Targeting voltage-gated sodium channels for treating neuropathic and inflammatory pain

Current Pharmaceutical Biotechnology

Volumn 12, Issue 10, 2011, Pages 1715-1719

  Cohen, Charles J ^a  

^a Xenon Pharmaceuticals   (Canada)

Author keywords

Analgesia; Nav; Pain; Voltage gated sodium channel

Indexed keywords

CARBAMAZEPINE; CDA 54; LAMOTRIGINE; LIDOCAINE; MEXILETINE; PHENYTOIN; SODIUM CHANNEL BLOCKING AGENT; SODIUM CHANNEL NAV1.3; SODIUM CHANNEL NAV1.7; SODIUM CHANNEL NAV1.8; SODIUM CHANNEL NAV1.9; UNCLASSIFIED DRUG; VOLTAGE GATED SODIUM CHANNEL; VOLTAGE GATED SODIUM CHANNEL BLOCKER;

ALLODYNIA; ANALGESIC ACTIVITY; CENTRAL NERVOUS SYSTEM; DIZZINESS; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG POTENCY; DRUG TARGETING; ELECTRIC ACTIVITY; HUMAN; HYPERALGESIA; INFLAMMATION; INFLAMMATORY PAIN; NAUSEA; NEUROPATHIC PAIN; NONHUMAN; PAIN; PERIPHERAL NERVOUS SYSTEM; RECEPTOR OCCUPANCY; REVIEW; SENSITIZATION; SOMNOLENCE;

EID: 80053493423     PISSN: 13892010     EISSN: 18734316     Source Type: Journal    
DOI: 10.2174/138920111798357249     Document Type: Review

References (52)

