Sodium Channel Blockers for the Treatment of Neuropathic Pain

Neurotherapeutics

Volumn 6, Issue 4, 2009, Pages 663-678

  Bhattacharya, Anindya ^a   Wickenden, Alan D ^a   Chaplan, Sandra R ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

drug discovery; neuropathic pain; selectivity; Sodium channel; subtype

Indexed keywords

A 803467; A 803497; AMIDINE; AMITRIPTYLINE; CARBAMAZEPINE; DESIPRAMINE; DULOXETINE; HARKOSERIDE; LAMOTRIGINE; LIDOCAINE; MEXILETINE; OXCARBAZEPINE; PHENYTOIN; RALFINAMIDE; RILUZOLE; SODIUM CHANNEL BLOCKING AGENT; TETRODOTOXIN; UNCLASSIFIED DRUG; VOLTAGE GATED CALCIUM CHANNEL;

ARTICLE; COMPLEX REGIONAL PAIN SYNDROME; DIABETIC NEUROPATHY; DRUG EFFICACY; DRUG SAFETY; DRUG TOLERABILITY; HUMAN; NEUROPATHIC PAIN; POSTHERPETIC NEURALGIA; PRIORITY JOURNAL;

ANIMALS; DRUG DISCOVERY; HUMANS; NEURALGIA; PERIPHERAL NERVOUS SYSTEM DISEASES; SODIUM CHANNEL BLOCKERS; SODIUM CHANNELS;

EID: 70349335964     PISSN: 19337213     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.nurt.2009.08.001     Document Type: Article

References (208)

1. Mitchell S.W. Gunshot Wounds and Other Injuries of Nerves (1864), Lippincott, Philadelphia
2. Rivera M.A., Aufderheide A.C., Cartmell L.W., Torres C.M., and Langsjoen O. Antiquity of coca-leaf chewing in the south central Andes: a 3,000 year archaeological record of coca-leaf chewing from northern Chile. J Psychoactive Drugs 37 (2005) 455-458
3. Fairley H.B. Anesthesia in the Inca empire. Rev Esp Anestesiol Reanim 54 (2007) 556-562
4. Gaedcke F. Ueber das Erythroxylin, dargestellt aus den Blattern des in Sudamerika cultivirten Strauches Erythroxylon Coca Lam. Archiv der Pharmazie 132 (1855) 141-150
5. Ruetsch Y.A., Boni T., and Borgeat A. From cocaine to ropivacaine: the history of local anesthetic drugs. Curr Top Med Chem 1 (2001) 175-182
6. Jones A.E. Sigmund Freud: Life and Work (1953), Hogarth Press, London
7. Cocaine Chemistry and New Local Anesthetics. Cal West Med 25 (1926) 232-233
8. Taylor I.B., Marks B.W., and Edmonds G. Intravenous administration of procaine hydrochloride during general anesthesia. Arch Surg 59 (1949) 714-723
9. Phillips O.C., Lyons W.B., Harris L.C., Nelson A.T., Graff T.D., and Frazier T.M. Intravenous lidocaine as an adjunct to general anesthesia: a clinical evaluation. Anesth Analg 39 (1960) 317-322
10. Bigelow N., and Harrison I. General analgesic effects of procaine. J Pharmacol Exp Ther 81 (1944) 368-373
11. Lemoyne J. Use of dimethyl-dithio-hydantoin in treatment of certain facial neuralgias. Ann Otolaryngol 67 (1950) 626-628
12. Kugelberg E., and Lindblom U. The mechanism of the pain in trigeminal neuralgia. J Neurol Neurosurg Psychiatry 22 (1959) 36-43
13. Blom S. Trigeminal neuralgia: its treatment with a new anticonvulsant drug (G-32883). Lancet 1 (1962) 839-840
14. Vaughan Williams E.M. Classification of antidysrhythmic drugs. Pharmacol Ther [B] 1 (1975) 115-138
15. Desanctis R.W. Electrical Conversion of Ventricular Tachycardia. Jama 191 (1965) 632-636
16. Carden N.L., and Steinhaus J.E. Lidocaine in cardiac resuscitation from ventricular fibrillation. Circ Res 4 (1956) 680-683
17. Vaughan Williams E.M. A classification of antiarrhythmic actions reassessed after a decade of new drugs. J Clin Pharmacol 24 (1984) 129-147
18. Loeser J.D., Ward Jr. A.A., and White Jr. L.E. Chronic deafferentation of human spinal cord neurons. J Neurosurg 29 (1968) 48-50
19. Burchiel K.J., and Wyler A.R. Ectopic action potential generation in peripheral trigeminal axons. Exp Neurol 62 (1978) 269-281
20. Boas R.A., Covino B.G., and Shahnarian A. Analgesic responses to i.v. lignocaine. Br J Anaesth 54 (1982) 501-505
21. Petersen P., and Kastrup J. Dercum's disease (adiposis dolorosa). Treatment of the severe pain with intravenous lidocaine. Pain 28 (1987) 77-80
22. Kastrup J., Petersen P., Dejgard A., Angelo H.R., and Hilsted J. Intravenous lidocaine infusion-a new treatment of chronic painful diabetic neuropathy?. Pain 28 (1987) 69-75
23. Lindstrom P., and Lindblom U. The analgesic effect of tocainide in trigeminal neuralgia. Pain 28 (1987) 45-50
24. Dejgard A., Petersen P., and Kastrup J. Mexiletine for treatment of chronic painful diabetic neuropathy. Lancet 1 (1988) 9-11
25. Watson C.P., Evans R.J., Reed K., Merskey H., Goldsmith L., and Warsh J. Amitriptyline versus placebo in postherpetic neuralgia. Neurology 32 (1982) 671-673
26. Leijon G., and Boivie J. Central post-stroke pain-a controlled trial of amitriptyline and carbamazepine. Pain 36 (1989) 27-36
27. Watson C.P., Vernich L., Chipman M., and Reed K. Nortriptyline versus amitriptyline in postherpetic neuralgia: a randomized trial. Neurology 51 (1998) 1166-1171
