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1
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0032966913
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Potent antihyperalgesic activity without tolerance produced by glycine site antagonist of N-Methyl-D-aspartate receptor GV196771A
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This paper describes the discovery of GV196771A, a selective glycine site antagonist of the NMDA receptor. The compound was found to have potent antihyperalgesic activity in several animal models for neuropathic pain, and was not accompanied by development of tolerance.
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Quartaroli M., Carignani C., Dal Forno G., Mugnaini M., Ugolini A., Arban R., Bettelini L., Maraia G., Belardetti F., Reggiani A.et al. Potent antihyperalgesic activity without tolerance produced by glycine site antagonist of N-Methyl-D-aspartate receptor GV196771A. J Pharmacol Exp Ther. 290:1999;158-169 This paper describes the discovery of GV196771A, a selective glycine site antagonist of the NMDA receptor. The compound was found to have potent antihyperalgesic activity in several animal models for neuropathic pain, and was not accompanied by development of tolerance.
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(1999)
J Pharmacol Exp Ther
, vol.290
, pp. 158-169
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Quartaroli, M.1
Carignani, C.2
Dal Forno, G.3
Mugnaini, M.4
Ugolini, A.5
Arban, R.6
Bettelini, L.7
Maraia, G.8
Belardetti, F.9
Reggiani, A.10
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2
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0035798403
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GV196771A, an NMDA receptor/glycine site antagonist, attenuates mechanical allodynia in neuropathic rats and reduces tolerance induced by morphine in mice
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Quartaroli M., Fasdelli N., Bettelini L., Maraia G., Corsi M. GV196771A, an NMDA receptor/glycine site antagonist, attenuates mechanical allodynia in neuropathic rats and reduces tolerance induced by morphine in mice. Eur J Pharmacol. 430:2001;219-227.
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(2001)
Eur J Pharmacol
, vol.430
, pp. 219-227
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Quartaroli, M.1
Fasdelli, N.2
Bettelini, L.3
Maraia, G.4
Corsi, M.5
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3
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0037058809
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A randomized, double-blind, placebo-controlled trial of a glycine antagonist in neuropathic pain
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This paper describes the clinical assessment and inability of GV196771A to be efficacious in several double-blind placebo-controlled trials in neuropathic pain. GV196771A was not efficacious for diabetic neuropathy, postherpetic neuralgia, complex regional pain syndrome or peripheral nerve injury.
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Wallace M.S., Rowbotham M.C., Katz N.P., Dworkin R.H., Dotson R.M., Galer B.S., Rauck R.L., Backonja M.M., Quessy S.N., Meisner P.D. A randomized, double-blind, placebo-controlled trial of a glycine antagonist in neuropathic pain. Neurology. 59:2002;1694-1700 This paper describes the clinical assessment and inability of GV196771A to be efficacious in several double-blind placebo-controlled trials in neuropathic pain. GV196771A was not efficacious for diabetic neuropathy, postherpetic neuralgia, complex regional pain syndrome or peripheral nerve injury.
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(2002)
Neurology
, vol.59
, pp. 1694-1700
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Wallace, M.S.1
Rowbotham, M.C.2
Katz, N.P.3
Dworkin, R.H.4
Dotson, R.M.5
Galer, B.S.6
Rauck, R.L.7
Backonja, M.M.8
Quessy, S.N.9
Meisner, P.D.10
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4
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0034977378
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N-methyl-D-aspartate receptor antagonists potentiate the antinociceptive effects of morphine in squirrel monkeys
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Allen R.M., Dykstra L.A. N-methyl-D-aspartate receptor antagonists potentiate the antinociceptive effects of morphine in squirrel monkeys. J Pharmacol Exp Ther. 298:2001;288-297.
