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MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans.
Atack JR, Wafford KA, Street LJ, Dawson GR, Tye S, Van Laere K, Bormans G, Sanabria-Bohórquez SM, De Lepeleire I, de Hoon JN, Van Hecken A, Burns HD, McKernan RM, Murphy MG, Hargreaves RJ. Atack JR, et al. Among authors: street lj. J Psychopharmacol. 2011 Mar;25(3):314-28. doi: 10.1177/0269881109354927. Epub 2010 Feb 10. J Psychopharmacol. 2011. PMID: 20147571 Clinical Trial.
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. 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
Evidence for a significant role of alpha 3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines.
Dias R, Sheppard WF, Fradley RL, Garrett EM, Stanley JL, Tye SJ, Goodacre S, Lincoln RJ, Cook SM, Conley R, Hallett D, Humphries AC, Thompson SA, Wafford KA, Street LJ, Castro JL, Whiting PJ, Rosahl TW, Atack JR, McKernan RM, Dawson GR, Reynolds DS. Dias R, et al. Among authors: street lj. J Neurosci. 2005 Nov 16;25(46):10682-8. doi: 10.1523/JNEUROSCI.1166-05.2005. J Neurosci. 2005. PMID: 16291941 Free PMC article.
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: street lj. J Psychopharmacol. 2011 Mar;25(3):329-44. doi: 10.1177/0269881109354928. Epub 2010 Feb 15. J Psychopharmacol. 2011. PMID: 20156926 Clinical Trial.
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: street lj. 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: street lj. 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. J Med Chem. 2004 Jul 1;47(14):3642-57. doi: 10.1021/jm0407613. J Med Chem. 2004. PMID: 15214791
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: street lj. 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
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: street lj. J Med Chem. 2005 Nov 17;48(23):7089-92. doi: 10.1021/jm058034a. J Med Chem. 2005. PMID: 16279764
66 results