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A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability.
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.
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.
PLoS One. 2016 Apr 6;11(4):e0152405. doi: 10.1371/journal.pone.0152405. eCollection 2016.
PLoS One. 2016.
PMID: 27050761
Free PMC article.
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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: alexandrou a.
Sci Transl Med. 2016 Apr 20;8(335):335ra56. doi: 10.1126/scitranslmed.aad7653.
Sci Transl Med. 2016.
PMID: 27099175
Clinical Trial.
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Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes.
Storer RI, Pike A, Swain NA, Alexandrou AJ, Bechle BM, Blakemore DC, Brown AD, Castle NA, Corbett MS, Flanagan NJ, Fengas D, Johnson MS, Jones LH, Marron BE, Payne CE, Printzenhoff D, Rawson DJ, Rose CR, Ryckmans T, Sun J, Theile JW, Torella R, Tseng E, Warmus JS.
Storer RI, et al. Among authors: alexandrou aj.
Bioorg Med Chem Lett. 2017 Nov 1;27(21):4805-4811. doi: 10.1016/j.bmcl.2017.09.056. Epub 2017 Sep 28.
Bioorg Med Chem Lett. 2017.
PMID: 29029933
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An Intracellular Allosteric Modulator Binding Pocket in SK2 Ion Channels Is Shared by Multiple Chemotypes.
Cho LT, Alexandrou AJ, Torella R, Knafels J, Hobbs J, Taylor T, Loucif A, Konopacka A, Bell S, Stevens EB, Pandit J, Horst R, Withka JM, Pryde DC, Liu S, Young GT.
Cho LT, et al. Among authors: alexandrou aj.
Structure. 2018 Apr 3;26(4):533-544.e3. doi: 10.1016/j.str.2018.02.017. Epub 2018 Mar 22.
Structure. 2018.
PMID: 29576321
Free article.
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The human ether-a'-go-go related gene (hERG) K+ channel blockade by the investigative selective-serotonin reuptake inhibitor CONA-437: limited dependence on S6 aromatic residues.
Alexandrou AJ, Milnes JT, Sun SZ, Fermini B, Kim SC, Jenkinson S, Leishman DJ, Witchel HJ, Hancox JC, Leaney JL.
Alexandrou AJ, et al.
J Physiol Pharmacol. 2014 Aug;65(4):511-23.
J Physiol Pharmacol. 2014.
PMID: 25179083
Free article.
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Mechanism of hERG K+ channel blockade by the fluoroquinolone antibiotic moxifloxacin.
Alexandrou AJ, Duncan RS, Sullivan A, Hancox JC, Leishman DJ, Witchel HJ, Leaney JL.
Alexandrou AJ, et al.
Br J Pharmacol. 2006 Apr;147(8):905-16. doi: 10.1038/sj.bjp.0706678.
Br J Pharmacol. 2006.
PMID: 16474415
Free PMC article.
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