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[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents.
Deskus JA, Dischino DD, Mattson RJ, Ditta JL, Parker MF, Denhart DJ, Zuev D, Huang H, Hartz RA, Ahuja VT, Wong H, Mattson GK, Molski TF, Grace JE Jr, Zueva L, Nielsen JM, Dulac H, Li YW, Guaraldi M, Azure M, Onthank D, Hayes M, Wexler E, McDonald J, Lodge NJ, Bronson JJ, Macor JE. Deskus JA, et al. Among authors: grace je jr. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6651-5. doi: 10.1016/j.bmcl.2012.08.112. Epub 2012 Sep 7. Bioorg Med Chem Lett. 2012. PMID: 23010264
P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice.
Meredith JE Jr, Thompson LA, Toyn JH, Marcin L, Barten DM, Marcinkeviciene J, Kopcho L, Kim Y, Lin A, Guss V, Burton C, Iben L, Polson C, Cantone J, Ford M, Drexler D, Fiedler T, Lentz KA, Grace JE Jr, Kolb J, Corsa J, Pierdomenico M, Jones K, Olson RE, Macor JE, Albright CF. Meredith JE Jr, et al. Among authors: grace je jr. J Pharmacol Exp Ther. 2008 Aug;326(2):502-13. doi: 10.1124/jpet.108.138974. Epub 2008 May 22. J Pharmacol Exp Ther. 2008. PMID: 18499745
Synthesis and evaluation of 5,5-diphenylimidazolones as potent human neuropeptide Y5 receptor antagonists.
Gillman KW, Higgins MA, Poindexter GS, Browning M, Clarke WJ, Flowers S, Grace JE Jr, Hogan JB, McGovern RT, Iben LG, Mattson GK, Ortiz A, Rassnick S, Russell JW, Antal-Zimanyi I. Gillman KW, et al. Among authors: grace je jr. Bioorg Med Chem. 2006 Aug 15;14(16):5517-26. doi: 10.1016/j.bmc.2006.04.042. Epub 2006 May 11. Bioorg Med Chem. 2006. PMID: 16697206
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