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Optimising a difficult Nav1.8 cell line assay for automated patch-clamp screening

The TTX-resistant sodium channel Nav1.8 is expressed in peripheral sensory nociceptors and is implicated in a range of inflammatory and visceral pain conditions such as irritable bowel syndrome (IBS)1. Nav1.8 channel function in sensory neurons changes after injury or inflammation, with a redistribution from the soma to axons and upregulated activity through inflammatory mediators and signalling pathways.

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Atrial‐like cardiomyocytes from human pluripotent stem cells are a robust preclinical model for assessing atrial‐selective pharmacology 

Devalla, H.D.; Schwach, V.; Ford, J.W.; Milnes, J.T.; El‐Haou, S.; Jackson, C.; Gkatzis, K.; Elliott, D.A.; de Sousa Lopes, S.M.C.; Mummery, C.L.; Verkerk, A.O.; Passier, R. EMBO Molecular Medicine 2015. 7 (4), 394-410

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Synthesis and biological evaluation of piperazine derivatives as novel isoform selective voltage-gated sodium (Nav) 1.3 channel modulators 

Jukič, M.; Frlan, R.; Chan, F.; Kirby, R.W.; Madge, D.J.; Tytgat, J.; Peigneur, S.; Anderluh, M.; Kikelj, D. Medicinal Chemistry Research. 2015, 24 (6), 2366-2380

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Open access to the KCNQ channel: Retigabine and second generation M-current openers
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Action of Clathrodin and Analogues on Voltage-Gated Sodium Channels 

Peigneur, S.; Žula, A.; Zidar, N.; Chan-Porter, F.; Kirby, R.; Madge, D.; Ilaš, J.; Kikelj, D.; Tytgat, J. Marine Drugs. 2014, 12(4), 2132-43

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Ligand- and structure-based virtual screening for clathrodin-derived human voltage-gated sodium channel modulators 

Tomašić, T.; Hartzoulakis. B.; Zidar. N.; Chan, F.; Kirby R.W.; Madge, D.J.; Peigneur, S.; Tytgat, J.; Kikelj, D. Journal of Chemical Information and Modelling. 2013, 53 (12), 3223-32

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Novel state-dependent voltage-gated sodium channel modulators, based on marine alkaloids from Agelas sponges 

Hodnik, Ž.; Tomašić, T.; Mašič L.P.; Chan, F.; Kirby, R.W.; Madge D.J.; Kikelj, D. European Journal of Medicinal Chemistry. 2013, 70, 154-64

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Human Electrophysiological and Pharmacological Properties of XEN-D0101: A Novel Atrial-Selective Kv1.5/IKur Inhibitor

Ford J.; Milnes J.; Wettwer E.; Christ T.; Rogers M.; Sutton K.; Madge D.; Virag L.; Jost N.; Horvath Z.; Matschke K.; Varro A.; Ravens, U. Journal of Cardiovascular Pharmacology. 2013, 61 (5), 408-415

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Voltage-clamp and current-clamp recordings from mammalian DRG neurons

Cummins, T.R.; Rush, A.M.; Estacion, M.; Dib-Hajj, S.D.; Waxman, S.G. Nature Protocols. 2009, 4, 1103-12 https://pubmed.ncbi.nlm.nih.gov/19617882/

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Recent advances in electrophysiology-based screening technology and the impact upon ion channel discovery research 

Southan, A.P.; Clark, G. Methods in Molecular Biology. 2009, 565, 187-208

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