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Sodium channel blockers for neuropathic pain

, PhD, , PhD, , PhD & , PhD
Pages 755-779 | Published online: 13 Apr 2010

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Mirko Rivara & Valentina Zuliani. (2016) Novel sodium channel antagonists in the treatment of neuropathic pain. Expert Opinion on Investigational Drugs 25:2, pages 215-226.
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Ken-ichiro Tanaka, Shota Sekino, Megumi Ikegami, Hiroko Ikeda & Junzo Kamei. (2015) Antihyperalgesic effects of ProTx-II, a Nav1.7 antagonist, and A803467, a Nav1.8 antagonist, in diabetic mice. Journal of Experimental Pharmacology 7, pages 11-16.
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Diego N. Messina, Emanuel D. Peralta, Alicia M. Seltzer, Sean I. Patterson & Cristian G. Acosta. (2022) Age-dependent and modality-specific changes in the phenotypic markers Nav1.8, ASIC3, P2X3 and TRPM8 in male rat primary sensory neurons during healthy aging. Biogerontology 24:1, pages 111-136.
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Han-Gang Yu, Gina Sizemore, Ivan Martinez & Peter Perrotta. (2022) Inhibition of SARS-CoV-2 Viral Channel Activity Using FDA-Approved Channel Modulators Independent of Variants. Biomolecules 12:11, pages 1673.
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Kuang-I. Cheng, Hung-Chen Wang, Kuang-Yi Tseng, Yi-Hsuan Wang, Chung-Yu Chang, Yi-Jing Chen, Chung-Sheng Lai, Dar-Ren Chen & Lin-Li Chang. (2022) Cilostazol Ameliorates Peripheral Neuropathic Pain in Streptozotocin-Induced Type I Diabetic Rats. Frontiers in Pharmacology 12.
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Georgina Palomés-Borrajo, Jordi Badia, Xavier Navarro & Clara Penas. (2021) Nerve Excitability and Neuropathic Pain is Reduced by BET Protein Inhibition After Spared Nerve Injury. The Journal of Pain 22:12, pages 1617-1630.
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Alessia Catalano, Carlo Franchini & Alessia Carocci. (2021) Voltage-Gated Sodium Channel Blockers: Synthesis of Mexiletine Analogues and Homologues. Current Medicinal Chemistry 28:8, pages 1535-1548.
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David R. Witty, Giuseppe AlvaroDominique DerjeanGerard M. P. GiblinKevin GunnCharles LargeDavid T. MacphersonValerie MorissetDavina OwenJoanne PalmerFrancois RugieroSimon TateChristopher A. Hinckley & Himanshu Naik. (2020) Discovery of Vixotrigine: A Novel Use-Dependent Sodium Channel Blocker for the Treatment of Trigeminal Neuralgia. ACS Medicinal Chemistry Letters 11:9, pages 1678-1687.
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Sigrid S. Skånland & Artur Cieślar-Pobuda. (2019) Off-label uses of drugs for depression. European Journal of Pharmacology 865, pages 172732.
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Taís de Campos Lima, Débora de Oliveira Santos, Júlia Borges Paes Lemes, Luana Mota Chiovato & Celina Monteiro da Cruz Lotufo. (2019) Hyperglycemia induces mechanical hyperalgesia and depolarization of the resting membrane potential of primary nociceptive neurons: Role of ATP-sensitive potassium channels. Journal of the Neurological Sciences 401, pages 55-61.
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Ravneet Kaur KhanguraJasmine SharmaAnjana BaliNirmal SinghAmteshwar Singh Jaggi. (2019) An integrated review on new targets in the treatment of neuropathic pain. The Korean Journal of Physiology & Pharmacology 23:1, pages 1.
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Weihua Cai, Qingzan Zhao, Jinping Shao, Jingjing Zhang, Lei Li, Xiuhua Ren, Songxue Su, Qian Bai, Ming Li, Xuemei Chen, Jian Wang, Jing Cao & Weidong Zang. (2018) MicroRNA-182 Alleviates Neuropathic Pain by Regulating Nav1.7 Following Spared Nerve Injury in Rats. Scientific Reports 8:1.