28. Pancrazio J.J., Kamatchi G.L., Roscoe A.K., and Lynch III C. Inhibition of neuronal Na+ channels by antidepressant drugs. J Pharmacol Exp Ther 284 (1998) 208-214
29. Barber M.J., Starmer C.F., and Grant A.O. Blockade of cardiac sodium channels by amitriptyline and diphenylhydantoin. Evidence for two use-dependent binding sites. Circ Res 69 (1991) 677-696
30. Dick I.E., Brochu R.M., Purohit Y., Kaczorowski G.J., Martin W.J., and Priest B.T. Sodium channel blockade may contribute to the analgesic efficacy of antidepressants. J Pain 8 (2007) 315-324
31. Govrin-Lippmann R., and Devor M. Ongoing activity in severed nerves: source and variation with time. Brain Res 159 (1978) 406-410
32. Bennett G.J., and Xie Y.K. A peripheral mononeuropathy in rat that produces disorders of pain sensation like those seen in man. Pain 33 (1988) 87-107
33. Seltzer Z., Dubner R., and Shir Y. A novel behavioral model of neuropathic pain disorders produced in rats by partial sciatic nerve injury. Pain 43 (1990) 205-218
34. Kim S.H., and Chung J.M. An experimental model for peripheral neuropathy produced by segmental spinal nerve ligation in the rat. Pain 50 (1992) 355-363
35. Kajander K.C., Wakisaka S., and Bennett G.J. Spontaneous discharge originates in the dorsal root ganglion at the onset of a painful peripheral neuropathy in the rat. Neurosci Lett 138 (1992) 225-228
36. Devor M., Wall P.D., and Catalan N. Systemic lidocaine silences ectopic neuroma and DRG discharge without blocking nerve conduction. Pain 48 (1992) 261-268
37. Ambrosio A.F., Soares-Da-Silva P., Carvalho C.M., and Carvalho A.P. Mechanisms of action of carbamazepine and its derivatives, oxcarbazepine, BIA 2-093, and BIA 2-024. Neurochem Res 27 (2002) 121-130
38. Tecoma E.S. Oxcarbazepine. Epilepsia 40 Suppl 5 (1999) S37-S46
39. Dogra S., Beydoun S., Mazzola J., Hopwood M., and Wan Y. Oxcarbazepine in painful diabetic neuropathy: a randomized, placebo-controlled study. Eur J Pain 9 (2005) 543-554
40. Grosskopf J., Mazzola J., Wan Y., and Hopwood M. A randomized, placebo-controlled study of oxcarbazepine in painful diabetic neuropathy. Acta Neurol Scand 114 (2006) 177-180
41. Errington A.C., Stohr T., Heers C., and Lees G. The investigational anticonvulsant lacosamide selectively enhances slow inactivation of voltage-gated sodium channels. Mol Pharmacol 73 (2008) 157-169
42. Wallace M.S., Rowbotham M., Bennett G.J., Jensen T.S., Pladna R., and Quessy S. A multicenter, double-blind, randomized, placebo-controlled crossover evaluation of a short course of 4030W92 in patients with chronic neuropathic pain. J Pain 3 (2002) 227-233
43. Hagen N.A., du Souich P., Lapointe B., et al. Tetrodotoxin for moderate to severe cancer pain: a randomized, double blind, parallel design multicenter study. J Pain Symptom Manage 35 (2008) 420-429
44. Bach F.W., Jensen T.S., Kastrup J., Stigsby B., and Dejgard A. The effect of intravenous lidocaine on nociceptive processing in diabetic neuropathy. Pain 40 (1990) 29-34
45. Ragsdale D.S., McPhee J.C., Scheuer T., and Catterall W.A. Common molecular determinants of local anesthetic, antiarrhythmic, and anticonvulsant block of voltage-gated Na+ channels. Proc Natl Acad Sci U S A 93 (1996) 9270-9275
46. Wagner II L.E., Eaton M., Sabnis S.S., and Gingrich K.J. Meperidine and lidocaine block of recombinant voltage-dependent Na+ channels: evidence that meperidine is a local anesthetic. Anesthesiology 91 (1999) 1481-1490
47. Wagner II L.E., Gingrich K.J., Kulli J.C., and Yang J. Ketamine blockade of voltage-gated sodium channels: evidence for a shared receptor site with local anesthetics. Anesthesiology 95 (2001) 1406-1413
48. Wang G.K., Russell C., and Wang S.Y. State-dependent block of voltage-gated Na+ channels by amitriptyline via the local anesthetic receptor and its implication for neuropathic pain. Pain 110 (2004) 166-174
49. Yarov-Yarovoy V., Brown J., Sharp E.M., Clare J.J., Scheuer T., and Catterall W.A. Molecular determinants of voltage-dependent gating and binding of pore-blocking drugs in transmembrane segment IIIS6 of the Na(+) channel alpha subunit. J Biol Chem 276 (2001) 20-27
50. Starmer C.F., Grant A.O., and Strauss H.C. Mechanisms of use-dependent block of sodium channels in excitable membranes by local anesthetics. Biophys J 46 (1984) 15-27
51. Schwarz W., Palade P.T., and Hille B. Local anesthetics. Effect of pH on use-dependent block of sodium channels in frog muscle. Biophys J 20 (1977) 343-368
52. Courtney K.R. Mechanism of frequency-dependent inhibition of sodium currents in frog myelinated nerve by the lidocaine derivative GEA. J Pharmacol Exp Ther 195 (1975) 225-236
53. Hille B. Local anesthetics: hydrophilic and hydrophobic pathways for the drug-receptor reaction. J Gen Physiol 69 (1977) 497-515
