthetics. Science 265, 1724-1728.
18. + channels. Proc Natl Acad Sci U S A 93, 9270-9275.
19. Roden DM (2001). Antiarrhythmic drugs. In Goodman and Gilman's the Pharmacological Basis of Therapeutics, ed.Hardman, JG, Limbird, LE, Molinoff, PB, Ruddon, RW & Gilman, AG, pp. 933-970. Macmillan Publishing Co., New York.
20. + channel blockade and to increases in heart rate. Implications for gene-specific therapy. Circulation 92, 3381-3386.
21. + channel. J Physiol 537, 701-714.
22. Valenzuela C, Snyders DJ, Bennett PB, Tamargo J & Hondeghem LM (1995). Stereoselective block of cardiac sodium channels by bupivacaine in guinea pig ventricular myocytes. Circulation 92, 3014-3024.
23. Wang DW, Yazawa K, Maita N, George ALJ & Bennett PB (1997). Pharmacological targeting of long QT mutant sodium channels. J Clin Invest 99, 1714-1720.
24. Wang GK, Brodwick MS, Eaton DC & Strichartz GR (1987). Inhibition of sodium currents by local anesthetics in chloramine-T treated squid axons. J General Physiol 89, 645-667.
25. Wang S-Y, Bonner K, Russell C & Wang GK (2003). Tryptophan scanning of D1S6 and D4S6 C-termini in voltage-gated sodium channels. Biophys J 85, 911-920.
26. Weiser T, Qu Y, Catterall WA & Scheuer T (1999). Differential interaction of R-mexiletine with the local anesthetic receptor site on brain and heart sodium channel alpha-subunits. Mol Pharmacol 56, 1238-1244.
27. Yeh JZ (1978). Sodium inactivation mechanism modulates QA-314 block of sodium channels in squid axons. Biophys J 24, 569-574.