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Xiaonan Liang, Gang Yu & Ruibin Su. (2018) Effects of ralfinamide in models of nerve injury and chemotherapy-induced neuropathic pain. European Journal of Pharmacology 823, pages 27-34.
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D.R. Witty, D.T. MacPherson & G.M.P Giblin. 2017. Comprehensive Medicinal Chemistry III. Comprehensive Medicinal Chemistry III 131 175 .
Marco Pieroni, Baojie Wan, Valentina Zuliani, Scott G. Franzblau, Gabriele Costantino & Mirko Rivara. (2015) Discovery of antitubercular 2,4-diphenyl-1H-imidazoles from chemical library repositioning and rational design. European Journal of Medicinal Chemistry 100, pages 44-49.
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Abderrahman El Bouakher, Hassan Allouchi, Isabelle Abrunhosa-Thomas, Yves Troin & Gérald Guillaumet. (2015) Suzuki-Miyaura Reactions of Halospirooxindole Derivatives. European Journal of Organic Chemistry 2015:16, pages 3450-3461.
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Giuseppe Lauria, Dan Ziegler, Rayaz Malik, Ingemar S. J. Merkies, Stephen G. Waxman & Catharina G. Faber. (2014) The Role of Sodium Channels in Painful Diabetic and Idiopathic Neuropathy. Current Diabetes Reports 14:10.
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Lorcan Browne, Katie Lidster, Sarah Al-Izki, Lisa Clutterbuck, Cristina Posada, A. W. Edith Chan, Dieter Riddall, John Garthwaite, David Baker & David L. Selwood. (2014) Imidazol-1-ylethylindazole Voltage-Gated Sodium Channel Ligands Are Neuroprotective during Optic Neuritis in a Mouse Model of Multiple Sclerosis. Journal of Medicinal Chemistry 57:7, pages 2942-2952.
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Eline K.M. Lebbe, Steve Peigneur, Ward Brullot, Thierry Verbiest & Jan Tytgat. (2014) Ala-7, His-10 and Arg-12 are crucial amino acids for activity of a synthetically engineered μ-conotoxin. Peptides 53, pages 300-306.
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Meichun Deng, Xuan Luo, Liping Jiang, Hanchun Chen, Jun Wang, Hailun He & Songping Liang. (2013) Synthesis and biological characterization of synthetic analogs of Huwentoxin-IV (Mu-theraphotoxin-Hh2a), a neuronal tetrodotoxin-sensitive sodium channel inhibitor. Toxicon 71, pages 57-65.
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Lik Tong Tan. (2013) Pharmaceutical agents from filamentous marine cyanobacteria. Drug Discovery Today 18:17-18, pages 863-871.
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Ryan M. Brady, Minmin Zhang, Robert Gable, Raymond S. Norton & Jonathan B. Baell. (2013) De novo design and synthesis of a μ-conotoxin KIIIA peptidomimetic. Bioorganic & Medicinal Chemistry Letters 23:17, pages 4892-4895.
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Sultan Chowdhury, Shifeng Liu, Jay A. Cadieux, Tom Hsieh, Mikhail Chafeev, Shaoyi Sun, Qi Jia, Jianyu Sun, Mark Wood, Jonathan Langille, Serguei Sviridov, Jianmin Fu, Zaihui Zhang, Ray Chui, Audrey Wang, Xing Cheng, Jing Zhong, Sazzad Hossain, Kuldip Khakh, Ivana Rajlic, Henry Verschoof, Rainbow Kwan & Wendy Young. (2012) Tetracyclic spirooxindole blockers of hNaV1.7: activity in vitro and in CFA-induced inflammatory pain model. Medicinal Chemistry Research 22:4, pages 1825-1836.