54. Hondeghem L.M., and Katzung B.G. Antiarrhythmic agents: the modulated receptor mechanism of action of sodium and calcium channel-blocking drugs. Annu Rev Pharmacol Toxicol 24 (1984) 387-423
55. Catterall W.A., Goldin A.L., and Waxman S.G. International Union of Pharmacology. XXXIX. Compendium of voltage-gated ion channels: sodium channels. Pharmacol Rev 55 (2003) 575-578
56. Catterall W.A., Goldin A.L., and Waxman S.G. International Union of Pharmacology. XLVII. Nomenclature and Structure-Function Relationships of Voltage-Gated Sodium Channels. Pharmacol Rev 57 (2005) 397-409
57. Catterall W.A., Cestele S., Yarov-Yarovoy V., Yu F.H., Konoki K., and Scheuer T. Voltage-gated ion channels and gating modifier toxins. Toxicon 49 (2007) 124-141
58. Bosmans F., and Tytgat J. Voltage-gated sodium channel modulation by scorpion alpha-toxins. Toxicon 49 (2007) 142-158
59. Wang J., Ou S.W., Wang Y.J., Kameyama M., Kameyama A., and Zong Z.H. Analysis of four novel variants of Nav1.5/SCN5A cloned from the brain. Neurosci Res (2009)
60. Ragsdale D.S. How do mutant Nav1.1 sodium channels cause epilepsy?. Brain Res Rev 58 (2008) 149-159
61. Vahedi K., Depienne C., Le Fort D., et al. Elicited repetitive daily blindness: a new phenotype associated with hemiplegic migraine and SCN1A mutations. Neurology 72 (2009) 1178-1183
62. Scalmani P., Rusconi R., Armatura E., et al. Effects in neocortical neurons of mutations of the Na(v)1.2 Na+ channel causing benign familial neonatal-infantile seizures. J Neurosci 26 (2006) 10100-10109
63. Colosimo E., Gambardella A., Mantegazza M., et al. Electroclinical features of a family with simple febrile seizures and temporal lobe epilepsy associated with SCN1A loss-of-function mutation. Epilepsia 48 (2007) 1691-1696
64. Fujiwara T. Clinical spectrum of mutations in SCN1A gene: severe myoclonic epilepsy in infancy and related epilepsies. Epilepsy Res 70 Suppl 1 (2006) S223-S230
65. Fujiwara T., Sugawara T., Mazaki-Miyazaki E., et al. Mutations of sodium channel alpha subunit type 1 (SCN1A) in intractable childhood epilepsies with frequent generalized tonic-clonic seizures. Brain 126 (2003) 531-546
66. Lossin C. A catalog of SCN1A variants. Brain Dev 31 (2009) 114-130
67. Lossin C., Rhodes T.H., Desai R.R., et al. Epilepsy-associated dysfunction in the voltage-gated neuronal sodium channel SCN1A. J Neurosci 23 (2003) 11289-11295
68. Mantegazza M., Gambardella A., Rusconi R., et al. Identification of an Nav1.1 sodium channel (SCN1A) loss-of-function mutation associated with familial simple febrile seizures. Proc Natl Acad Sci U S A 102 (2005) 18177-18182
69. Meisler M.H., and Kearney J.A. Sodium channel mutations in epilepsy and other neurological disorders. J Clin Invest 115 (2005) 2010-2017
70. Sugawara T., Mazaki-Miyazaki E., Fukushima K., et al. Frequent mutations of SCN1A in severe myoclonic epilepsy in infancy. Neurology 58 (2002) 1122-1124
71. Vanoye C.G., Lossin C., Rhodes T.H., and George Jr. A.L. Single-channel properties of human NaV1.1 and mechanism of channel dysfunction in SCN1A-associated epilepsy. J Gen Physiol 127 (2006) 1-14
72. Jurkat-Rott K., and Lehmann-Horn F. Genotype-phenotype correlation and therapeutic rationale in hyperkalemic periodic paralysis. Neurotherapeutics 4 (2007) 216-224
73. Lehmann-Horn F., Jurkat-Rott K., and Rudel R. Periodic paralysis: understanding channelopathies. Curr Neurol Neurosci Rep 2 (2002) 61-69
74. Sternberg D., Maisonobe T., Jurkat-Rott K., et al. Hypokalaemic periodic paralysis type 2 caused by mutations at codon 672 in the muscle sodium channel gene SCN4A. Brain 124 (2001) 1091-1099
75. Rogart R.B., Cribbs L.L., Muglia L.K., Kephart D.D., and Kaiser M.W. Molecular cloning of a putative tetrodotoxin-resistant rat heart Na+ channel isoform. Proc Natl Acad Sci U S A 86 (1989) 8170-8174
76. Remme C.A., Wilde A.A., and Bezzina C.R. Cardiac sodium channel overlap syndromes: different faces of SCN5A mutations. Trends Cardiovasc Med 18 (2008) 78-87
77. Zimmer T., and Surber R. SCN5A channelopathies-an update on mutations and mechanisms. Prog Biophys Mol Biol 98 (2008) 120-136
78. McKinney B.C., Chow C.Y., Meisler M.H., and Murphy G.G. Exaggerated emotional behavior in mice heterozygous null for the sodium channel Scn8a (Nav1.6). Genes Brain Behav 7 (2008) 629-638
79. Chen Y.H., Dale T.J., Romanos M.A., Whitaker W.R., Xie X.M., and Clare J.J. Cloning, distribution and functional analysis of the type III sodium channel from human brain. Eur J Neurosci 12 (2000) 4281-4289
80. Black J.A., Liu S., Tanaka M., Cummins T.R., and Waxman S.G. Changes in the expression of tetrodotoxin-sensitive sodium channels within dorsal root ganglia neurons in inflammatory pain. Pain 108 (2004) 237-247
81. Dib-Hajj S.D., Fjell J., Cummins T.R., et al. Plasticity of sodium channel expression in DRG neurons in the chronic constriction injury model of neuropathic pain. Pain 83 (1999) 591-600
