Local anesthetic anchoring to cardiac sodium channels: Implications into tissue-selective drug targeting

Circulation Research

Volumn 85, Issue 1, 1999, Pages 88-98

  Li, Ronald A ^a   Tsushima, Robert G ^a   Himmeldirk, Klaus ^b   Dime, David S ^b   Backx, Peter H ^a,c  

^a UNIVERSITY HEALTH NETWORK   (Canada)

^b Toronto Research Chemicals Inc   (Canada)

^c TORONTO GENERAL HOSPITAL   (Canada)

Author keywords

Cardiac; Drug targeting; Local anesthetic; Methanethiosulfonate; Na+ channel

Indexed keywords

BENZOCAINE; CYSTEINE; DITHIOTHREITOL; LIDOCAINE; LOCAL ANESTHETIC AGENT; POLYETHYLENE; SODIUM CHANNEL; SULFONIC ACID DERIVATIVE;

ANIMAL CELL; ARTICLE; DISULFIDE BOND; DRUG ACTIVITY; DRUG BINDING SITE; DRUG TARGETING; HUMAN; HUMAN CELL; MALE; NONHUMAN; PRIORITY JOURNAL; RAT;

EID: 0033538613     PISSN: 00097330     EISSN: None     Source Type: Journal    
DOI: 10.1161/01.RES.85.1.88     Document Type: Article

References (44)

