The sodium channel as a target for local anesthetic drugs

Frontiers in Pharmacology

Volumn 2 NOV, Issue , 2011, Pages

  Fozzard, Harry A ^a   Sheets, Michael F ^b   Hanck, Dorothy A ^a  

^a UNIVERSITY OF CHICAGO   (United States)

^b UNIVERSITY OF UTAH SCHOOL OF MEDICINE   (United States)

Author keywords

Gating currents; Lidocaine; Local anesthetics; Molecular modeling; Na channel

Indexed keywords

ALANINE; ANALGESIC AGENT; ANTICONVULSIVE AGENT; ASPARAGINE; BENZOCAINE; ETIDOCAINE; FLECAINIDE; ISOLEUCINE; LEUCINE; LIDOCAINE; LIDOCAINE ETHOBROMIDE; LOCAL ANESTHETIC AGENT; PHENYLALANINE; POTASSIUM CHANNEL; SODIUM CHANNEL; SODIUM CHANNEL NAV1.2; SODIUM CHANNEL NAV1.4; SODIUM CHANNEL NAV1.5; SODIUM CHANNEL NAVAB; TYROSINE; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ANALGESIC ACTIVITY; ANTIARRHYTHMIC ACTIVITY; ARTICLE; BINDING AFFINITY; BINDING SITE; CHANNEL GATING; CRYSTAL STRUCTURE; DRUG PENETRATION; DRUG PROTEIN BINDING; DRUG SENSITIVITY; DRUG SPECIFICITY; DRUG TARGETING; HEART ARRHYTHMIA; HUMAN; MOLECULAR DOCKING; NERVE BLOCK; NERVE CELL MEMBRANE STEADY POTENTIAL; NONHUMAN; POINT MUTATION; PROTEIN CONFORMATION; PROTEIN DOMAIN; PROTEIN STRUCTURE; PROTEIN TARGETING; UNSPECIFIED SIDE EFFECT;

EID: 84862555263     PISSN: None     EISSN: 16639812     Source Type: Journal    
DOI: 10.3389/fphar.2011.00068     Document Type: Article

References (40)