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(2001)
J Pharmacol Exp Ther
, vol.298
, pp. 288-297
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Allen, R.M.1
Dykstra, L.A.2
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5
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0036805378
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The glycine/NMDA receptor antagonist (+)-HA966 enhances the peripheral effect of morphine in neuropathic rats
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Martinez V., Christensen D., Kayser V. The glycine/NMDA receptor antagonist (+)-HA966 enhances the peripheral effect of morphine in neuropathic rats. Pain. 99:2002;537-545.
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(2002)
Pain
, vol.99
, pp. 537-545
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Martinez, V.1
Christensen, D.2
Kayser, V.3
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6
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0037468414
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Tricyclic indole 2-carboxylic acids: Highly in vivo active and selective antagonists for the glycine binding site of the NMDA receptor
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Katayama S., Nobuyuki A., Kodo T., Masumoto S., Hourai S., Tamamura C., Tanaka H., Nagata R. Tricyclic indole 2-carboxylic acids: highly in vivo active and selective antagonists for the glycine binding site of the NMDA receptor. J Med Chem. 46:2003;691-701.
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(2003)
J Med Chem
, vol.46
, pp. 691-701
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Katayama, S.1
Nobuyuki, A.2
Kodo, T.3
Masumoto, S.4
Hourai, S.5
Tamamura, C.6
Tanaka, H.7
Nagata, R.8
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7
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0035144105
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Genetic enhancement of inflammatory pain by forebrain NR2B overexpression
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Wei F., Wang G., Kerchner G.A., Kim S.J., Xu H., Chen Z., Zhuo M. Genetic enhancement of inflammatory pain by forebrain NR2B overexpression. Nat Neurosci. 4:2001;164-169.
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(2001)
Nat Neurosci
, vol.4
, pp. 164-169
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Wei, F.1
Wang, G.2
Kerchner, G.A.3
Kim, S.J.4
Xu, H.5
Chen, Z.6
Zhuo, M.7
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8
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0036092615
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Changes in gene expression and neuronal phenotype in brain stem pain modulatory circuitry after inflammation
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Miki K., Zhou Q., Guo W., Guan Y., Terayama R., Dubner R., Ren K. Changes in gene expression and neuronal phenotype in brain stem pain modulatory circuitry after inflammation. J Neurophysiol. 87:2002;750-760.
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(2002)
J Neurophysiol
, vol.87
, pp. 750-760
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Miki, K.1
Zhou, Q.2
Guo, W.3
Guan, Y.4
Terayama, R.5
Dubner, R.6
Ren, K.7
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9
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13344261412
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Impairment of suckling response, trigeminal neuronal pattern formation, and hippocampal LTD in NMDA receptor epsilon 2 subunit mutant mice
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Kutsuwada T., Sakimura K., Manabe T., Takayama C., Katakura N., Kushiya E., Natsume R., Watanabe M., Inoue Y., Yagi T. Impairment of suckling response, trigeminal neuronal pattern formation, and hippocampal LTD in NMDA receptor epsilon 2 subunit mutant mice. Neuron. 16:1996;333-344.
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(1996)
Neuron
, vol.16
, pp. 333-344
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Kutsuwada, T.1
Sakimura, K.2
Manabe, T.3
Takayama, C.4
Katakura, N.5
Kushiya, E.6
Natsume, R.7
Watanabe, M.8
Inoue, Y.9
Yagi, T.10
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10
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0032559283
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Importance of the intracellular domain of NR2 subunits for NMDA receptor function in vivo
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Sprengel R., Suchanek B., Amico C., Brusa R., Burnaschev N., Rozov A., Hvalby O., Jensen V., Paulsen O., Andersen P.et al. Importance of the intracellular domain of NR2 subunits for NMDA receptor function in vivo. Cell. 92:1998;279-289.
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(1998)
Cell
, vol.92
, pp. 279-289
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Sprengel, R.1
Suchanek, B.2
Amico, C.3
Brusa, R.4
Burnaschev, N.5
Rozov, A.6
Hvalby, O.7
Jensen, V.8
Paulsen, O.9
Andersen, P.10
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11
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0035968917
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Regulation of acute nociceptive responses by the NMDA receptor GluRε2 subunit
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Wainai T., Takeuchi T., Seo N., Mishina M. Regulation of acute nociceptive responses by the NMDA receptor GluRε2 subunit. Mol Neurosci. 12:2001;3169-3172.
