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Items: 1 to 20 of 128

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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.

J Psychopharmacol. 2011 Mar;25(3):329-44. doi: 10.1177/0269881109354928. Epub 2010 Feb 15.

PMID:
20156926
4.

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
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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.

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

PMID:
16183706
7.
8.

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
9.

The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics.

Atack JR.

Expert Opin Investig Drugs. 2005 May;14(5):601-18. Review.

PMID:
15926867
10.

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.

PMID:
19779131
11.

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.

12.

Subtype-selective GABA(A) receptor modulation yields a novel pharmacological profile: the design and development of TPA023.

Atack JR.

Adv Pharmacol. 2009;57:137-85. doi: 10.1016/S1054-3589(08)57004-9. Epub 2009 Nov 27. Review.

PMID:
20230761
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Reinforcing effects of compounds lacking intrinsic efficacy at α1 subunit-containing GABAA receptor subtypes in midazolam- but not cocaine-experienced rhesus monkeys.

Shinday NM, Sawyer EK, Fischer BD, Platt DM, Licata SC, Atack JR, Dawson GR, Reynolds DS, Rowlett JK.

Neuropsychopharmacology. 2013 May;38(6):1006-14. doi: 10.1038/npp.2012.265. Epub 2012 Dec 27.

16.

Anxioselective anxiolytics: on a quest for the Holy Grail.

Skolnick P.

Trends Pharmacol Sci. 2012 Nov;33(11):611-20. doi: 10.1016/j.tips.2012.08.003. Epub 2012 Sep 14. Review.

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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
19.

Antinociceptive Effects of a Novel α2/α3-Subtype Selective GABAA Receptor Positive Allosteric Modulator.

Lewter LA, Fisher JL, Siemian JN, Methuku KR, Poe MM, Cook JM, Li JX.

ACS Chem Neurosci. 2017 Jun 21;8(6):1305-1312. doi: 10.1021/acschemneuro.6b00447. Epub 2017 Feb 13.

20.

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.

J Neurosci. 2005 Nov 16;25(46):10682-8.

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