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Michela De Bellis, Annamaria De Luca, Jean F. Desaphy, Roberta Carbonara, Judith A. Heiny, Ann Kennedy, Alessia Carocci, Maria M. Cavalluzzi, Giovanni Lentini, Carlo Franchini & Diana Conte Camerino. (2013) Combined Modifications of Mexiletine Pharmacophores for New Lead Blockers of Nav1.4 Channels. Biophysical Journal 104:2, pages 344-354.
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René Markgraf, Enrico Leipold, Jana Schirmeyer, Marianne Paolini‐Bertrand, Oliver Hartley & Stefan H Heinemann. (2012) Mechanism and molecular basis for the sodium channel subtype specificity of µ‐conopeptide CnIIIC. British Journal of Pharmacology 167:3, pages 576-586.
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Inger Kers, Istvan Macsari, Gabor Csjernyik, Martin Nylöf, Karin Skogholm, Lars Sandberg, Alexander Minidis, Tjerk Bueters, Jonas Malmborg, Anders B. Eriksson, Per-Eric Lund, Elisabet Venyike, Lei Luo, Jan-Erik Nyström & Yevgeni Besidski. (2012) Phenethyl nicotinamides, a novel class of NaV1.7 channel blockers: Structure and activity relationship. Bioorganic & Medicinal Chemistry Letters 22:19, pages 6108-6115.
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Julie K. Klint, Sebastian Senff, Darshani B. Rupasinghe, Sing Yan Er, Volker Herzig, Graham M. Nicholson & Glenn F. King. (2012) Spider-venom peptides that target voltage-gated sodium channels: Pharmacological tools and potential therapeutic leads. Toxicon 60:4, pages 478-491.
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Inger Kers, Gabor Csjernyik, Istvan Macsari, Martin Nylöf, Lars Sandberg, Karin Skogholm, Tjerk Bueters, Anders B. Eriksson, Sandra Oerther, Per-Eric Lund, Elisabet Venyike, Jan-Erik Nyström & Yevgeni Besidski. (2012) Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers. Bioorganic & Medicinal Chemistry Letters 22:17, pages 5618-5624.
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Istvan Macsari, Yevgeni Besidski, Gabor Csjernyik, Linda I. Nilsson, Lars Sandberg, Ulrika Yngve, Kristofer Åhlin, Tjerk Bueters, Anders B. Eriksson, Per-Eric Lund, Elisabet Venyike, Sandra Oerther, Karin Hygge Blakeman, Lei Luo & Per I. Arvidsson. (2012) 3-Oxoisoindoline-1-carboxamides: Potent, State-Dependent Blockers of Voltage-Gated Sodium Channel Na V 1.7 with Efficacy in Rat Pain Models . Journal of Medicinal Chemistry 55:15, pages 6866-6880.
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Hanh Nho Nguyen, Howie Bregman, John L. Buchanan, Bingfan Du, Elma Feric, Liyue Huang, Xingwen Li, Joseph Ligutti, Dong Liu, Annika B. Malmberg, David J. Matson, Jeff S. McDermott, Vinod F. Patel, Ben Wilenkin, Anruo Zou, Stefan I. McDonough & Erin F. DiMauro. (2012) Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists. Bioorganic & Medicinal Chemistry Letters 22:2, pages 1055-1060.
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Michael E Hildebrand, Janette Mezeyova, Paula L Smith, Michael W Salter, Elizabeth Tringham & Terrance P Snutch. (2011) Identification of Sodium Channel Isoforms That Mediate Action Potential Firing in Lamina I/II Spinal Cord Neurons. Molecular Pain 7, pages 1744-8069-7-67.
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Istvan Macsari, Lars Sandberg, Yevgeni Besidski, Ylva Gravenfors, Tobias Ginman, Johan Bylund, Tjerk Bueters, Anders B. Eriksson, Per-Eric Lund, Elisabet Venyike & Per I. Arvidsson. (2011) Phenyl isoxazole voltage-gated sodium channel blockers: Structure and activity relationship. Bioorganic & Medicinal Chemistry Letters 21:13, pages 3871-3876.
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Philippe G. Nantermet & Darrell A. Henze. 2011. 19 32 .

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