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(2001)
Mol Neurosci
, vol.12
, pp. 3169-3172
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Wainai, T.1
Takeuchi, T.2
Seo, N.3
Mishina, M.4
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12
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0035970522
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Pharmacological characterization of interactions of RO 25-6981 with the NR2B (ε2) subunit
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Lynch D.R., Shim S.S., Seifert K.M., Kurapathi S., Mutel V., Gallagher M.J., Guttmann R.P. Pharmacological characterization of interactions of RO 25-6981 with the NR2B (ε2) subunit. Eur J Pharmacol. 416:2001;185-195.
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(2001)
Eur J Pharmacol
, vol.416
, pp. 185-195
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Lynch, D.R.1
Shim, S.S.2
Seifert, K.M.3
Kurapathi, S.4
Mutel, V.5
Gallagher, M.J.6
Guttmann, R.P.7
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13
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0036720776
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Pharmacological characterization of RO 63-1908 (1-[2-(4-Hydroxy-phenoxy)-ethyl]-4-(4-methyl-benzyl)-piperidin-4-ol), a novel subtype-selective N-methyl-D-aspartate antagonist
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This paper describes the pharmacological characterization of Ro 63-1908, an NR2B selective antagonist. This compound was shown to be efficacious in animal models of seizure and protective against cortical damage in permanent focal ischemia while producing no adverse cardiovascular or CNS side effects, making it a promising candidate for efficacy in neuropathic pain.
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Gill R., Alanine A., Bourson A., Buttelmann B., Fischer G., Heitz M., Kew J., Levet-Trafit B., Lorez H., Malherbe P.et al. Pharmacological characterization of RO 63-1908 (1-[2-(4-Hydroxy-phenoxy)-ethyl]-4-(4-methyl-benzyl)-piperidin-4-ol), a novel subtype-selective N-methyl-D-aspartate antagonist. J Pharmacol Exp Ther. 302:2002;940-948 This paper describes the pharmacological characterization of Ro 63-1908, an NR2B selective antagonist. This compound was shown to be efficacious in animal models of seizure and protective against cortical damage in permanent focal ischemia while producing no adverse cardiovascular or CNS side effects, making it a promising candidate for efficacy in neuropathic pain.
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(2002)
J Pharmacol Exp Ther
, vol.302
, pp. 940-948
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Gill, R.1
Alanine, A.2
Bourson, A.3
Buttelmann, B.4
Fischer, G.5
Heitz, M.6
Kew, J.7
Levet-Trafit, B.8
Lorez, H.9
Malherbe, P.10
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14
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0036122295
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Studies on the subtype selectivity of CP-101, 606: Evidence for two classes of NR2B-selective NMDA receptor antagonists
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Chazot P.L., Lawrence S., Thompson C.L. Studies on the subtype selectivity of CP-101, 606: evidence for two classes of NR2B-selective NMDA receptor antagonists. Neuropharmacology. 42:2002;319-324.
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(2002)
Neuropharmacology
, vol.42
, pp. 319-324
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Chazot, P.L.1
Lawrence, S.2
Thompson, C.L.3
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15
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0030771671
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Antinociceptive activity of CP-101, 606, an NMDA receptor NR2B subunit antagonist
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Taniguchi K., Katsuhiro S., Mizutani M., Shimada K., Ishikawa T., Menniti F.S., Nagahisa A. Antinociceptive activity of CP-101, 606, an NMDA receptor NR2B subunit antagonist. Br J Pharmacol. 122:1997;809-812.
