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Quantitative measurement of changes in amyloid-beta(40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide].
Best JD, Jay MT, Otu F, Ma J, Nadin A, Ellis S, Lewis HD, Pattison C, Reilly M, Harrison T, Shearman MS, Williamson TL, Atack JR. Best JD, et al. Among authors: atack jr. J Pharmacol Exp Ther. 2005 May;313(2):902-8. doi: 10.1124/jpet.104.081174. Epub 2005 Mar 2. J Pharmacol Exp Ther. 2005. PMID: 15743924
In vivo characterization of Abeta(40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat.
Best JD, Jay MT, Otu F, Churcher I, Reilly M, Morentin-Gutierrez P, Pattison C, Harrison T, Shearman MS, Atack JR. Best JD, et al. Among authors: atack jr. J Pharmacol Exp Ther. 2006 May;317(2):786-90. doi: 10.1124/jpet.105.100271. Epub 2006 Jan 27. J Pharmacol Exp Ther. 2006. PMID: 16443723
The novel gamma secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of notch-related pathology in the Tg2576 mouse.
Best JD, Smith DW, Reilly MA, O'Donnell R, Lewis HD, Ellis S, Wilkie N, Rosahl TW, Laroque PA, Boussiquet-Leroux C, Churcher I, Atack JR, Harrison T, Shearman MS. Best JD, et al. Among authors: atack jr. J Pharmacol Exp Ther. 2007 Feb;320(2):552-8. doi: 10.1124/jpet.106.114330. Epub 2006 Nov 10. J Pharmacol Exp Ther. 2007. PMID: 17099072
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
An inverse agonist selective for alpha5 subunit-containing GABAA receptors enhances cognition.
Dawson GR, Maubach KA, Collinson N, Cobain M, Everitt BJ, MacLeod AM, Choudhury HI, McDonald LM, Pillai G, Rycroft W, Smith AJ, Sternfeld F, Tattersall FD, Wafford KA, Reynolds DS, Seabrook GR, Atack JR. Dawson GR, et al. Among authors: atack jr. J Pharmacol Exp Ther. 2006 Mar;316(3):1335-45. doi: 10.1124/jpet.105.092320. Epub 2005 Dec 2. J Pharmacol Exp Ther. 2006. PMID: 16326923
Enhanced learning and memory and altered GABAergic synaptic transmission in mice lacking the alpha 5 subunit of the GABAA receptor.
Collinson N, Kuenzi FM, Jarolimek W, Maubach KA, Cothliff R, Sur C, Smith A, Otu FM, Howell O, Atack JR, McKernan RM, Seabrook GR, Dawson GR, Whiting PJ, Rosahl TW. Collinson N, et al. Among authors: atack jr. J Neurosci. 2002 Jul 1;22(13):5572-80. doi: 10.1523/JNEUROSCI.22-13-05572.2002. J Neurosci. 2002. PMID: 12097508 Free PMC article.
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
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
187 results