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Page 1
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. Van Laere K, et al. Among authors: atack jr. Biol Psychiatry. 2008 Jul 15;64(2):153-61. doi: 10.1016/j.biopsych.2008.01.021. Epub 2008 Mar 14. Biol Psychiatry. 2008. PMID: 18339360 Clinical Trial.
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. J Psychopharmacol. 2011 Mar;25(3):314-28. doi: 10.1177/0269881109354927. Epub 2010 Feb 10. J Psychopharmacol. 2011. PMID: 20147571 Clinical Trial.
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. J Psychopharmacol. 2011 Mar;25(3):329-44. doi: 10.1177/0269881109354928. Epub 2010 Feb 15. J Psychopharmacol. 2011. PMID: 20156926 Clinical Trial.
Occupancy of human brain GABA(A) receptors by the novel α5 subtype-selective benzodiazepine site inverse agonist α5IA as measured using [¹¹C]flumazenil PET imaging.
Eng W, Atack JR, Bergstrom M, Sanabria S, Appel L, Dawson GR, Sciberras D, Hargreaves RJ, Langstrom B, Burns HD. Eng W, et al. Among authors: atack jr. Neuropharmacology. 2010 Dec;59(7-8):635-9. doi: 10.1016/j.neuropharm.2010.07.024. Epub 2010 Aug 7. Neuropharmacology. 2010. PMID: 20696179
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. Atack JR, et al. J Pharmacol Exp Ther. 2010 Jan;332(1):17-25. doi: 10.1124/jpet.109.157909. Epub 2009 Sep 24. J Pharmacol Exp Ther. 2010. PMID: 19779131
Comparison of lorazepam [7-chloro-5-(2-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one] occupancy of rat brain gamma-aminobutyric acid(A) receptors measured using in vivo [3H]flumazenil (8-fluoro 5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid ethyl ester) binding and [11C]flumazenil micro-positron emission tomography.
Atack JR, Scott-Stevens P, Beech JS, Fryer TD, Hughes JL, Cleij MC, Baron JC, Clark JC, Hargreaves RJ, Aigbirhio FI. Atack JR, et al. J Pharmacol Exp Ther. 2007 Mar;320(3):1030-7. doi: 10.1124/jpet.106.114884. Epub 2006 Dec 12. J Pharmacol Exp Ther. 2007. PMID: 17164474
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. Atack JR, et al. J Pharmacol Exp Ther. 2009 Nov;331(2):470-84. doi: 10.1124/jpet.109.157636. Epub 2009 Aug 24. J Pharmacol Exp Ther. 2009. PMID: 19704033
187 results