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(1997)
Br J Pharmacol
, vol.122
, pp. 809-812
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Taniguchi, K.1
Katsuhiro, S.2
Mizutani, M.3
Shimada, K.4
Ishikawa, T.5
Menniti, F.S.6
Nagahisa, A.7
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16
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0036145275
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Inhibition of neuropathic pain by decreased expression of the tetrodotoxin resistant sodium channel, NAV1.8
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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. 95:2002;143-152.
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(2002)
Pain
, vol.95
, pp. 143-152
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Lai, J.1
Gold, M.S.2
Kim, C.S.3
Bian, D.4
Ossipov, M.H.5
Hunter, J.C.6
Porreca, F.7
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17
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0001059602
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A comparison of the potential role of the tetrodotoxin-insensitive sodium channels, PN3/SNS and NaN/SNS2, in rat models of chronic pain
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Porreca F., Lai J., Bian D., Wegert S., Ossipov M., Eglen R.M., Kassotakis L., Novakovic S., Rabert D.K., Sangameswaran L., Hunter J.C. 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 USA. 96:1999;7640-7644.
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(1999)
Proc Natl Acad Sci USA
, vol.96
, pp. 7640-7644
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Porreca, F.1
Lai, J.2
Bian, D.3
Wegert, S.4
Ossipov, M.5
Eglen, R.M.6
Kassotakis, L.7
Novakovic, S.8
Rabert, D.K.9
Sangameswaran, L.10
Hunter, J.C.11
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18
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0033363999
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The tetrodotoxin-resistant sodium channel SNS has a specialized function in pain pathways
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Akopian A.M., Souslova V., England S., Okuse K., Ogata N., Ure J., Smith A., Kerr B.J., McMahon S.B., Boyce S.et al. The tetrodotoxin-resistant sodium channel SNS has a specialized function in pain pathways. Nat Neurosci. 2:1999;541-548.
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(1999)
Nat Neurosci
, vol.2
, pp. 541-548
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Akopian, A.M.1
Souslova, V.2
England, S.3
Okuse, K.4
Ogata, N.5
Ure, J.6
Smith, A.7
Kerr, B.J.8
McMahon, S.B.9
Boyce, S.10
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19
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0036813714
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Deficits in visceral pain and referred hyperalgesia in Nav1.8 (SNS/PN3)-null mice
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This paper shows that SNS/PN3 null mice showed blunted responses and no referred hyperalgesia in response to intracolonic capsaicin indicating the essential role for Nav1.8 in mediating spontaneous activity in sensitized nociceptors.
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Laird J., Souslova V., Wood J.N., Cervero F. Deficits in visceral pain and referred hyperalgesia in Nav1.8 (SNS/PN3)-null mice. J Neurosci. 22:2002;8352-8356 This paper shows that SNS/PN3 null mice showed blunted responses and no referred hyperalgesia in response to intracolonic capsaicin indicating the essential role for Nav1.8 in mediating spontaneous activity in sensitized nociceptors.
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(2002)
J Neurosci
, vol.22
, pp. 8352-8356
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Laird, J.1
Souslova, V.2
Wood, J.N.3
Cervero, F.4
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20
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0035829033
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A role for the TTX-resistant sodium channel Nav 1.9 in NGF-induced hyperalgesia, but not neuropathic pain
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Kerr B.J., Souslova V., McMahon S.B., Wood J.N. A role for the TTX-resistant sodium channel Nav 1.9 in NGF-induced hyperalgesia, but not neuropathic pain. Neuroreport. 12:2001;3077-3080.
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(2001)
Neuroreport
, vol.12
, pp. 3077-3080
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Kerr, B.J.1
Souslova, V.2
McMahon, S.B.3
Wood, J.N.4
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23
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0034237501
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Systemic lidocaine for neuropathic pain relief
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Mao J., Chen L.L. Systemic lidocaine for neuropathic pain relief. Pain. 87:2000;7-17.
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(2000)
Pain
, vol.87
, pp. 7-17
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Mao, J.1
Chen, L.L.2
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