82. Waxman S.G., Kocsis J.D., and Black J.A. Type III sodium channel mRNA is expressed in embryonic but not adult spinal sensory neurons, and is reexpressed following axotomy. J Neurophysiol 72 (1994) 466-470
83. Cummins T.R., and Waxman S.G. Downregulation of tetrodotoxin-resistant sodium currents and upregulation of a rapidly repriming tetrodotoxin-sensitive sodium current in small spinal sensory neurons after nerve injury. J Neurosci 17 (1997) 3503-3514
84. Fukuoka T., Kobayashi K., Yamanaka H., Obata K., Dai Y., and Noguchi K. Comparative study of the distribution of the alpha-subunits of voltage-gated sodium channels in normal and axotomized rat dorsal root ganglion neurons. J Comp Neurol 510 (2008) 188-206
85. Zhao P., Waxman S.G., and Hains B.C. Sodium channel expression in the ventral posterolateral nucleus of the thalamus after peripheral nerve injury. Mol Pain 2 (2006) 27
86. Guo F., Yu N., Cai J.Q., et al. Voltage-gated sodium channel Nav1.1, Nav1.3 and beta1 subunit were up-regulated in the hippocampus of spontaneously epileptic rat. Brain Res Bull 75 (2008) 179-187
87. Bartolomei F., Gastaldi M., Massacrier A., Planells R., Nicolas S., and Cau P. Changes in the mRNAs encoding subtypes I, II and III sodium channel alpha subunits following kainate-induced seizures in rat brain. J Neurocytol 26 (1997) 667-678
88. Nassar M.A., Baker M.D., Levato A., et al. Nerve injury induces robust allodynia and ectopic discharges in Nav1.3 null mutant mice. Mol Pain 2 (2006) 33
89. Hains B.C., Saab C.Y., Klein J.P., Craner M.J., and Waxman S.G. Altered sodium channel expression in second-order spinal sensory neurons contributes to pain after peripheral nerve injury. J Neurosci 24 (2004) 4832-4839
90. Lindia J.A., Kohler M.G., Martin W.J., and Abbadie C. Relationship between sodium channel NaV1.3 expression and neuropathic pain behavior in rats. Pain 117 (2005) 145-153
91. Sangameswaran L., Fish L.M., Koch B.D., et al. A novel tetrodotoxin-sensitive, voltage-gated sodium channel expressed in rat and human dorsal root ganglia. J Biol Chem 272 (1997) 14805-14809
92. Toledo-Aral J.J., Moss B.L., He Z.J., et al. Identification of PN1, a predominant voltage-dependent sodium channel expressed principally in peripheral neurons. Proc Natl Acad Sci U S A 94 (1997) 1527-1532
93. Thakor D.K., Lin A., Matsuka Y., et al. Increased peripheral nerve excitability and local NaV1.8 mRNA up-regulation in painful neuropathy. Mol Pain 5 (2009) 14
94. Kretschmer T., Happel L.T., England J.D., et al. Accumulation of PN1 and PN3 sodium channels in painful human neuroma-evidence from immunocytochemistry. Acta Neurochir (Wien) 144 (2002) 803-810 discussion 810
95. Cummins T.R., Howe J.R., and Waxman S.G. Slow closed-state inactivation: a novel mechanism underlying ramp currents in cells expressing the hNE/PN1 sodium channel. J Neurosci 18 (1998) 9607-9619
96. Nassar M.A., Stirling L.C., Forlani G., et al. Nociceptor-specific gene deletion reveals a major role for Nav1.7 (PN1) in acute and inflammatory pain. Proc Natl Acad Sci U S A 101 (2004) 12706-12711
97. Nassar M.A., Levato A., Stirling L.C., and Wood J.N. Neuropathic pain develops normally in mice lacking both Nav1.7 and Nav1.8. Mol Pain 1 (2005) 24
98. Djouhri L., Fang X., Okuse K., Wood J.N., Berry C.M., and Lawson S.N. The TTX-resistant sodium channel Nav1.8 (SNS/PN3): expression and correlation with membrane properties in rat nociceptive primary afferent neurons. J Physiol 550 (2003) 739-752
99. Devor M. Ectopic discharge in Abeta afferents as a source of neuropathic pain. Exp Brain Res 196 (2009) 115-128
100. Fertleman C.R., Baker M.D., Parker K.A., et al. SCN9A mutations in paroxysmal extreme pain disorder: allelic variants underlie distinct channel defects and phenotypes. Neuron 52 (2006) 767-774
101. Yang Y., Wang Y., Li S., et al. Mutations in SCN9A, encoding a sodium channel alpha subunit, in patients with primary erythermalgia. J Med Genet 41 (2004) 171-174
102. Cox J.J., Reimann F., Nicholas A.K., et al. An SCN9A channelopathy causes congenital inability to experience pain. Nature 444 (2006) 894-898
103. Goldberg Y.P., MacFarlane J., MacDonald M.L., et al. Loss-of-function mutations in the Nav1.7 gene underlie congenital indifference to pain in multiple human populations. Clin Genet 71 (2007) 311-319
104. Nilsen K.B., Nicholas A.K., Woods C.G., Mellgren S.I., Nebuchennykh M., and Aasly J. Two novel SCN9A mutations causing insensitivity to pain. Pain 143 (2009) 155-158
105. Ahmad S., Dahllund L., Eriksson A.B., et al. A stop codon mutation in SCN9A causes lack of pain sensation. Hum Mol Genet 16 (2007) 2114-2121