1. Hahnenkamp, K.; Durieux, M. E.; Hahnenkamp, A.; Schauerte, S. K.; Hoenemann, C. W.; Vegh, V.; Theilmeier, G.; Hollmann, M. W. Local anaesthetics inhibit signalling of human NMDA receptors recombinantly expressed in Xenopus laevis oocytes: role of protein kinase C. Br. J. Anaesth., 2006, 96 (1), 77-87.
2. Hollmann, M. W.; Durieux, M. E.; Graf, B. M. Novel local anaesthetics and novel indications for local anaesthetics. Curr. Opin. Anaesthesiol., 2001, 14 (6), 741-749.
3. Leffler, A.; Fischer, M. J.; Rehner, D.; Kienel, S.; Kistner, K.; Sauer, S. K.; Gavva, N. R.; Reeh, P. W.; Nau, C. The vanilloid receptor TRPV1 is activated and sensitized by local anesthetics in rodent sensory neurons. J. Clin. Invest., 2008, 118 (2), 763-776.
4. Chiang, N.; Schwab, J. M.; Fredman, G.; Kasuga, K.; Gelman, S.; Serhan, C. N. Anesthetics impact the resolution of inflammation. PLoS One, 2008, 3 (4), e1879.
5. de Klaver, M. J.; Buckingham, M. G.; Rich, G. F. Lidocaine attenuates cytokineinduced cell injury in endothelial and vascular smooth muscle cells. Anesth. Analg., 2003, 97 (2), 465-470.
6. Gallos, G.; Jones, D. R.; Nasr, S. H.; Emala, C. W.; Lee, H. T. Local anesthetics reduce mortality and protect against renal and hepatic dysfunction in murine septic peritonitis. Anesthesiology, 2004, 101 (4), 902-911.
7. Strichartz, G. R. Novel ideas of local anaesthetic actions on various ion channels to ameliorate postoperative pain. Br. J. Anaesth., 2008, 101(1), 45-47.
8. Xiao, W. H.; Bennett, G. J. C-fiber spontaneous discharge evoked by chronic inflammation is suppressed by a long-term infusion of lidocaine yielding nanogram per milliliter plasma levels. Pain, 2008, 137 (1), 218-228.
9. Whiteside, G. T.; Adedoyin, A.; Leventhal, L. Predictive validity of animal pain models? A comparison of the pharmacokineticpharmacodynamic relationship for pain drugs in rats and humans. Neuropharmacology, 2008, 54 (5), 767-775.
10. Wallace, M. S.; Dyck, J. B.; Rossi, S. S.; Yaksh, T. L. Computercontrolled lidocaine infusion for the evaluation of neuropathic pain after peripheral nerve injury. Pain, 1996, 66 (1), 69-77.
11. Abram, S. E.; Yaksh, T. L. Systemic lidocaine blocks nerve injury-induced hyperalgesia and nociceptor-driven spinal sensitization in the rat. Anesthesiology, 1994, 80 (2), 383-391.
12. Chaplan, S. R.; Bach, F. W.; Shafer, S. L.; Yaksh, T. L. Prolonged alleviation of tactile allodynia by intravenous lidocaine in neuropathic rats. Anesthesiology, 1995, 83 (4), 775-785.
13. Sinnott, C. J.; Garfield, J. M.; Strichartz, G. R. Differential efficacy of intravenous lidocaine in alleviating ipsilateral versus contralateral neuropathic pain in the rat. Pain, 1999, 80 (3), 521-531.
14. Bean, B. P.; Cohen, C. J.; Tsien, R. W. Lidocaine block of cardiac sodium channels. J. Gen. Physiol., 1983, 81 (5), 613-642.
15. Hille, B. Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reaction. J. Gen. Physiol., 1977, 69 (4), 497-515.
16. Felix, J. P.; Williams, B. S.; Priest, B. T.; Brochu, R. M.; Dick, I. E.; Warren, V. A.; Yan, L.; Slaughter, R. S.; Kaczorowski, G. J.; Smith, M. M.; Garcia, M. L. Functional assay of voltage-gated sodium channels using membrane potential-sensitive dyes. Assay Drug Dev. Technol., 2004, 2 (3), 260-268.
17. Mao, J.; Chen, L. L. Systemic lidocaine for neuropathic pain relief. Pain, 2000, 87 (1), 7-17.
18. Pieper, J. A.; Slaughter, R. L.; Anderson, G. D.; Wyman, M. G.; Lalka, D. Lidocaine clinical pharmacokinetics. Drug Intell. Clin. Pharm., 1982, 16 (4), 291-294.
19. Ilyin, V. I.; Hodges, D. D.; Whittemore, E. R.; Carter, R. B.; Cai, S. X.; Woodward, R. M. V102862 (Co 102862): a potent, broad-spectrum state-dependent blocker of mammalian voltagegated sodium channels. Br. J. Pharmacol., 2005, 144 (6), 801-812.
20. Kuo, C. C.; Bean, B. P. Slow binding of phenytoin to inactivated sodium channels in rat hippocampal neurons. Mol. Pharmacol., 1994, 46 (4), 716-725
21. Ogutu, B. R.; Newton, C. R.; Muchohi, S. N.; Otieno, G. O.; Edwards, G.; Watkins, W. M.; Kokwaro, G. O. Pharmacokinetics and clinical effects of phenytoin and fosphenytoin in children with severe malaria and status epilepticus. Br. J. Clin. Pharmacol., 2003, 56 (1), 112-119.