1. Hille B. Mechanisms of block. In: Hille B, ed. Ionic Channels of Excitable Membranes. 2nd ed. Sunderland, Mass: Sinauer; 1992: 390-422.
2. Butterworth JF, Strichartz GR. Molecular mechanisms of local anesthetics: a review. Anesthesiology. 1990;72:711-734.
3. Hudson AJ, Ebers GC, Bulman DE. The skeletal muscle sodium and chloride channel diseases. Brain. 1995;118:547-563.
4. Kuck KH, Siebels J, Schneider MA. Therapeutic consequences of newer studies addressing the problem of myocardial ischemia and ventricular arrhythmias. Herz. 1995;20:213-218.
5. + channel blockade and to increases in heart rate: implications for gene-specific therapy. Circulation. 1995;92:3381-3386.
6. Shimizu W, Antzelevitch C. Sodium channel block with mexiletine is effective in reducing dispersion of repolarization and preventing torsade de pointes in LQT2 and LQT3 models of the long-QT syndrome. Circulation. 1997;96:2038-2047.
7. Hille B. Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reaction. J Gen Physiol. 1977;69:497-515.
8. Bean BP, Cohen CJ, Tsien RW. Lidocaine block of cardiac sodium channels. J Gen Physiol. 1983;81:613-642.
9. Nuss HB, Tomaselli GF, Marbán E. Cardiac sodium channels (hH1) are intrinsically more sensitive to block by lidocaine than are skeletal muscle (μ1) channels. J Gen Physiol. 1995;106:1193-1209.
10. + channel subtypes. Biophys J. 1996;70:1700-1708.
11. Wright SN, Wang S-Y, Kallen RG, Wang GK. Differences in steady-state inactivation between Na channel isoforms affect local anesthetic binding affinity. Biophys J. 1997;73:779-788.
12. + channels by local anesthetics. Science. 1994;265:1724-1728.
13. Noda M, Ikeda T, Kayano T, Suzuki H, Takeshima H, Kurasaki M, Takahashi H, Numa S. Existence of distinct sodium channel messenger RNAs in rat brain. Nature. 1986;320:188-192.
14. + channel isoform. Proc Natl Acad Sci U S A. 1989;86:8170-8174.
15. Trimmer J S, Cooperman SS, Tomiko SA, Zhou J, Crean SM, Boyle MB, Kallen RG, Sheng Z, Barchi RL, Sigworth FJ, Goodman RH, Agnew WS, Mandel G. Primary structure and functional expression of a mammalian skeletal muscle sodium channel. Neuron. 1989;3:33-49.
16. Akopian AN, Sivilotti L, Wood JN. A tetrodotoxin-resistant voltage-gated sodium channel expressed by sensory neurons. Nature. 1996;37:257-262.
17. + channels. Soc Gen Physiol Ser. 1995;50:1-16.
18. + channel by a quaternary ammonium ion: catalysis by a transition-intermediate state. J Physiol. 1993;471:319-341.
19. Backx PH, Yue DT, Lawrence JH, Marbán E, Tomaselli GF. Molecular localization of an ion-binding site within the pore of mammalian sodium channels. Science. 1992;257:248-251.
20. + channel revealed by cysteine mutagenesis. Neuron. 1996;16:1037-1047.
21. Kirsch GE, Alam M, Hartmann HA. Differential effects of sulfhydryl reagents on saxitoxin and tetrodotoxin block of voltage-dependent Na channels. Biophys J. 1994;67:2305-2315.
22. Kunkel TA. Rapid and efficient site-specific mutagenesis without phenotypic selection. Proc Natl Acad Sci U S A. 1985;82:488-492.
23. Sanger F, Nicklen S, Coulson AR. DNA sequencing with chain-terminating inhibitors. Proc Natl Acad Sci U S A. 1977;74:5463-5467.
24. Gellens ME, George AL Jr, Chen L, Chahine M, Horn R, Barchi RL, Kallen RG. Primary structure and functional expression of the human cardiac tetrodotoxin-insensitive voltage-dependent sodium channel. Proc Natl Acad Sci U S A. 1992;89:554-558.
25. 1-subunit of the rat brain sodium channel. Science. 1992;256:839-842.
26. 1 subunit in rat skeletal muscle is selectively associated with the tetrodotoxin-sensitive α subunit isoform. Neuron. 1993;11:915-922.
27. + channel gene expression in rat ventricle. J Physiol. 1997;507:271-286.
28. Hamill OP, Marty A, Neher E, Sakmann B, Sigworth FJ. Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches. Pflügers Arch. 1981;391:85-100.
29. Zar JH. Biostatistical Analysis. Upper Saddle River, NJ: Prentice Hall; 1996.
30. + channel pores revealed by single-and double-cysteine replacements. J Gen Physiol. 1997;110:59-72.
31. + channels containing the equine hyperkalemic periodic paralysis mutation. Am J Physiol. 1998;275:C389-C400.
32. + currents by benzocaine homologs. Biophys J. 1996;70:194-201.
33. Schmidtmayer J, Ulbricht W. Interaction of lidocaine and benzocaine in blocking sodium channels. Pflügers Arch. 1980;387:47-54.
34. + channels. Proc Natl Acad Sci U S A. 1996;93: 9270-9275.
35. + channels. Pflügers Arch. 1998;435:293-302.
36. Elliott JR, Haydon DA, Hendry BM. Local anaesthetic effects of benzene and structurally related molecules, including benzocaine, on the squid giant axon. Pflügers Arch. 1987;409:589-595.
37. Zamponi GW, French RJ, Dissecting lidocaine action: diethylamide and phenol mimic separate modes of lidocaine block of sodium channels from heart and skeletal muscle. Biophys J. 1993;65:2335-2347.
38. Sunami A, Dudley SC Jr, Fozzard HA. Sodium channel selectivity filter regulates antiarrhythmic drug binding. Proc Natl Acad Sci U S A. 1997; 94:14126-14131.
39. + channels is critical for lidocaine binding. Circulation. 1998;98(suppl I):I-467.
40. + channel. Science. 1991;251:939-942.
41. + conduction and selectivity. Science. 1998;280: 69-77.
42. Bokesch PM, Post C, Strichartz G. Structure-activity relationship of lidocaine homologs producing tonic and frequency-dependent impulse blockade in nerve. J Pharmacol Exp Ther. 1986;237:773-781.
43. Ehring GR, Moyer JW, Hondeghem LM. Quantitative structure activity studies of antiarrhythmic properties in a series of lidocaine and procainamide derivatives. J Pharmacol Exp Ther. 1988;244:479-492.
44. Sheldon RS, Hill RJ, Taouis M, Wilson LM. Aminoalkyl structural requirements for interaction of lidocaine with the class 1 antiarrhythmic drug receptor on rat cardiac myocytes. Mol Pharmacol. 1991;39: 609-614.