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2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.
Kassick AJ, Jiang J, Bunda J, Wilson D, Bao J, Lu H, Lin P, Ball RG, Doss GA, Tong X, Tsao KL, Wang H, Chicchi G, Karanam B, Tschirret-Guth R, Samuel K, Hora DF, Kumar S, Madeira M, Eng W, Hargreaves R, Purcell M, Gantert L, Cook J, DeVita RJ, Mills SG. Kassick AJ, et al. Among authors: eng w. J Med Chem. 2013 Jul 25;56(14):5940-8. doi: 10.1021/jm400751p. Epub 2013 Jul 9. J Med Chem. 2013. PMID: 23808489
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.
Jiang J, Bunda JL, Doss GA, Chicchi GG, Kurtz MM, Tsao KL, Tong X, Zheng S, Upthagrove A, Samuel K, Tschirret-Guth R, Kumar S, Wheeldon A, Carlson EJ, Hargreaves R, Burns D, Hamill T, Ryan C, Krause SM, Eng W, DeVita RJ, Mills SG. Jiang J, et al. Among authors: eng w. J Med Chem. 2009 May 14;52(9):3039-46. doi: 10.1021/jm8016514. J Med Chem. 2009. PMID: 19354254
Discovery of [¹¹C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors.
Cox CD, Hostetler ED, Flores BA, Evelhoch JL, Fan H, Gantert L, Holahan M, Eng W, Joshi A, McGaughey G, Meng X, Purcell M, Raheem IT, Riffel K, Yan Y, Renger JJ, Smith SM, Coleman PJ. Cox CD, et al. Among authors: eng w. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4893-4898. doi: 10.1016/j.bmcl.2015.05.080. Epub 2015 Jun 1. Bioorg Med Chem Lett. 2015. PMID: 26077491
Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use.
Liu P, Lin LS, Hamill TG, Jewell JP, Lanza TJ Jr, Gibson RE, Krause SM, Ryan C, Eng W, Sanabria S, Tong X, Wang J, Levorse DA, Owens KA, Fong TM, Shen CP, Lao J, Kumar S, Yin W, Payack JF, Springfield SA, Hargreaves R, Burns HD, Goulet MT, Hagmann WK. Liu P, et al. Among authors: eng w. J Med Chem. 2007 Jul 26;50(15):3427-30. doi: 10.1021/jm070131b. Epub 2007 Jul 3. J Med Chem. 2007. PMID: 17608398
Preclinical Characterization of the Phosphodiesterase 10A PET Tracer [(11)C]MK-8193.
Hostetler ED, Fan H, Joshi AD, Zeng Z, Eng W, Gantert L, Holahan M, Meng X, Miller P, O'Malley S, Purcell M, Riffel K, Salinas C, Williams M, Ma B, Buist N, Smith SM, Coleman PJ, Cox CD, Flores BA, Raheem IT, Cook JJ, Evelhoch JL. Hostetler ED, et al. Among authors: eng w. Mol Imaging Biol. 2016 Aug;18(4):579-87. doi: 10.1007/s11307-015-0910-0. Mol Imaging Biol. 2016. PMID: 26596571
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
144 results