1. Ahern, C. A., Eastwood, A. L., Dougherty, D. A., and Horn, R. (2008). Electrostatic contributions of aromatic residues in the local anesthetic receptor of voltage-gated sodium channels. Circ. Res. 102, 86-94.
2. Alpert, L. A., Fozzard, H. A., Hanck, D. A., and Makielski, J. C. (1989). Is there a second external lidocaine binding site on mammalian cardiac cells? Am. J. Physiol. 257, H79-H84.
3. Arcisio-Miranda, M., Muroi, Y., Chowdhury, S., and Chanda, B. (2010). Molecular mechanism of allosteric modification of voltagedependent sodium channels by local anesthetics. J. Gen. Physiol. 136, 541-554.
4. Bennett, P. B., Valenzuela, C., Chen, L.-Q., and Kallen, R. G. (1995). On the molecular nature of the lidocaine receptor of cardiac Na channels: modification of block by alterations in α-subunit IIIIV interdomain. Circ. Res. 7, 584-592.
5. Bezanilla, F. (2000). The voltage sensor in voltage dependent ion channels. Physiol. Rev. 80, 555-592.
6. Bruhova, I., Tikhonov, D. B., and Zhorov, B. S. (2008). Access and binding of local anesthetics in the closed sodium channel. Mol. Pharmacol. 74, 1033-1045.
7. Catterall, W. A. (2000). From ionic currents to molecular mechanisms: the structure and function of voltagegated sodium channels. Neuron 26, 13-25.
8. Chahine, M., George, A. L. Jr., Zhou, M., Ji, S., Sun, W., Barchi, R. L., and Horn, R. (1994). Sodium channel mutations in paramyotonia congenital uncouple inactivation from activation. Neuron 12, 281-294.
9. Doyle, D. A., Cabral, J. M., Pfuetzner, R. A., Kuo, A., Gulbis, J. M., Cohen, S. L., Chait, B. T., and MacKinnon, R. (1998). The structure of the potassium channel: molecular basis of K conduction and selectivity. Science 280, 69-77.
10. Grant, A. O., Deitz, M. A., Gilliam, F. R. III, and Starmer, C. F. (1989). Blockade of cardiac sodium channels by lidocaine. Circ. Res. 65, 1247-1262.
11. Guy, H. R., and Seetharamulu, P. (1986). Molecular model of the action potential sodium channel. Proc. Natl. Acad. Sci. U.S.A. 83, 508-512.
12. Hanck, D. A., Makielski, J. C., and Sheets, M. F. (1994). Kinetic effects of quaternary lidocaineblock of cardiac sodium currents: a gating current study. J. Gen. Physiol. 103, 19-43.
13. Hanck, D. A., Nikitina, E., McNulty, M. M., Fozzard, H. A., Lipkind, G. M., and Sheets, M. F. (2009). Using lidocaine and benzocaine to link sodium channel molecular configurations to state-dependent antiarrhythmic drug affinity. Circ. Res. 105, 492-499.
14. Hille, B. (1977). Local anesthetics: hydrophylic and hydrophobic pathways for the drug-receptor reaction. J. Gen. Physiol. 69, 497-515.
15. Hille, B. (2001). Ion Channels in Excitable Membranes. Sunderland, MA: Sinauer Associates, Inc.
16. Jiang, Y., Lee, A., Chen, J., Cadene, M., Chait, B. T., and MacKinnon, R. (2002). The open pore conformation of potassium channels. Nature 417, 523-526.
17. Lee, P. J., Sunami, A., and Fozzard, H. A. (2001). Cardiac-specific external paths for lidocaine, defined by isoform-specific residues, accelerate recovery from use-dependent block. Circ. Res. 89, 1014-1021.
18. Li, H. L., Galue, A., Meadows, L., and Ragsdale, D. S. (1999). A molecular basis for the different local anesthetic affinities of resting versus open and inactivated states of the sodium channel. Mol. Pharmacol. 55, 134-141.
19. Lipkind, G. M., and Fozzard, H. A. (2005). Molecular modeling of local anesthetic drug binding by voltagegated sodium channels. Mol. Pharmacol. 68, 1611-1622.
20. Liu, H., Atkins, J., and Kass, R. S. (2003). Common molecular determinants of flecainide and lidocaine block of heart Na channels: evidence from experiments with neutral and quaternary flecainide analogs. J. Gen. Physiol. 121, 199-214.
21. Long, S. B., Campbell, E. B., and MacKinnon, R. (2005). Crystal structure of a mammalian voltage-dependent Shaker family K channel. Science 309, 897-903.
22. McNulty, M. M., Edgerton, G. B., Shah, R. D., Hanck, D. A., Fozzard, H. A., and Lipkind, G. M. (2007). Charge at the lidocaine binding site residue Phe-1759 affects permeation in human cardiac voltagegated sodium channels. J. Physiol. (Lond.) 581, 741-755.
23. Muroi, Y., and Chanda, B. (2008). Local anesthetics disrupt energetic coupling between the voltage-sensing segments of a sodium channel. J. Gen. Physiol. 133, 1-15.
24. Narahashi, T., and Frasier, D. T. (1971). Site of action and active form of local anesthetics. Neurosci. Res. 4, 65-99.
25. Ong, B. H., Tomaselli, G. F., and Balser, J. R. (2000). A structural rearrangement in the sodium channel pore linked to slow inactivation and use dependence. J. Gen. Physiol. 116, 653-662.
26. Patino, G. A., and Isom, L. L. (2010). Electrophysiology and beyond: multiple roles of Na channel β subunits in development and disease. Neurosci. Lett. 486, 53-59.
27. Patton, D. E., West, J. W., Catterall, W. A., and Goldin, A. L. (1992). Amino acid residues required for fast sodium channel inactivation. Proc. Natl. Acad. Sci. USA 89, 10905-10909.
28. Payandeh, J., Scheuer, T., Zheng, N., and Catterall, W. A. (2011). The crystal structure of a voltagegated sodium channel. Nature 475, 353-358.
29. Qu, Y., Rogers, J., Tanada, T., Scheuer, T., and Catterall, W. A. (1995). Molecular determinants of drug access to the receptor site for antiarrhythmic drugs in the cardiac Na channel. Proc. Natl. Acad. Sci. U.S.A. 92, 11839-11843.
30. Ragsdale, D. S., McPhee, J. C., Scheuer, T., and Catterall, W. A. (1994). Molecular determinants of statedependent block of Na channels by local anesthetics. Science 265, 1724-1728.
31. Sheets, M. F., Fozzard, H. A., Lipkind, G. M., and Hanck, D. A. (2010). Sodium channel molecular conformations and antiarrhythmic drug affinity. Trends Cardiovasc. Med. 20, 16-21.
32. Sheets, M. F., and Hanck, D. A. (2003). Molecular action of lidocaine on the voltage sensors of sodium channels. J. Gen. Physiol. 121, 163-175.
33. Sheets, M. F., and Hanck, D. A. (2007). Outward stabilization of the S4 segments in domains III and IV enhances lidocaine block of sodium channels. J. Physiol. (Lond.) 582, 317-334.
34. Sheets, M. F., Kyle, J. W., Kallen, R. G., and Hanck, D. A. (1999). The Na channel voltage sensor associated with inactivation is localized to the external charged residues of domain IV, S4. Biophys. J. 77, 747-757.
35. Strichartz, G. R. (1973). The inhibition of sodium currents in myelinated nerve by quaternary derivatives of lidocaine. J. Gen. Physiol. 62, 37-57.
36. Sunami, A., Dudley, S. C. Jr., and Fozzard, H. A. (1997). Sodium channel selectivity filter regulates antiarrhythmic drug binding. Proc. Natl. Acad. Sci. U.S.A. 94, 14126-14131.
37. Vedantham, V., and Cannon, S. C. (1999). The position of the fast-inactivation gate during lidocaine block of voltage-gated Na channels. J. Gen. Physiol. 113, 7-16.
38. Wang, S.-Y., Mitchell, J., Moczydlowski, E., and Wang, G. K. (2004). Block of inactivation-deficient Na channels by local anesthetics in stably transfected mammalian cells: evidence for drug binding along the activation pathway. J. Gen. Physiol. 124, 691-701.
39. Yarov-Yarovoy, V., McPhee, J. C., Idavoog, D., Pate, C., Scheuer, T., and Catterall, W. A. (2002). Role of amino acid residues in transmembrane segments IS6 and IIS6 of the Na channel α-subunit in voltage-dependent gating and drug block. J. Biol. Chem. 277, 35393-35401.
40. Zamponi, G. W., Doyle, D. D., and French, R. J. (1993). Fast lidocaine block of cardiac and skeletal muscle sodium channels: one site with two routes of access. Biophys. J. 65, 80-90.