Characterization of three diaminopyrimidines as potent and selective antagonists of P2X3 and P2X2/3 receptors within vivoefficacy in a pain model

Autor: Andrew J. Powell, SJ Medhurst, I Lago, YH Chen, Caterina Virginio, Elisa Ballini, A Buson, Laura Aldegheri, Wolfgang Jarolimek, Angelo Giacometti, Scott G. Summerfield, Corrado Carignani

Publikováno v: British Journal of Pharmacology. 163:1315-1325

BACKGROUND AND PURPOSE P2X3 and P2X2/3 receptors are highly localized on the peripheral and central pathways of nociceptive signal transmission. The discovery of A-317491 allowed their validation as chronic inflammatory and neuropathic pain targets,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5cfc5cb5618f6069f6fd999a3e92cfa6
https://doi.org/10.1111/j.1476-5381.2011.01322.x

Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor.

Autor: Abberley L; Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom., Bebius A, Beswick PJ, Billinton A, Collis KL, Dean DK, Fonfria E, Gleave RJ, Medhurst SJ, Michel AD, Moses AP, Patel S, Roman SA, Scoccitti T, Smith B, Steadman JG, Walter DS

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Nov 15; Vol. 20 (22), pp. 6370-4. Date of Electronic Publication: 2010 Sep 22.

Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor.

Autor: Beswick PJ; Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex CM19 5AW, UK., Billinton A, Chambers LJ, Dean DK, Fonfria E, Gleave RJ, Medhurst SJ, Michel AD, Moses AP, Patel S, Roman SA, Roomans S, Senger S, Stevens AJ, Walter DS

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Aug 01; Vol. 20 (15), pp. 4653-6. Date of Electronic Publication: 2010 Jun 08.

Novel histamine H3 receptor antagonists GSK189254 and GSK334429 are efficacious in surgically-induced and virally-induced rat models of neuropathic pain.

Autor: Medhurst SJ; Neurology and GI Centre of Excellence for Drug Discovery, GlaxoSmithKline, Third Avenue, Harlow, Essex CM19 5AW, UK School of Veterinary Medicine, College of Medicine and Veterinary Medicine, University of Edinburgh, Summerhall, Edinburgh EH9 1QH, UK., Collins SD, Billinton A, Bingham S, Dalziel RG, Brass A, Roberts JC, Medhurst AD, Chessell IP

Publikováno v: Pain [Pain] 2008 Aug 15; Vol. 138 (1), pp. 61-69. Date of Electronic Publication: 2007 Dec 31.

Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and capsaicin-induced secondary allodynia in rats.

Autor: Medhurst AD; Neurology and GI Centre of Excellence for Drug Discovery, GlaxoSmithKline, Third Avenue, Harlow, Essex CM19 5AW, UK. andy.medhurst@gsk.com, Briggs MA, Bruton G, Calver AR, Chessell I, Crook B, Davis JB, Davis RP, Foley AG, Heslop T, Hirst WD, Medhurst SJ, Ociepka S, Ray A, Regan CM, Sargent B, Schogger J, Stean TO, Trail BK, Upton N, White T, Orlek B, Wilson DM

Publikováno v: Biochemical pharmacology [Biochem Pharmacol] 2007 Apr 15; Vol. 73 (8), pp. 1182-94. Date of Electronic Publication: 2007 Jan 07.