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Page 1
The discovery of the benzazepine class of histamine H3 receptor antagonists.
Wilson DM, Apps J, Bailey N, Bamford MJ, Beresford IJ, Briggs MA, Calver AR, Crook B, Davis RP, Davis S, Dean DK, Harris L, Heightman TD, Panchal T, Parr CA, Quashie N, Steadman JG, Schogger J, Sehmi SS, Stean TO, Takle AK, Trail BK, White T, Witherington J, Worby A, Medhurst AD. Wilson DM, et al. Among authors: medhurst ad. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6897-901. doi: 10.1016/j.bmcl.2013.09.089. Epub 2013 Oct 5. Bioorg Med Chem Lett. 2013. PMID: 24161834
Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists.
Ahmed M, Briggs MA, Bromidge SM, Buck T, Campbell L, Deeks NJ, Garner A, Gordon L, Hamprecht DW, Holland V, Johnson CN, Medhurst AD, Mitchell DJ, Moss SF, Powles J, Seal JT, Stean TO, Stemp G, Thompson M, Trail B, Upton N, Winborn K, Witty DR. Ahmed M, et al. Among authors: medhurst ad. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4867-71. doi: 10.1016/j.bmcl.2005.06.107. Bioorg Med Chem Lett. 2005. PMID: 16143522
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: medhurst sj. 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
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. 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
Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists.
Trani G, Baddeley SM, Briggs MA, Chuang TT, Deeks NJ, Johnson CN, Khazragi AA, Mead TL, Medhurst AD, Milner PH, Quinn LP, Ray AM, Rivers DA, Stean TO, Stemp G, Trail BK, Witty DR. Trani G, et al. Among authors: medhurst ad. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5698-700. doi: 10.1016/j.bmcl.2008.08.010. Epub 2008 Aug 7. Bioorg Med Chem Lett. 2008. PMID: 18793848
Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
Wilson DM, Apps J, Bailey N, Bamford MJ, Beresford IJ, Brackenborough K, Briggs MA, Brough S, Calver AR, Crook B, Davis RK, Davis RP, Davis S, Dean DK, Harris L, Heslop T, Holland V, Jeffrey P, Panchal TA, Parr CA, Quashie N, Schogger J, Sehmi SS, Stean TO, Steadman JG, Trail B, Wald J, Worby A, Takle AK, Witherington J, Medhurst AD. Wilson DM, et al. Among authors: medhurst ad. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6890-6. doi: 10.1016/j.bmcl.2013.09.090. Epub 2013 Oct 5. Bioorg Med Chem Lett. 2013. PMID: 24269482
Preclinical investigations into the antipsychotic potential of the novel histamine H3 receptor antagonist GSK207040.
Southam E, Cilia J, Gartlon JE, Woolley ML, Lacroix LP, Jennings CA, Cluderay JE, Reavill C, Rourke C, Wilson DM, Dawson LA, Medhurst AD, Jones DN. Southam E, et al. Among authors: medhurst ad. Psychopharmacology (Berl). 2009 Jan;201(4):483-94. doi: 10.1007/s00213-008-1310-9. Epub 2008 Sep 3. Psychopharmacology (Berl). 2009. PMID: 18762914
Differences in the central nervous system distribution and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand binding, site-directed mutagenesis, and molecular modeling.
Hirst WD, Abrahamsen B, Blaney FE, Calver AR, Aloj L, Price GW, Medhurst AD. Hirst WD, et al. Among authors: medhurst ad. Mol Pharmacol. 2003 Dec;64(6):1295-308. doi: 10.1124/mol.64.6.1295. Mol Pharmacol. 2003. PMID: 14645659
67 results