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GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models.
Medhurst AD, Atkins AR, Beresford IJ, Brackenborough K, Briggs MA, Calver AR, Cilia J, Cluderay JE, Crook B, Davis JB, Davis RK, Davis RP, Dawson LA, Foley AG, Gartlon J, Gonzalez MI, Heslop T, Hirst WD, Jennings C, Jones DN, Lacroix LP, Martyn A, Ociepka S, Ray A, Regan CM, Roberts JC, Schogger J, Southam E, Stean TO, Trail BK, Upton N, Wadsworth G, Wald JA, White T, Witherington J, Woolley ML, Worby A, Wilson DM. Medhurst AD, et al. Among authors: regan cm. J Pharmacol Exp Ther. 2007 Jun;321(3):1032-45. doi: 10.1124/jpet.107.120311. Epub 2007 Feb 27. J Pharmacol Exp Ther. 2007. PMID: 17327487
SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models.
Hirst WD, Stean TO, Rogers DC, Sunter D, Pugh P, Moss SF, Bromidge SM, Riley G, Smith DR, Bartlett S, Heidbreder CA, Atkins AR, Lacroix LP, Dawson LA, Foley AG, Regan CM, Upton N. Hirst WD, et al. Among authors: regan cm. Eur J Pharmacol. 2006 Dec 28;553(1-3):109-19. doi: 10.1016/j.ejphar.2006.09.049. Epub 2006 Sep 29. Eur J Pharmacol. 2006. PMID: 17069795
Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and capsaicin-induced secondary allodynia in rats.
Medhurst AD, 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. Medhurst AD, et al. Among authors: regan cm. Biochem Pharmacol. 2007 Apr 15;73(8):1182-94. doi: 10.1016/j.bcp.2007.01.007. Epub 2007 Jan 7. Biochem Pharmacol. 2007. PMID: 17276409
The selective 5-HT6 receptor antagonists SB-271046 and SB-399885 potentiate NCAM PSA immunolabeling of dentate granule cells, but not neurogenesis, in the hippocampal formation of mature Wistar rats.
Foley AG, Hirst WD, Gallagher HC, Barry C, Hagan JJ, Upton N, Walsh FS, Hunter AJ, Regan CM. Foley AG, et al. Among authors: regan cm. Neuropharmacology. 2008 Jun;54(8):1166-74. doi: 10.1016/j.neuropharm.2008.03.012. Epub 2008 Apr 1. Neuropharmacology. 2008. PMID: 18455201
152 results