106. Drenth J.P., and Waxman S.G. Mutations in sodium-channel gene SCN9A cause a spectrum of human genetic pain disorders. J Clin Invest 117 (2007) 3603-3609
107. Cheng X., Dib-Hajj S.D., Tyrrell L., and Waxman S.G. Mutation I136V alters electrophysiological properties of the Na(v)1.7 channel in a family with onset of erythromelalgia in the second decade. Mol Pain 4 (2008) 1
108. Choi J.S., Dib-Hajj S.D., and Waxman S.G. Inherited erythermalgia: limb pain from an S4 charge-neutral Na channelopathy. Neurology 67 (2006) 1563-1567
109. Cummins T.R., Dib-Hajj S.D., and Waxman S.G. Electrophysiological properties of mutant Nav1.7 sodium channels in a painful inherited neuropathy. J Neurosci 24 (2004) 8232-8236
110. Dib-Hajj S.D., Rush A.M., Cummins T.R., et al. Gain-of-function mutation in Nav1.7 in familial erythromelalgia induces bursting of sensory neurons. Brain 128 (2005) 1847-1854
111. Han C., Rush A.M., Dib-Hajj S.D., et al. Sporadic onset of erythermalgia: a gain-of-function mutation in Nav1.7. Ann Neurol 59 (2006) 553-558
112. Harty T.P., Dib-Hajj S.D., Tyrrell L., et al. Na(V)1.7 mutant A863P in erythromelalgia: effects of altered activation and steady-state inactivation on excitability of nociceptive dorsal root ganglion neurons. J Neurosci 26 (2006) 12566-12575
113. Lampert A., Dib-Hajj S.D., Tyrrell L., and Waxman S.G. Size matters: Erythromelalgia mutation S241T in Nav1.7 alters channel gating. J Biol Chem 281 (2006) 36029-36035
114. Sheets P.L., Jackson II J.O., Waxman S.G., Dib-Hajj S.D., and Cummins T.R. A Nav1.7 channel mutation associated with hereditary erythromelalgia contributes to neuronal hyperexcitability and displays reduced lidocaine sensitivity. J Physiol 581 (2007) 1019-1031
115. Dib-Hajj S.D., Yang Y., and Waxman S.G. Genetics and molecular pathophysiology of Na(v)1.7-related pain syndromes. Adv Genet 63 (2008) 85-110
116. Jarecki B.W., Sheets P.L., Jackson II J.O., and Cummins T.R. Paroxysmal Extreme Pain Disorder mutations within the D3/S4-S5 Linker of Nav1.7 cause moderate destabilization of fast-inactivation. J Physiol (2008) jphysiol.2008.154906
117. Zimmermann K., Leffler A., Babes A., et al. Sensory neuron sodium channel Nav1.8 is essential for pain at low temperatures. Nature 447 (2007) 855-858
118. Abrahamsen B., Zhao J., Asante C.O., et al. The Cell and Molecular Basis of Mechanical, Cold, and Inflammatory Pain. Science 321 (2008) 702-705
119. Okuse K., Chaplan S.R., McMahon S.B., et al. Regulation of expression of the sensory neuron-specific sodium channel SNS in inflammatory and neuropathic pain. Mol Cell Neurosci 10 (1997) 196-207
120. Decosterd I., Ji R.R., Abdi S., Tate S., and Woolf C.J. The pattern of expression of the voltage-gated sodium channels Na(v)1.8 and Na(v)1.9 does not change in uninjured primary sensory neurons in experimental neuropathic pain models. Pain 96 (2002) 269-277
121. Novakovic S.D., Tzoumaka E., McGivern J.G., et al. Distribution of the tetrodotoxin-resistant sodium channel PN3 in rat sensory neurons in normal and neuropathic conditions. J Neurosci 18 (1998) 2174-2187
122. Dong X.W., Goregoaker S., Engler H., et al. Small interfering RNA-mediated selective knockdown of Na(V)1.8 tetrodotoxin-resistant sodium channel reverses mechanical allodynia in neuropathic rats. Neuroscience 146 (2007) 812-821
123. Joshi S.K., Mikusa J.P., Hernandez G., et al. Involvement of the TTX-resistant sodium channel Nav 1.8 in inflammatory and neuropathic, but not post-operative, pain states. Pain 123 (2006) 75-82
124. Lai J., Gold M.S., Kim C.S., et al. Inhibition of neuropathic pain by decreased expression of the tetrodotoxin-resistant sodium channel, NaV1.8. Pain 95 (2002) 143-152
125. Roza C., Laird J.M., Souslova V., Wood J.N., and Cervero F. The tetrodotoxin-resistant Na+ channel Nav1.8 is essential for the expression of spontaneous activity in damaged sensory axons of mice. J Physiol 550 (2003) 921-926
126. Cummins T.R., Dib-Hajj S.D., Black J.A., Akopian A.N., Wood J.N., and Waxman S.G. A novel persistent tetrodotoxin-resistant sodium current in SNS-null and wild-type small primary sensory neurons. J Neurosci 19 (1999) RC43
127. Dib-Hajj S.D., Tyrrell L., Cummins T.R., Black J.A., Wood P.M., and Waxman S.G. Two tetrodotoxin-resistant sodium channels in human dorsal root ganglion neurons. FEBS Lett 462 (1999) 117-120
128. Dib-Hajj S., Black J.A., Cummins T.R., and Waxman S.G. NaN/Nav1.9: a sodium channel with unique properties. Trends Neurosci 25 (2002) 253-259
129. Dib-Hajj S.D., Tyrrell L., Black J.A., and Waxman S.G. NaN, a novel voltage-gated Na channel, is expressed preferentially in peripheral sensory neurons and down-regulated after axotomy. Proc Natl Acad Sci U S A 95 (1998) 8963-8968
