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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: castro jl. J Med Chem. 2004 Apr 22;47(9):2176-9. doi: 10.1021/jm031076j. J Med Chem. 2004. PMID: 15084116
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
Collins I, Moyes C, Davey WB, Rowley M, Bromidge FA, Quirk K, Atack JR, McKernan RM, Thompson SA, Wafford K, Dawson GR, Pike A, Sohal B, Tsou NN, Ball RG, Castro JL. Collins I, et al. Among authors: castro jl. J Med Chem. 2002 Apr 25;45(9):1887-900. doi: 10.1021/jm0110789. J Med Chem. 2002. PMID: 11960500
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
Carling RW, Moore KW, Street LJ, Wild D, Isted C, Leeson PD, Thomas S, O'Connor D, McKernan RM, Quirk K, Cook SM, Atack JR, Wafford KA, Thompson SA, Dawson GR, Ferris P, Castro JL. Carling RW, et al. Among authors: castro jl. J Med Chem. 2004 Mar 25;47(7):1807-22. doi: 10.1021/jm031020p. J Med Chem. 2004. PMID: 15027873
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor.
Mitchinson A, Atack JR, Blurton P, Carling RW, Castro JL, Curley KS, Russell MG, Marshall G, McKernan RM, Moore KW, Narquizian R, Smith A, Street LJ, Thompson SA, Wafford K. Mitchinson A, et al. Among authors: castro jl. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3441-4. doi: 10.1016/j.bmcl.2004.04.085. Bioorg Med Chem Lett. 2004. PMID: 15177449
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: castro jl. J Med Chem. 2004 Jul 1;47(14):3642-57. doi: 10.1021/jm0407613. J Med Chem. 2004. PMID: 15214791
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.
Russell MG, Carling RW, Atack JR, Bromidge FA, Cook SM, Hunt P, Isted C, Lucas M, McKernan RM, Mitchinson A, Moore KW, Narquizian R, Macaulay AJ, Thomas D, Thompson SA, Wafford KA, Castro JL. Russell MG, et al. Among authors: castro jl. J Med Chem. 2005 Mar 10;48(5):1367-83. doi: 10.1021/jm040883v. J Med Chem. 2005. PMID: 15743180
Pyrazolopyridinones as functionally selective GABAA ligands.
Blackaby WP, Atack JR, Bromidge F, Lewis R, Russell MG, Smith A, Wafford K, McKernan RM, Street LJ, Castro JL. Blackaby WP, et al. Among authors: castro jl. Bioorg Med Chem Lett. 2005 Nov 15;15(22):4998-5002. doi: 10.1016/j.bmcl.2005.08.006. Bioorg Med Chem Lett. 2005. PMID: 16153832
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: castro jl. J Med Chem. 2005 Sep 22;48(19):6004-11. doi: 10.1021/jm050249x. J Med Chem. 2005. PMID: 16162003
7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.
Carling RW, Madin A, Guiblin A, Russell MG, Moore KW, Mitchinson A, Sohal B, Pike A, Cook SM, Ragan IC, McKernan RM, Quirk K, Ferris P, Marshall G, Thompson SA, Wafford KA, Dawson GR, Atack JR, Harrison T, Castro JL, Street LJ. Carling RW, et al. Among authors: castro jl. J Med Chem. 2005 Nov 17;48(23):7089-92. doi: 10.1021/jm058034a. J Med Chem. 2005. PMID: 16279764
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Goodacre SC, Hallett DJ, Carling RW, Castro JL, Reynolds DS, Pike A, Wafford KA, Newman R, Atack JR, Street LJ. Goodacre SC, et al. Among authors: castro jl. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1582-5. doi: 10.1016/j.bmcl.2005.12.027. Epub 2005 Dec 27. Bioorg Med Chem Lett. 2006. PMID: 16384707
200 results