22. Hirsch, L. J.; Weintraub, D.; Du, Y.; Buchsbaum, R.; Spencer, H. T.; Hager, M.; Straka, T.; Bazil, C. W.; Adams, D. J.; Resor, S. R. Jr.; Morrell, M. J. Correlating lamotrigine serum concentrations with tolerability in patients with epilepsy. Neurology, 2004, 63 (6), 1022-1026.
23. Kuo, C. C.; Lu, L. Characterization of lamotrigine inhibition of Na+ channels in rat hippocampal neurones. Br. J. Pharmacol., 1997, 121 (6), 1231-1238.
24. Kuo, C. C.; Chen, R. S.; Lu, L.; Chen, R. C. Carbamazepine inhibition of neuronal Na+ currents: quantitative distinction from phenytoin and possible therapeutic implications. Mol. Pharmacol., 1997, 51 (6), 1077-1083.
25. Tomson, T.; Tybring, G.; Bertilsson, L.; Ekbom, K.; Rane, A. Carbamazepine therapy in trigeminal neuralgia: clinical effects in relation to plasma concentration. Arch. Neurol., 1980, 37 (11), 699-703.
26. McGowan, E.; Hoyt, S. B.; Li, X.; Lyons, K. A.; Abbadie, C. A peripherally acting Na(v)1.7 sodium channel blocker reverses hyperalgesia and allodynia on rat models of inflammatory and neuropathic pain. Anesth. Analg., 2009, 109 (3), 951-958.
27. Williams, B. S.; Felix, J. P.; Priest, B. T.; Brochu, R. M.; Dai, K.; Hoyt, S. B.; London, C.; Tang, Y. S.; Duffy, J. L.; Parsons, W. H.; Kaczorowski, G. J.; Garcia, M. L. Characterization of a new class of potent inhibitors of the voltage-gated sodium channel Nav1.7. Biochemistry, 2007, 46 (50), 14693-14703.
28. Brochu, R. M.; Dick, I. E.; Tarpley, J. W.; McGowan, E.; Gunner, D.; Herrington, J.; Shao, P. P.; Ok, D.; Li, C.; Parsons, W. H.; Stump, G. L.; Regan, C. P.; Lynch, J. J. Jr.; Lyons, K. A.; McManus, O. B.; Clark, S.; Ali, Z.; Kaczorowski, G. J.; Martin, W. J.; Priest, B. T. Block of peripheral nerve sodium channels selectively inhibits features of neuropathic pain in rats. Mol. Pharmacol., 2006, 69 (3), 823-832.
29. Devor, M.; Wall, P. D.; Catalan, N. Systemic lidocaine silences ectopic neuroma and DRG discharge without blocking nerve conduction. Pain, 1992, 48 (2), 261-268.
30. Dong, H.; Fan, Y. H.; Wang, Y. Y.; Wang, W. T.; Hu, S. J. Lidocaine suppresses subthreshold oscillations by inhibiting persistent Na(+) current in injured dorsal root ganglion neurons. Physiol. Res., 2008, 57 (4), 639-645.
31. Liu, X.; Zhou, J. L.; Chung, K.; Chung, J. M. Ion channels associated with the ectopic discharges generated after segmental spinal nerve injury in the rat. Brain Res., 2001, 900 (1), 119-127.
32. Xie, W.; Strong, J. A.; Zhang, J. M. Early blockade of injured primary sensory afferents reduces glial cell activation in two rat neuropathic pain models. Neuroscience, 2009, 160 (4), 847-857.
33. Wallace, M. S.; Magnuson, S.; Ridgeway, B. Efficacy of oral mexiletine for neuropathic pain with allodynia: a double-blind, placebo-controlled, crossover study. Reg. Anesth. Pain Med., 2000, 25 (5), 459-467.
34. Ragsdale, D. S. How do mutant Nav1.1 sodium channels cause epilepsy? Brain Res. Rev., 2008, 58 (1), 149-159.
35. Yu, F. H.; Mantegazza, M.; Westenbroek, R. E.; Robbins, C. A.; Kalume, F.; Burton, K. A.; Spain, W. J.; McKnight, G. S.; Scheuer, T.; Catterall, W. A. Reduced sodium current in GABAergic interneurons in a mouse model of severe myoclonic epilepsy in infancy. Nat. Neurosci., 2006, 9 (9), 1142-1149.
36. Raymond, C. K.; Castle, J.; Garrett-Engele, P.; Armour, C. D.; Kan, Z.; Tsinoremas, N.; Johnson, J. M. Expression of alternatively spliced sodium channel alpha-subunit genes. Unique splicing patterns are observed in dorsal root ganglia. J. Biol. Chem., 2004, 279 (44), 46234-46241.
37. Dib-Hajj, S. D.; Black, J. A.; Waxman, S. G. Voltage-gated sodium channels: therapeutic targets for pain. Pain Med., 2009, 10 (7), 1260-1269.
38. England, S. Voltage-gated sodium channels: the search for subtype-selective analgesics. Exp. Opin. Invest. Drugs, 2008, 17 (12), 1849-1864.
39. Priest, B. T. Future potential and status of selective sodium channel blockers for the treatment of pain. Curr. Opin. Drug Discov. Devel., 2009, 12 (5), 682-692.
40. Cox, J. J.; Reimann, F.; Nicholas, A. K.; Thornton, G.; Roberts, E.; Springell, K.; Karbani, G.; Jafri, H.; Mannan, J.; Raashid, Y.; Al-Gazali, L.; Hamamy, H.; Valente, E. M.; Gorman, S.; Williams, R.; McHale, D. P.; Wood, J. N.; Gribble, F. M.; Woods, C. G. An SCN9A channelopathy causes congenital inability to experience pain. Nature, 2006, 444 (7121), 894-898.