130. Tate S., Benn S., Hick C., et al. Two sodium channels contribute to the TTX-R sodium current in primary sensory neurons. Nat Neurosci 1 (1998) 653-655
131. Porreca F., Lai J., Bian D., et al. A comparison of the potential role of the tetrodotoxin-insensitive sodium channels, PN3/SNS and NaN/SNS2, in rat models of chronic pain. Proc Natl Acad Sci U S A 96 (1999) 7640-7644
132. Priest B.T., Murphy B.A., Lindia J.A., et al. Contribution of the tetrodotoxin-resistant voltage-gated sodium channel NaV1.9 to sensory transmission and nociceptive behavior. Proc Natl Acad Sci U S A 102 (2005) 9382-9387
133. Smith E.S.J., and Momin A. Persistent pain: the contribution of NaV1.9. J Physiol (2008) jphysiol.2008.152520
134. Jarvis M.F., Honore P., Shieh C.C., et al. A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci U S A 104 (2007) 8520-8525
135. Kort M.E., Drizin I., Gregg R.J., et al. Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain. J Med Chem 51 (2008) 407-416
136. McGaraughty S., Chu K.L., Scanio M.J., Kort M.E., Faltynek C.R., and Jarvis M.F. A selective Nav1.8 sodium channel blocker, A-803467 [5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], attenuates spinal neuronal activity in neuropathic rats. J Pharmacol Exp Ther 324 (2008) 1204-1211
137. Felix J.P., Williams B.S., Priest B.T., et al. Functional assay of voltage-gated sodium channels using membrane potential-sensitive dyes. Assay Drug Dev Technol 2 (2004) 260-268
138. Hoyt S.B., London C., Gorin D., et al. Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain. Bioorg Med Chem Lett 17 (2007) 4630-4634
139. Hoyt S.B., London C., Ok H., et al. Benzazepinone Na(v)1.7 blockers: Potential treatments for neuropathic pain. Bioorg Med Chem Lett (2007)
140. Williams B.S., Felix J.P., Priest B.T., et al. Characterization of a new class of potent inhibitors of the voltage-gated sodium channel Nav1.7. Biochemistry 46 (2007) 14693-14703
141. London C., Hoyt S.B., Parsons W.H., et al. Imidazopyridines: a novel class of hNav1.7 channel blockers. Bioorg Med Chem Lett 18 (2008) 1696-1701
142. Liu C.J., Priest B.T., Bugianesi R.M., et al. A high-capacity membrane potential FRET-based assay for NaV1.8 channels. Assay Drug Dev Technol 4 (2006) 37-48
143. Trivedi S., Dekermendjian K., Julien R., et al. Cellular HTS Assays for Pharmacological Characterization of Na(V)1.7 Modulators. Assay Drug Dev Technol (2007)
144. Vickery R.G., Amagasu S.M., Chang R., et al. Comparison of the pharmacological properties of rat Na(V)1.8 with rat Na(V)1.2a and human Na(V)1.5 voltage-gated sodium channel subtypes using a membrane potential sensitive dye and FLIPR. Receptors Channels 10 (2004) 11-23
145. Benjamin E.R., Pruthi F., Olanrewaju S., et al. State-dependent compound inhibition of Nav1.2 sodium channels using the FLIPR Vm dye: on-target and off-target effects of diverse pharmacological agents. J Biomol Screen 11 (2006) 29-39
146. Bhattacharya A, Wang Q, Wu N, Chaplan SR, Wickenden AD. Assay dependent activity of the sodium channel gating modifier protoxin-I: implications for sodium channel drug discovery. In: Experimental Biology; 2009; New Orleans, LA, 2009.
147. Middleton R.E., Warren V.A., Kraus R.L., et al. Two tarantula peptides inhibit activation of multiple sodium channels. Biochemistry 41 (2002) 14734-14747
148. Castle N., Printzenhoff D., Zellmer S., Antonio B., Wickenden A., and Silvia C. Sodium channel inhibitor drug discovery using automated high throughput electrophysiology platforms. Comb Chem High Throughput Screen 12 (2009) 107-122
149. Schmalhofer W., Calhoun J., Burrows R., et al. ProTx-II, a selective inhibitor of NaV1.7 sodium channels, blocks action potential propagation in nociceptors. Mol Pharmacol (2008) mol.108.047670
150. Escoubas P., and Bosmans F. Spider peptide toxins as leads for drug development. Expert Opinion on Drug Discovery 2 (2007) 823-835
151. Xiao Y., Bingham J.P., Zhu W., Moczydlowski E., Liang S., and Cummins T.R. Tarantula huwentoxin-IV inhibits neuronal sodium channels by binding to receptor site 4 and trapping the domain ii voltage sensor in the closed configuration. J Biol Chem 283 (2008) 27300-27313
152. Bosmans F., Martin-Eauclaire M.F., and Swartz K.J. Deconstructing voltage sensor function and pharmacology in sodium channels. Nature 456 (2008) 202-208
153. Sokolov S., Kraus R.L., Scheuer T., and Catterall W.A. Inhibition of Sodium Channel Gating by Trapping the Domain II Voltage Sensor with Protoxin II. Mol Pharmacol 73 (2008) 1020-1028
154. Smith J.J., Cummins T.R., Alphy S., and Blumenthal K.M. Molecular Interactions of the Gating Modifier Toxin ProTx-II with Nav1.5: Implied existence of a novel toxin binding site coupled to activation. J Biol Chem 282 (2007) 12687-12697
