The position of the fast-inactivation gate during lidocaine block of voltage-gated Na+ channels

Journal of General Physiology

Volumn 113, Issue 1, 1999, Pages 7-16

  Vedantham, Vasanth ^a   Cannon, Stephen C ^a,b  

^a HARVARD MEDICAL SCHOOL   (United States)

^b MASSACHUSETTS GENERAL HOSPITAL   (United States)

Author keywords

Antiarrhythmic; Local anesthetic; Methanethiosulfonate; Patch clamp; SkM1

Indexed keywords

CYSTEINE; LIDOCAINE; PHENYLALANINE; SODIUM CHANNEL; SODIUM ION; THIOMESYLIC ACID METHYL ESTER; TRIMETHYLAMMONIUM SALT DERIVATIVE;

AMINO ACID SUBSTITUTION; ANESTHESIA MECHANISM; ANIMAL CELL; ARTICLE; CELL MEMBRANE DEPOLARIZATION; CHANNEL GATING; CONTROLLED STUDY; HYPERPOLARIZATION; LOCAL ANESTHESIA; NONHUMAN; OOCYTE; RAT; SKELETAL MUSCLE; SODIUM CURRENT; XENOPUS LAEVIS;

ANESTHETICS, LOCAL; ANIMALS; ELECTRIC STIMULATION; ELECTROPHYSIOLOGY; ION CHANNEL GATING; LIDOCAINE; MEMBRANE POTENTIALS; MUSCLE, SKELETAL; OOCYTES; PATCH-CLAMP TECHNIQUES; RATS; SODIUM CHANNEL BLOCKERS; SODIUM CHANNELS; XENOPUS;

EID: 0032890559     PISSN: 00221295     EISSN: None     Source Type: Journal    
DOI: 10.1085/jgp.113.1.7     Document Type: Article

References (25)

1. Balser, J.R., H.B. Nuss, D.W. Orias, D.C. Johns, E. Marban, G.F. Tomaselli, and J.H. Lawrence. 1996. Local anesthetics as effectors of allosteric gating. Lidocaine effects on inactivation-deficient rat skeletal muscle sodium channels. J. Clin. Invest. 98:2874-2886.
2. Bean, B.P., C.J. Cohen, and R.W. Tsien. 1983. Lidocaine block of cardiac sodium channels. J. Gen. Physiol. 81:613-642.
3. + channels. Modification of block by alterations in the alpha-subunit III-IV interdomain. Circ. Res. 77:584-592.
4. Butterworth, J.F., and G.R. Strichartz. 1990. Molecular mechanisms of local anesthesia: a review. Anesthesiology. 72:711-734.
5. Cahalan, M.D. 1978. Local anesthetic block of sodium channels in normal and pronase-treated squid giant axons. Biophys. J. 23: 285-311.
6. 1 subunit: a deletion analysis. Pflügers Arch. 431: 186-195.
7. Hanck, D.A., C. Makielski, and M.F. Sheets. 1994. Kinetic effects of quaternary lidocaine block of cardiac sodium channels: a gating current study. J. Gen. Physiol. 103:19-43.
8. Hille, B. 1978. Local anesthetic action on inactivation of the Na channel in nerve and skeletal muscle. In Biophysical Aspects of Cardiac Muscle. M. Morad, editor. Academic Press, Inc., New York. 55-74.
9. Hille, B. 1977. Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reaction. J. Gen. Physiol. 69:497-515.
10. Hondeghem, L.M., and B.G. Katzung. 1977. Time and voltage dependent interaction of antiarryhthmic drugs with cardiac sodium channels. Biochim. Biophys. Acta. 472:397-398.
11. Josephson, I.R., and Y. Chi. 1994. Voltage- and concentration-dependent effects of lidocaine on cardiac Na channel and Ca channel gating charge movements. Pflügers Arch. 428:485-491.
12. + channel inactivation gate during inactivation. J. Biol. Chem. 271:30971-30979.
13. Kuo, C., and B.P. Bean. 1994. Sodium channels must deactivate to recover from inactivation. Neuron. 12:819-829.
14. + channel. Neuron. 19: 175-184.
15. Nuss, H.B., G.F. Tomaselli, and E. Marban. 1995. Cardiac sodium channels (hH1) are intrinsically more sensitive to block by lidocaine than are skeletal muscle (μ1) channels. J. Gen. Physiol. 106:1193-1209.
16. + channels by local anesthetics. Science. 265:1724-1728.
17. Shepley, M.P., G.R. Strichartz, and G.K. Wang. 1983. Local anaesthetics block non-inactivating sodium channels in a use-dependent manner in amphibian myelinated axons. J. Physiol. (Lond.). 341:62P.
18. Strichartz, G., and G.K. Wang. 1986. The kinetic basis for phasic local anesthetic blockade of neuronal sodium channels. In Molecular and Cellular Mechanisms of Anesthetics. S.H. Roth and K.W. Miller, editors. Plenum Publishing Corp., New York. 217-225.
19. Strichartz, G.R. 1973. The inhibition of sodium currents in myelinated nerve by quaternary derivatives of lidocaine. J. Gen. Physiol. 62:37-57.
20. + channels. J. Gen. Physiol. 111:83-93.
21. Wang, G.K., M.S. Brodwick, D.C. Eaton, and G.R. Strichartz. 1987. Inhibition of sodium currents by local anesthetics in chloramine-T-treated squid axons. The role of channel activation. J. Gen. Physiol. 89:645-667.
22. +-channel inactivation. Proc. Natl. Acad. Sci. USA. 89:10910-10914.
23. Wright, S.N., S. Wang, R.G. Kallen, and G.K. Wang. 1997. Differences in steady-state inactivation between Na channel isoforms affect local anesthetic binding affinity. Biophys. J. 73:779-788.
24. Yeh, J.Z. 1978. Sodium inactivation mechanism modulates QX-314 block of sodium channels in squid axons. Biophys. J. 24:569-574.
25. Yeh, J.Z., and J. Tanguy. 1985. Na channel activation gate modulates slow recovery from use-dependent block by local anesthetics in squid giant axons. Biophys. J. 47:685-694.