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TPA023 [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], an agonist selective for alpha2- and alpha3-containing GABAA receptors, is a nonsedating anxiolytic in rodents and primates.
Atack JR, Wafford KA, Tye SJ, Cook SM, Sohal B, Pike A, Sur C, Melillo D, Bristow L, Bromidge F, Ragan I, Kerby J, Street L, Carling R, Castro JL, Whiting P, Dawson GR, McKernan RM. Atack JR, et al. Among authors: carling r. J Pharmacol Exp Ther. 2006 Jan;316(1):410-22. doi: 10.1124/jpet.105.089920. Epub 2005 Sep 23. J Pharmacol Exp Ther. 2006. PMID: 16183706
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. J Med Chem. 2004 Mar 25;47(7):1807-22. doi: 10.1021/jm031020p. J Med Chem. 2004. PMID: 15027873
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: carling rw. 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: carling rw. J Med Chem. 2005 Mar 10;48(5):1367-83. doi: 10.1021/jm040883v. J Med Chem. 2005. PMID: 15743180
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. 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: carling rw. 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
Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype.
McKernan RM, Rosahl TW, Reynolds DS, Sur C, Wafford KA, Atack JR, Farrar S, Myers J, Cook G, Ferris P, Garrett L, Bristow L, Marshall G, Macaulay A, Brown N, Howell O, Moore KW, Carling RW, Street LJ, Castro JL, Ragan CI, Dawson GR, Whiting PJ. McKernan RM, et al. Among authors: carling rw. Nat Neurosci. 2000 Jun;3(6):587-92. doi: 10.1038/75761. Nat Neurosci. 2000. PMID: 10816315
Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist.
Atack JR, Hallett DJ, Tye S, Wafford KA, Ryan C, Sanabria-Bohórquez SM, Eng WS, Gibson RE, Burns HD, Dawson GR, Carling RW, Street LJ, Pike A, De Lepeleire I, Van Laere K, Bormans G, de Hoon JN, Van Hecken A, McKernan RM, Murphy MG, Hargreaves RJ. Atack JR, et al. Among authors: carling rw. J Psychopharmacol. 2011 Mar;25(3):329-44. doi: 10.1177/0269881109354928. Epub 2010 Feb 15. J Psychopharmacol. 2011. PMID: 20156926 Clinical Trial.
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: carling rw. J Med Chem. 2004 Apr 22;47(9):2176-9. doi: 10.1021/jm031076j. J Med Chem. 2004. PMID: 15084116
73 results