41. Goldberg, Y. P.; MacFarlane, J.; MacDonald, M. L.; Thompson, J.; Dube, M. P.; Mattice, M.; Fraser, R.; Young, C.; Hossain, S.; Pape, T.; Payne, B.; Radomski, C.; Donaldson, G.; Ives, E.; Cox, J.; Younghusband, H. B.; Green, R.; Duff, A.; Boltshauser, E.; Grinspan, G. A.; Dimon, J. H.; Sibley, B. G.; Andria, G.; Toscano, E.; Kerdraon, J.; Bowsher, D.; Pimstone, S. N.; Samuels, M. E.; Sherrington, R.; Hayden, M. R. Loss-of-function mutations in the Nav1.7 gene underlie congenital indifference to pain in multiple human populations. Clin. Genet., 2007, 71 (4), 311-319.
42. Estacion, M.; Harty, T. P.; Choi, J. S.; Tyrrell, L.; Dib-Hajj, S. D.; Waxman, S. G. A sodium channel gene SCN9A polymorphism that increases nociceptor excitability. Ann. Neurol., 2009, 66 (6), 862-866.
43. Reimann, F.; Cox, J. J.; Belfer, I.; Diatchenko, L.; Zaykin, D. V.; McHale, D. P.; Drenth, J. P.; Dai, F.; Wheeler, J.; Sanders, F.; Wood, L.; Wu, T. X.; Karppinen, J.; Nikolajsen, L.; Mannikko, M.; Max, M. B.; Kiselycznyk, C.; Poddar, M.; Te Morsche, R. H.; Smith, S.; Gibson, D.; Kelempisioti, A.; Maixner, W.; Gribble, F. M.; Woods, C. G. Pain perception is altered by a nucleotide polymorphism in SCN9A. Proc. Natl. Acad. Sci. USA, 2010, 107 (11), 5148-5153.
44. Singh, N. A.; Pappas, C.; Dahle, E. J.; Claes, L. R.; Pruess, T. H.; De Jonghe, P.; Thompson, J.; Dixon, M.; Gurnett, C.; Peiffer, A.; White, H. S.; Filloux, F.; Leppert, M. F. A role of SCN9A in human epilepsies, as a cause of febrile seizures and as a potential modifier of Dravet syndrome. PLoS Genet., 2009, 5 (9), e1000649.
45. Royer, A.; van Veen, T. A.; Le Bouter, S.; Marionneau, C.; Griol- Charhbili, V.; Leoni, A. L.; Steenman, M.; van Rijen, H. V.; Demolombe, S.; Goddard, C. A.; Richer, C.; Escoubet, B.; Jarry- Guichard, T.; Colledge, W. H.; Gros, D.; de Bakker, J. M.; Grace, A. A.; Escande, D.; Charpentier, F., Mouse model of SCN5Alinked hereditary Lenegre's disease: age-related conduction slowing and myocardial fibrosis. Circulation, 2005, 111 (14), 1738-1746.
46. Bezzina, C. R.; Shimizu, W.; Yang, P.; Koopmann, T. T.; Tanck, M. W.; Miyamoto, Y.; Kamakura, S.; Roden, D. M.; Wilde, A. A. Common sodium channel promoter haplotype in asian subjects underlies variability in cardiac conduction. Circulation, 2006, 113 (3), 338-344.
47. Meisler, M. H.; O'Brien, J. E.; Sharkey, L. M. The sodium channel gene family: epilepsy mutations, gene interactions and modifier effects. J. Physiol., 2010, 588(Pt 11),1841-1848
48. Akopian, A. N.; Souslova, V.; England, S.; Okuse, K.; Ogata, N.; Ure, J.; Smith, A.; Kerr, B. J.; McMahon, S. B.; Boyce, S.; Hill, R.; Stanfa, L. C.; Dickenson, A. H.; Wood, J. N. The tetrodotoxinresistant sodium channel SNS has a specialized function in pain pathways. Nat. Neurosci., 1999, 2 (6), 541-548.
49. Dong, X. W.; Goregoaker, S.; Engler, H.; Zhou, X.; Mark, L.; Crona, J.; Terry, R.; Hunter, J.; Priestley, T. Small interfering RNA-mediated selective knockdown of Na(V)1.8 tetrodotoxinresistant sodium channel reverses mechanical allodynia in neuropathic rats. Neuroscience, 2007, 146 (2), 812-821
50. Lai, J.; Gold, M. S.; Kim, C. S.; Bian, D.; Ossipov, M. H.; Hunter, J. C.; Porreca, F. Inhibition of neuropathic pain by decreased expression of the tetrodotoxin-resistant sodium channel, NaV1.8. Pain, 2002, 95 (1-2), 143-152.
51. Jarvis, M. F.; Honore, P.; Shieh, C. C.; Chapman, M.; Joshi, S.; Zhang, X. F.; Kort, M.; Carroll, W.; Marron, B.; Atkinson, R.; Thomas, J.; Liu, D.; Krambis, M.; Liu, Y.; McGaraughty, S.; Chu, K.; Roeloffs, R.; Zhong, C.; Mikusa, J. P.; Hernandez, G.; Gauvin, D.; Wade, C.; Zhu, C.; Pai, M.; Scanio, M.; Shi, L.; Drizin, I.; Gregg, R.; Matulenko, M.; Hakeem, A.; Gross, M.; Johnson, M.; Marsh, K.; Wagoner, P. K.; Sullivan, J. P.; Faltynek, C. R.; Krafte, D. S. A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc. Natl. Acad. Sci. USA, 2007, 104 (20), 8520-8525.
52. Kinloch, R. A.; Rees, H.; England, S.; Monhemius, R.; Suzuki, R.; Mace, H.; Jinks, J.; Ackley, M.; Lewis, M.; Speed, B.; Mahoney, J.; Harrison, W.; Bannon, A. In vivo characterization of two novel selective Nav1.8 modulators Soc. Neurosci. Abs., 2009, 359.355.