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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
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
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
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
van Niel MB, Collins I, Beer MS, Broughton HB, Cheng SK, Goodacre SC, Heald A, Locker KL, MacLeod AM, Morrison D, Moyes CR, O'Connor D, Pike A, Rowley M, Russell MG, Sohal B, Stanton JA, Thomas S, Verrier H, Watt AP, Castro JL. van Niel MB, et al. Among authors: castro jl. J Med Chem. 1999 Jun 17;42(12):2087-104. doi: 10.1021/jm981133m. J Med Chem. 1999. PMID: 10377215
2,7-diazabicyclo[3.3.0]octanes as novel h5-HT receptor agonists.
Russell MG, Beer MS, Stanton JA, Sohal B, Mortishire-Smith RJ, Castro JL. Russell MG, et al. Among authors: castro jl. Bioorg Med Chem Lett. 1999 Sep 6;9(17):2491-6. doi: 10.1016/s0960-894x(99)00409-6. Bioorg Med Chem Lett. 1999. PMID: 10498195
199 results