7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol... [J Med Chem. 2005] - PubMed

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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. [J Pharmacol Exp Ther. 2006]
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, et al. J Pharmacol Exp Ther. 2006 Jan; 316(1):410-22. Epub 2005 Sep 23.
Review GABAA receptor subtype-selective modulators. I. α2/α3-selective agonists as non-sedating anxiolytics. [Curr Top Med Chem. 2011]
Review GABAA receptor subtype-selective modulators. I. α2/α3-selective agonists as non-sedating anxiolytics.
Atack JR. Curr Top Med Chem. 2011; 11(9):1176-202.
Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 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 (TPA023) in rats, primates, and humans. [J Pharmacol Exp Ther. 2010]
Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 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 (TPA023) in rats, primates, and humans.
Atack JR, Wong DF, Fryer TD, Ryan C, Sanabria S, Zhou Y, Dannals RF, Eng WS, Gibson RE, Burns HD, et al. J Pharmacol Exp Ther. 2010 Jan; 332(1):17-25. Epub 2009 Sep 24.
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. [J Med Chem. 2004]
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, et al. J Med Chem. 2004 Mar 25; 47(7):1807-22.
Review GABAA receptor subtype-selective modulators. II. α5-selective inverse agonists for cognition enhancement. [Curr Top Med Chem. 2011]
Review GABAA receptor subtype-selective modulators. II. α5-selective inverse agonists for cognition enhancement.
Atack JR. Curr Top Med Chem. 2011; 11(9):1203-14.

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Cited by 5 PubMed Central articles

GABA(A) receptor α subunits differentially contribute to diazepam tolerance after chronic treatment. [PLoS One. 2012]
GABA(A) receptor α subunits differentially contribute to diazepam tolerance after chronic treatment.
Vinkers CH, van Oorschot R, Nielsen EØ, Cook JM, Hansen HH, Groenink L, Olivier B, Mirza NR. PLoS One. 2012; 7(8):e43054. Epub 2012 Aug 13.
Review Use of multicomponent reactions in developing small-molecule tools to study GABAA receptor mechanism and function. [Future Med Chem. 2011]
Review Use of multicomponent reactions in developing small-molecule tools to study GABAA receptor mechanism and function.
Lewis RW, Hess GP, Ganem B. Future Med Chem. 2011 Feb; 3(2):243-50.
Reducing abuse liability of GABAA/benzodiazepine ligands via selective partial agonist efficacy at alpha1 and alpha2/3 subtypes. [J Pharmacol Exp Ther. 2010]
Reducing abuse liability of GABAA/benzodiazepine ligands via selective partial agonist efficacy at alpha1 and alpha2/3 subtypes.
Ator NA, Atack JR, Hargreaves RJ, Burns HD, Dawson GR. J Pharmacol Exp Ther. 2010 Jan; 332(1):4-16. Epub 2009 Sep 29.

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7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl...
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.
J Med Chem. 2005 Nov 17 ;48(23):7089-92.

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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.

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