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Page 1
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
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
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
[18F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptor.
Burns HD, Van Laere K, Sanabria-Bohórquez S, Hamill TG, Bormans G, Eng WS, Gibson R, Ryan C, Connolly B, Patel S, Krause S, Vanko A, Van Hecken A, Dupont P, De Lepeleire I, Rothenberg P, Stoch SA, Cote J, Hagmann WK, Jewell JP, Lin LS, Liu P, Goulet MT, Gottesdiener K, Wagner JA, de Hoon J, Mortelmans L, Fong TM, Hargreaves RJ. Burns HD, et al. Proc Natl Acad Sci U S A. 2007 Jun 5;104(23):9800-5. doi: 10.1073/pnas.0703472104. Epub 2007 May 29. Proc Natl Acad Sci U S A. 2007. PMID: 17535893 Free PMC article.
Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers.
Hamill TG, Krause S, Ryan C, Bonnefous C, Govek S, Seiders TJ, Cosford ND, Roppe J, Kamenecka T, Patel S, Gibson RE, Sanabria S, Riffel K, Eng W, King C, Yang X, Green MD, O'Malley SS, Hargreaves R, Burns HD. Hamill TG, et al. Among authors: eng w. Synapse. 2005 Jun 15;56(4):205-16. doi: 10.1002/syn.20147. Synapse. 2005. PMID: 15803497
Synthesis, characterization, and monkey PET studies of [¹⁸F]MK-1312, a PET tracer for quantification of mGluR1 receptor occupancy by MK-5435.
Hostetler ED, Eng W, Joshi AD, Sanabria-Bohórquez S, Kawamoto H, Ito S, O'Malley S, Krause S, Ryan C, Patel S, Williams M, Riffel K, Suzuki G, Ozaki S, Ohta H, Cook J, Burns HD, Hargreaves R. Hostetler ED, et al. Among authors: eng w. Synapse. 2011 Feb;65(2):125-35. doi: 10.1002/syn.20826. Synapse. 2011. PMID: 20524178
Evaluation of [¹⁸F]MK-0911, a positron emission tomography (PET) tracer for opioid receptor-like 1 (ORL1), in rhesus monkey and human.
Hostetler ED, Sanabria-Bohórquez S, Eng W, Joshi AD, Patel S, Gibson RE, O'Malley S, Krause SM, Ryan C, Riffel K, Bi S, Okamoto O, Kawamoto H, Ozaki S, Ohta H, de Groot T, Bormans G, Depré M, de Hoon J, De Lepeleire I, Reynders T, Cook JJ, Burns HD, Egan M, Cho W, van Laere K, Hargreaves RJ. Hostetler ED, et al. Among authors: eng w. Neuroimage. 2013 Mar;68:1-10. doi: 10.1016/j.neuroimage.2012.11.053. Epub 2012 Dec 11. Neuroimage. 2013. PMID: 23238431
144 results