155. Dib-Hajj S.D., Binshtok A.M., Cummins T.R., Jarvis M.F., Samad T., and Zimmermann K. Voltage-gated sodium channels in pain states: Role in pathophysiology and targets for treatment. Brain Res Rev 60 (2009) 65-83
156. Waxman S.G. Channel, neuronal and clinical function in sodium channelopathies: from genotype to phenotype. Nat Neurosci 10 (2007) 405-409
157. Cummins T.R., and Rush A.M. Voltage-gated sodium channel blockers for the treatment of neuropathic pain. Expert Rev Neurother 7 (2007) 1597-1612
158. Cummins T.R., Sheets P.L., and Waxman S.G. The roles of sodium channels in nociception: Implications for mechanisms of pain. Pain 131 (2007) 243-257
159. Wood J.N., and Boorman J. Voltage-gated sodium channel blockers; target validation and therapeutic potential. Curr Top Med Chem 5 (2005) 529-537
160. Wood J.N., Boorman J.P., Okuse K., and Baker M.D. Voltage-gated sodium channels and pain pathways. J Neurobiol 61 (2004) 55-71
161. England S. Voltage-gated sodium channels: the search for subtype-selective analgesics. Expert Opinion on Investigational Drugs 17 (2008) 1849-1864
162. Momin A., and Wood J.N. Sensory neuron voltage-gated sodium channels as analgesic drug targets. Curr Opin Neurobiol 18 (2008) 383-388
163. Priest B.T., and Kaczorowski G.J. Blocking sodium channels to treat neuropathic pain. Expert Opin Ther Targets 11 (2007) 291-306
164. Hargus N.J., and Patel M.K. Voltage-gated Na+ channels in neuropathic pain. Expert Opinion on Investigational Drugs 16 (2007) 635-646
165. Catterall W.A. From ionic currents to molecular mechanisms: the structure and function of voltage-gated sodium channels. Neuron 26 (2000) 13-25
166. Kalso E., Tasmuth T., and Neuvonen P.J. Amitriptyline effectively relieves neuropathic pain following treatment of breast cancer. Pain 64 (1996) 293-302
167. Kautio A.L., Haanpaa M., Saarto T., and Kalso E. Amitriptyline in the treatment of chemotherapy-induced neuropathic symptoms. J Pain Symptom Manage 35 (2008) 31-39
168. Campbell F.G., Graham J.G., and Zilkha K.J. Clinical trial of carbazepine (tegretol) in trigeminal neuralgia. J Neurol Neurosurg Psychiatry 29 (1966) 265-267
169. Killian J.M., and Fromm G.H. Carbamazepine in the treatment of neuralgia. Use of side effects. Arch Neurol 19 (1968) 129-136
170. Rull J.A., Quibrera R., Gonzalez-Millan H., and Lozano Castaneda O. Symptomatic treatment of peripheral diabetic neuropathy with carbamazepine (Tegretol): double blind crossover trial. Diabetologia 5 (1969) 215-218
171. Harke H., Gretenkort P., Ladleif H.U., Rahman S., and Harke O. The response of neuropathic pain and pain in complex regional pain syndrome I to carbamazepine and sustained-release morphine in patients pretreated with spinal cord stimulation: a double-blinded randomized study. Anesth Analg 92 (2001) 488-495
172. Kishore-Kumar R., Max M.B., Schafer S.C., et al. Desipramine relieves postherpetic neuralgia. Clin Pharmacol Ther 47 (1990) 305-312
173. Max M.B., Kishore-Kumar R., Schafer S.C., et al. Efficacy of desipramine in painful diabetic neuropathy: a placebo-controlled trial. Pain 45 (1991) 3-9 discussion 1-2
174. Goldstein D.J., Lu Y., Detke M.J., Lee T.C., and Iyengar S. Duloxetine vs. placebo in patients with painful diabetic neuropathy. Pain 116 (2005) 109-118
175. Raskin J., Pritchett Y.L., Wang F., et al. A double-blind, randomized multicenter trial comparing duloxetine with placebo in the management of diabetic peripheral neuropathic pain. Pain Med 6 (2005) 346-356
176. Wernicke J.F., Pritchett Y.L., D'Souza D.N., et al. A randomized controlled trial of duloxetine in diabetic peripheral neuropathic pain. Neurology 67 (2006) 1411-1420
177. Rauck R.L., Shaibani A., Biton V., Simpson J., and Koch B. Lacosamide in painful diabetic peripheral neuropathy: a phase 2 double-blind placebo-controlled study. Clin J Pain 23 (2007) 150-158
178. Shaibani A., Fares S., Selam J.L., et al. Lacosamide in Painful Diabetic Neuropathy: An 18-Week Double-Blind Placebo-Controlled Trial. J Pain (2009)
179. Wymer J.P., Simpson J., Sen D., and Bongardt S. Efficacy and safety of lacosamide in diabetic neuropathic pain: an 18-week double-blind placebo-controlled trial of fixed-dose regimens. Clin J Pain 25 (2009) 376-385
180. Zakrzewska J.M., Chaudhry Z., Nurmikko T.J., Patton D.W., and Mullens E.L. Lamotrigine (lamictal) in refractory trigeminal neuralgia: results from a double-blind placebo controlled crossover trial. Pain 73 (1997) 223-230
181. McCleane G. 200 mg daily of lamotrigine has no analgesic effect in neuropathic pain: a randomised, double-blind, placebo controlled trial. Pain 83 (1999) 105-107
182. Eisenberg E., Lurie Y., Braker C., Daoud D., and Ishay A. Lamotrigine reduces painful diabetic neuropathy: a randomized, controlled study. Neurology 57 (2001) 505-509
