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68 results

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A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability.
Payne CE, Brown AR, Theile JW, Loucif AJ, Alexandrou AJ, Fuller MD, Mahoney JH, Antonio BM, Gerlach AC, Printzenhoff DM, Prime RL, Stockbridge G, Kirkup AJ, Bannon AW, England S, Chapman ML, Bagal S, Roeloffs R, Anand U, Anand P, Bungay PJ, Kemp M, Butt RP, Stevens EB. Payne CE, et al. Among authors: stevens eb. Br J Pharmacol. 2015 May;172(10):2654-70. doi: 10.1111/bph.13092. Epub 2015 Apr 10. Br J Pharmacol. 2015. PMID: 25625641 Free PMC article.
GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P ) channel opener, reduces rat dorsal root ganglion neuron excitability.
Loucif AJC, Saintot PP, Liu J, Antonio BM, Zellmer SG, Yoger K, Veale EL, Wilbrey A, Omoto K, Cao L, Gutteridge A, Castle NA, Stevens EB, Mathie A. Loucif AJC, et al. Among authors: stevens eb. Br J Pharmacol. 2018 Jun;175(12):2272-2283. doi: 10.1111/bph.14098. Epub 2017 Dec 29. Br J Pharmacol. 2018. PMID: 29150838 Free PMC article.
Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release.
Alexandrou AJ, Brown AR, Chapman ML, Estacion M, Turner J, Mis MA, Wilbrey A, Payne EC, Gutteridge A, Cox PJ, Doyle R, Printzenhoff D, Lin Z, Marron BE, West C, Swain NA, Storer RI, Stupple PA, Castle NA, Hounshell JA, Rivara M, Randall A, Dib-Hajj SD, Krafte D, Waxman SG, Patel MK, Butt RP, Stevens EB. Alexandrou AJ, et al. Among authors: stevens eb. PLoS One. 2016 Apr 6;11(4):e0152405. doi: 10.1371/journal.pone.0152405. eCollection 2016. PLoS One. 2016. PMID: 27050761 Free PMC article.
The discovery and optimization of benzimidazoles as selective NaV1.8 blockers for the treatment of pain.
Brown AD, Bagal SK, Blackwell P, Blakemore DC, Brown B, Bungay PJ, Corless M, Crawforth J, Fengas D, Fenwick DR, Gray V, Kemp M, Klute W, Malet Sanz L, Miller D, Murata Y, Payne CE, Skerratt S, Stevens EB, Warmus JS. Brown AD, et al. Among authors: stevens eb. Bioorg Med Chem. 2019 Jan 1;27(1):230-239. doi: 10.1016/j.bmc.2018.12.002. Epub 2018 Dec 4. Bioorg Med Chem. 2019. PMID: 30538065
Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.
Bagal SK, Bungay PJ, Denton SM, Gibson KR, Glossop MS, Hay TL, Kemp MI, Lane CA, Lewis ML, Maw GN, Million WA, Payne CE, Poinsard C, Rawson DJ, Stammen BL, Stevens EB, Thompson LR. Bagal SK, et al. Among authors: stevens eb. ACS Med Chem Lett. 2015 Apr 29;6(6):650-4. doi: 10.1021/acsmedchemlett.5b00059. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26101568 Free PMC article.
Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia.
Cao L, McDonnell A, Nitzsche A, Alexandrou A, Saintot PP, Loucif AJ, Brown AR, Young G, Mis M, Randall A, Waxman SG, Stanley P, Kirby S, Tarabar S, Gutteridge A, Butt R, McKernan RM, Whiting P, Ali Z, Bilsland J, Stevens EB. Cao L, et al. Among authors: stevens eb. Sci Transl Med. 2016 Apr 20;8(335):335ra56. doi: 10.1126/scitranslmed.aad7653. Sci Transl Med. 2016. PMID: 27099175 Clinical Trial.
Characterizing human stem cell-derived sensory neurons at the single-cell level reveals their ion channel expression and utility in pain research.
Young GT, Gutteridge A, Fox H, Wilbrey AL, Cao L, Cho LT, Brown AR, Benn CL, Kammonen LR, Friedman JH, Bictash M, Whiting P, Bilsland JG, Stevens EB. Young GT, et al. Among authors: stevens eb. Mol Ther. 2014 Aug;22(8):1530-1543. doi: 10.1038/mt.2014.86. Epub 2014 May 15. Mol Ther. 2014. PMID: 24832007 Free PMC article.
Ion channels as therapeutic targets: a drug discovery perspective.
Bagal SK, Brown AD, Cox PJ, Omoto K, Owen RM, Pryde DC, Sidders B, Skerratt SE, Stevens EB, Storer RI, Swain NA. Bagal SK, et al. Among authors: stevens eb. J Med Chem. 2013 Feb 14;56(3):593-624. doi: 10.1021/jm3011433. Epub 2012 Nov 29. J Med Chem. 2013. PMID: 23121096 Review.
Corrigendum to "Investigation of the structure activity relationship of flufenamic acid derivatives at the human TRESK channel K2P18.1" [Bioorg. Med. Chem. Lett. 26 (2016) 4919-4924].
Monteillier A, Loucif A, Omoto K, Stevens EB, Lainez S, Saintot PP, Cao L, Pryde DC. Monteillier A, et al. Among authors: stevens eb. Bioorg Med Chem Lett. 2017 May 1;27(9):2082. doi: 10.1016/j.bmcl.2017.02.063. Epub 2017 Mar 17. Bioorg Med Chem Lett. 2017. PMID: 28320618 No abstract available.
68 results