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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: krause sm. J Med Chem. 2009 May 14;52(9):3039-46. doi: 10.1021/jm8016514. J Med Chem. 2009. PMID: 19354254
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: krause sm. J Med Chem. 2007 Jul 26;50(15):3427-30. doi: 10.1021/jm070131b. Epub 2007 Jul 3. J Med Chem. 2007. PMID: 17608398
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. Synapse. 2005 Jun 15;56(4):205-16. doi: 10.1002/syn.20147. Synapse. 2005. PMID: 15803497
[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.
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. Among authors: krause s. 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
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: krause sm. Neuroimage. 2013 Mar;68:1-10. doi: 10.1016/j.neuroimage.2012.11.053. Epub 2012 Dec 11. Neuroimage. 2013. PMID: 23238431
64 results