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Page 1
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
Sternfeld F, Carling RW, Jelley RA, Ladduwahetty T, Merchant KJ, Moore KW, Reeve AJ, Street LJ, O'Connor D, Sohal B, Atack JR, Cook S, Seabrook G, Wafford K, Tattersall FD, Collinson N, Dawson GR, Castro JL, MacLeod AM. Sternfeld F, et al. Among authors: macleod am. J Med Chem. 2004 Apr 22;47(9):2176-9. doi: 10.1021/jm031076j. J Med Chem. 2004. PMID: 15084116
Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.
Street LJ, Sternfeld F, Jelley RA, Reeve AJ, Carling RW, Moore KW, McKernan RM, Sohal B, Cook S, Pike A, Dawson GR, Bromidge FA, Wafford KA, Seabrook GR, Thompson SA, Marshall G, Pillai GV, Castro JL, Atack JR, MacLeod AM. Street LJ, et al. Among authors: macleod am. J Med Chem. 2004 Jul 1;47(14):3642-57. doi: 10.1021/jm0407613. J Med Chem. 2004. PMID: 15214791
A new pyridazine series of GABAA alpha5 ligands.
van Niel MB, Wilson K, Adkins CH, Atack JR, Castro JL, Clarke DE, Fletcher S, Gerhard U, Mackey MM, Malpas S, Maubach K, Newman R, O'Connor D, Pillai GV, Simpson PB, Thomas SR, MacLeod AM. van Niel MB, et al. Among authors: macleod am. J Med Chem. 2005 Sep 22;48(19):6004-11. doi: 10.1021/jm050249x. J Med Chem. 2005. PMID: 16162003
Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction.
Jones P, Atack JR, Braun MP, Cato BP, Chambers MS, O'Connor D, Cook SM, Hobbs SC, Maxey R, Szekeres HJ, Szeto N, Wafford KA, MacLeod AM. Jones P, et al. Among authors: macleod am. Bioorg Med Chem Lett. 2006 Feb 15;16(4):872-5. doi: 10.1016/j.bmcl.2005.11.012. Epub 2005 Nov 21. Bioorg Med Chem Lett. 2006. PMID: 16303300
In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist.
Atack JR, Maubach KA, Wafford KA, O'Connor D, Rodrigues AD, Evans DC, Tattersall FD, Chambers MS, MacLeod AM, Eng WS, Ryan C, Hostetler E, Sanabria SM, Gibson RE, Krause S, Burns HD, Hargreaves RJ, Agrawal NG, McKernan RM, Murphy MG, Gingrich K, Dawson GR, Musson DG, Petty KJ. Atack JR, et al. Among authors: macleod am. J Pharmacol Exp Ther. 2009 Nov;331(2):470-84. doi: 10.1124/jpet.109.157636. Epub 2009 Aug 24. J Pharmacol Exp Ther. 2009. PMID: 19704033
243 results