Atomic determinants of state-dependent block of sodium channels by charged local anesthetics and benzocaine

FEBS Letters

Volumn 580, Issue 26, 2006, Pages 6027-6032

  Tikhonov, Denis B ^a   Bruhova, Iva ^a   Zhorov, Boris S ^a  

^a MCMASTER UNIVERSITY   (Canada)

Author keywords

Channel block; Homology modeling; Ion permeation; Lidocaine; Monte Carlo minimization; QX 314; Slow inactivation

Indexed keywords

AMMONIUM DERIVATIVE; BENZOCAINE; LIDOCAINE; LOCAL ANESTHETIC AGENT; SODIUM CHANNEL; SODIUM ION;

ARTICLE; CHELATION; DRUG BINDING; MOLECULAR MODEL; NONHUMAN; PRIORITY JOURNAL; SODIUM DEPLETION;

ANESTHETICS, LOCAL; BENZOCAINE; BINDING SITES; HUMANS; LIDOCAINE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; MUSCLE PROTEINS; PROTEIN CONFORMATION; SODIUM; SODIUM CHANNELS;

EID: 33750532138     PISSN: 00145793     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.febslet.2006.10.035     Document Type: Article

References (28)

1. Nau C., and Wang G.K. Interactions of local anesthetics with voltage-gated Na+ channels. J. Membr. Biol. 201 (2004) 1-8
2. Fozzard H.A., Lee P.J., and Lipkind G.M. Mechanism of local anesthetic drug action on voltage-gated sodium channels. Curr. Pharm. Des. 11 (2005) 2671-2686
3. Hille B. Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reaction. J. Gen. Physiol. 69 (1977) 497-515
4. Wang S.Y., Barile M., and Wang G.K. Disparate role of Na(+) channel D2-S6 residues in batrachotoxin and local anesthetic action. Mol. Pharmacol 59 (2001) 1100-1107
5. Yarov-Yarovoy V., McPhee J.C., Idsvoog D., Pate C., Scheuer T., and Catterall W.A. Role of amino acid residues in transmembrane segments IS6 and IIS6 of the Na+ channel alpha subunit in voltage-dependent gating and drug block. J. Biol. Chem. 277 (2002) 35393-35401
6. Li H.L., Galue A., Meadows L., and Ragsdale D.S. A molecular basis for the different local anesthetic affinities of resting versus open and inactivated states of the sodium channel. Mol. Pharmacol. 55 (1999) 134-141
7. Wang G.K., Quan C., and Wang S. A common local anesthetic receptor for benzocaine and etidocaine in voltage-gated mu1 Na+ channels. Pflugers Arch. 435 (1998) 293-302
8. + currents by benzocaine homologs. Biophys. J. 70 (1996) 94-201
9. Meeder T., and Ulbricht W. Action of benzocaine on sodium channels of frog nodes of Ranvier treated with chloramine-T. Pflugers Arch. 409 (1987) 265-273
10. + channel. Nature 423 (2003) 33-41
11. Doyle D.A., Morais Cabral J., Pfuetzner R.A., Kuo A., Gulbis J.M., Cohen S.L., Chait B.T., and MacKinnon R. The structure of the potassium channel: molecular basis of K+ conduction and selectivity. Science 280 (1998) 69-77
12. Zhorov B.S., and Tikhonov D.B. Potassium, sodium, calcium and glutamate-gated channels: pore architecture and ligand action. J. Neurochem. 88 (2004) 782-799
13. Tikhonov D.B., and Zhorov B.S. Modeling P-loops domain of sodium channel: homology with potassium channels and interaction with ligands. Biophys. J. 88 (2005) 184-197
14. + channel-Fab complex at 2.0 A resolution. Nature 414 (2001) 43-48
15. + channels by local anesthetics. Science 265 (1994) 1724-1728
16. Lipkind G.M., and Fozzard H.A. Molecular modeling of local anesthetic drug binding by voltage-gated sodium channels. Mol. Pharmacol. 68 (2005) 1611-1622
17. + channel. Proc. Natl. Acad. Sci. USA 92 (1995) 11839-11843
18. Sunami A., Glaaser I.W., and Fozzard H.A. Structural and gating changes of the sodium channel induced by mutation of a residue in the upper third of IVS6, creating an external access path for local anesthetics. Mol. Pharmacol. 59 (2001) 684-691
19. Lee P.J., Sunami A., and Fozzard H.A. Cardiac-specific external paths for lidocaine, defined by isoform-specific residues, accelerate recovery from use-dependent block. Circ. Res. 89 (2001) 1014-1021
20. + selectivity filter: charge balance and coupling of ion binding to a protein conformational change underlie high conduction rates. J. Mol. Biol. 333 (2003) 965-975
21. Grissmer S., and Cahalan M. TEA prevents inactivation while blocking open K+ channels in human T lymphocytes. Biophys. J. 55 (1989) 203-206
22. + channels. Proc. Natl. Acad. Sci. USA 88 (1991) 5092-5095
23. Lenaeus M.J., Vamvouka M., Focia P.J., and Gross A. Structural basis of TEA blockade in a model potassium channel. Nat. Struct. Mol. Biol. 12 (2005) 454-459
24. Berneche S., and Roux B. A gate in the selectivity filter of potassium channels. Structure 13 (2005) 591-600
25. Elliott J.R., Haydon D.A., and Hendry B.M. The mechanisms of sodium current inhibition by benzocaine in the squid giant axon. Pflugers Arch. 409 (1987) 596-600
26. Tikhonov D.B., and Zhorov B.S. Sodium channel activators: model of binding inside the pore and a possible mechanism of action. FEBS Lett. 579 (2005) 4207-4212
27. Wang S.Y., Mitchell J., Tikhonov D.B., Zhorov B.S., and Wang G.K. How batrachotoxin modifies the sodium channel permeation pathway: computer modeling and site-directed mutagenesis. Mol. Pharmacol. 69 (2006) 788-795
28. Brock M.W., Mathes C., and Gilly W.F. Selective open-channel block of Shaker (Kv1) potassium channels by s-nitrosodithiothreitol (SNDTT). J. Gen. Physiol. 118 (2001) 113-134