183. Vestergaard K., Andersen G., Gottrup H., Kristensen B.T., and Jensen T.S. Lamotrigine for central poststroke pain: a randomized controlled trial. Neurology 56 (2001) 184-190
184. Finnerup N.B., Sindrup S.H., Bach F.W., Johannesen I.L., and Jensen T.S. Lamotrigine in spinal cord injury pain: a randomized controlled trial. Pain 96 (2002) 375-383
185. Simpson D.M., McArthur J.C., Olney R., et al. Lamotrigine for HIV-associated painful sensory neuropathies: a placebo-controlled trial. Neurology 60 (2003) 1508-1514
186. Rao R.D., Flynn P.J., Sloan J.A., et al. Efficacy of lamotrigine in the management of chemotherapy-induced peripheral neuropathy: a phase 3 randomized, double-blind, placebo-controlled trial, N01C3. Cancer 112 (2008) 2802-2808
187. Kastrup J., Bach F.W., Petersen P., et al. Lidocaine treatment of painful diabetic neuropathy and endogenous opioid peptides in plasma. Clin J Pain 5 (1989) 239-244
188. Ellemann K., Sjogren P., Banning A.M., Jensen T.S., Smith T., and Geertsen P. Trial of intravenous lidocaine on painful neuropathy in cancer patients. Clin J Pain 5 (1989) 291-294
189. Rowbotham M.C., Reisner-Keller L.A., and Fields H.L. Both intravenous lidocaine and morphine reduce the pain of postherpetic neuralgia. Neurology 41 (1991) 1024-1028
190. Bruera E., Ripamonti C., Brenneis C., Macmillan K., and Hanson J. A randomized double-blind crossover trial of intravenous lidocaine in the treatment of neuropathic cancer pain. J Pain Symptom Manage 7 (1992) 138-140
191. Medrik-Goldberg T., Lifschitz D., Pud D., Adler R., and Eisenberg E. Intravenous lidocaine, amantadine, and placebo in the treatment of sciatica: a double-blind, randomized, controlled study. Reg Anesth Pain Med 24 (1999) 534-540
192. Wallace M.S., Ridgeway B.M., Leung A.Y., Gerayli A., and Yaksh T.L. Concentration-effect relationship of intravenous lidocaine on the allodynia of complex regional pain syndrome types I and II. Anesthesiology 92 (2000) 75-83
193. Attal N., Gaude V., Brasseur L., et al. Intravenous lidocaine in central pain: a double-blind, placebo-controlled, psychophysical study. Neurology 54 (2000) 564-574
194. Finnerup N.B., Biering-Sorensen F., Johannesen I.L., et al. Intravenous lidocaine relieves spinal cord injury pain: a randomized controlled trial. Anesthesiology 102 (2005) 1023-1030
195. Tremont-Lukats I.W., Hutson P.R., and Backonja M.M. A randomized, double-masked, placebo-controlled pilot trial of extended IV lidocaine infusion for relief of ongoing neuropathic pain. Clin J Pain 22 (2006) 266-271
196. Backonja M., and Gombar K.A. Response of central pain syndromes to intravenous lidocaine. J Pain Symptom Manage 7 (1992) 172-178
197. Attal N., Rouaud J., Brasseur L., Chauvin M., and Bouhassira D. Systemic lidocaine in pain due to peripheral nerve injury and predictors of response. Neurology 62 (2004) 218-225
198. Sakurai M., and Kanazawa I. Positive symptoms in multiple sclerosis: their treatment with sodium channel blockers, lidocaine and mexiletine. J Neurol Sci 162 (1999) 162-168
199. Chabal C., Jacobson L., Russell L.C., and Burchiel K.J. Pain responses to perineuromal injection of normal saline, gallamine, and lidocaine in humans. Pain 36 (1989) 321-325
200. Chabal C., Jacobson L., Mariano A., Chaney E., and Britell C.W. The use of oral mexiletine for the treatment of pain after peripheral nerve injury. Anesthesiology 76 (1992) 513-517
201. Stracke H., Meyer U.E., Schumacher H.E., and Federlin K. Mexiletine in the treatment of diabetic neuropathy. Diabetes Care 15 (1992) 1550-1555
202. Chiou-Tan F.Y., Tuel S.M., Johnson J.C., Priebe M.M., Hirsh D.D., and Strayer J.R. Effect of mexiletine on spinal cord injury dysesthetic pain. Am J Phys Med Rehabil 75 (1996) 84-87
203. Oskarsson P., Ljunggren J.G., and Lins P.E. Efficacy and safety of mexiletine in the treatment of painful diabetic neuropathy. The Mexiletine Study Group. Diabetes Care 20 (1997) 1594-1597
204. Wright J.M., Oki J.C., and Graves III L. Mexiletine in the symptomatic treatment of diabetic peripheral neuropathy. Ann Pharmacother 31 (1997) 29-34
205. Wallace M.S., Magnuson S., and Ridgeway B. Efficacy of oral mexiletine for neuropathic pain with allodynia: a double-blind, placebo-controlled, crossover study. Reg Anesth Pain Med 25 (2000) 459-467
206. Saudek C.D., Werns S., and Reidenberg M.M. Phenytoin in the treatment of diabetic symmetrical polyneuropathy. Clin Pharmacol Ther 22 (1977) 196-199
207. Chadda V.S., and Mathur M.S. Double blind study of the effects of diphenylhydantoin sodium on diabetic neuropathy. J Assoc Physicians India 26 (1978) 403-406
208. Galer B.S., Twilling L.L., Harle J., Cluff R.S., Friedman E., and Rowbotham M.C. Lack of efficacy of riluzole in the treatment of peripheral neuropathic pain conditions. Neurology 55 (2000) 971-975