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Items: 1 to 20 of 105

1.

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. doi: 10.1124/jpet.109.158303. Epub 2009 Sep 29.

2.

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, Vega JM, Vessy L, Scott-Stevens P, Beech JS, Baron JC, Sohal B, Schrag ML, Aigbirhio FI, McKernan RM, Hargreaves RJ.

J Pharmacol Exp Ther. 2010 Jan;332(1):17-25. doi: 10.1124/jpet.109.157909. Epub 2009 Sep 24.

3.

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.

J Pharmacol Exp Ther. 2006 Jan;316(1):410-22. Epub 2005 Sep 23.

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Pharmacodynamic and pharmacokinetic effects of TPA023, a GABA(A) alpha(2,3) subtype-selective agonist, compared to lorazepam and placebo in healthy volunteers.

de Haas SL, de Visser SJ, van der Post JP, de Smet M, Schoemaker RC, Rijnbeek B, Cohen AF, Vega JM, Agrawal NG, Goel TV, Simpson RC, Pearson LK, Li S, Hesney M, Murphy MG, van Gerven JM.

J Psychopharmacol. 2007 Jun;21(4):374-83. Epub 2006 Nov 8.

PMID:
17092968
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Changes in relative potency among positive GABA(A) receptor modulators upon discontinuation of chronic benzodiazepine treatment in rhesus monkeys.

McMahon LR, Javors MA, France CP.

Psychopharmacology (Berl). 2007 May;192(1):135-45. Epub 2007 Jan 24.

PMID:
17245585
11.

In vivo characterization and dynamic receptor occupancy imaging of TPA023B, an alpha 2/alpha 3/alpha 5 subtype selective gamma-aminobutyric acid-a partial agonist.

Van Laere K, Bormans G, Sanabria-Bohórquez SM, de Groot T, Dupont P, De Lepeleire I, de Hoon J, Mortelmans L, Hargreaves RJ, Atack JR, Burns HD.

Biol Psychiatry. 2008 Jul 15;64(2):153-61. doi: 10.1016/j.biopsych.2008.01.021. Epub 2008 Mar 14.

PMID:
18339360
12.

Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site.

Atack JR.

Curr Drug Targets CNS Neurol Disord. 2003 Aug;2(4):213-32. Review.

PMID:
12871032
13.

Discriminative stimulus properties of GABAA receptor positive allosteric modulators TPA023, ocinaplon and NG2-73 in rats trained to discriminate chlordiazepoxide or zolpidem.

Vinkers CH, Olivier B, Hanania T, Min W, Schreiber R, Hopkins SC, Campbell U, Paterson N.

Eur J Pharmacol. 2011 Oct 1;668(1-2):190-3. doi: 10.1016/j.ejphar.2011.06.054. Epub 2011 Jul 8.

PMID:
21762686
14.

Discriminative stimulus effects of L-838,417 (7-tert-butyl-3-(2,5-difluoro-phenyl)-6-(2-methyl-2H-[1,2,4]triazol-3-ylmethoxy)-[1,2,4]triazolo[4,3-b]pyridazine): role of GABA(A) receptor subtypes.

Licata SC, Platt DM, Rüedi-Bettschen D, Atack JR, Dawson GR, Van Linn ML, Cook JM, Rowlett JK.

Neuropharmacology. 2010 Feb;58(2):357-64. doi: 10.1016/j.neuropharm.2009.10.004. Epub 2009 Oct 22.

15.

Reversal of ketamine-induced working memory impairments by the GABAAalpha2/3 agonist TPA023.

Castner SA, Arriza JL, Roberts JC, Mrzljak L, Christian EP, Williams GV.

Biol Psychiatry. 2010 May 15;67(10):998-1001. doi: 10.1016/j.biopsych.2010.01.001. Epub 2010 Feb 26.

PMID:
20189164
16.

In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist.

Atack JR, Maubach KA, Wafford KA, O'Connor D, Rodrigues AD, Evans DC, Tattersall FD, Chambers MS, MacLeod AM, Eng WS, Ryan C, Hostetler E, Sanabria SM, Gibson RE, Krause S, Burns HD, Hargreaves RJ, Agrawal NG, McKernan RM, Murphy MG, Gingrich K, Dawson GR, Musson DG, Petty KJ.

J Pharmacol Exp Ther. 2009 Nov;331(2):470-84. doi: 10.1124/jpet.109.157636. Epub 2009 Aug 24.

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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.

J Psychopharmacol. 2011 Mar;25(3):314-28. doi: 10.1177/0269881109354927. Epub 2010 Feb 10.

PMID:
20147571
20.

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.

J Med Chem. 2005 Nov 17;48(23):7089-92.

PMID:
16279764
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