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Quantitative projection of human brain penetration of the H3 antagonist PF-03654746 by integrating rat-derived brain partitioning and PET receptor occupancy.
Sawant-Basak A, Chen L, Shaffer CL, Palumbo D, Schmidt A, Tseng E, Spracklin DK, Gallezot JD, Labaree D, Nabulsi N, Huang Y, Carson RE, McCarthy T. Sawant-Basak A, et al. Among authors: shaffer cl. Xenobiotica. 2017 Feb;47(2):119-126. doi: 10.3109/00498254.2016.1166531. Epub 2016 Jun 29. Xenobiotica. 2017. PMID: 27353353
Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates.
Stepan AF, Claffey MM, Reese MR, Balan G, Barreiro G, Barricklow J, Bohanon MJ, Boscoe BP, Cappon GD, Chenard LK, Cianfrogna J, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Ghosh S, Hou X, Houle C, Karki K, Lazzaro JT, Mancuso JY, Marcek JM, Miller EL, Moen MA, O'Neil S, Sakurada I, Skaddan M, Parikh V, Smith DL, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Won A, Wright AS, Whritenour J, Zasadny K, Zaleska MM, Zhang L, Shaffer CL. Stepan AF, et al. Among authors: shaffer cl. J Med Chem. 2017 Sep 28;60(18):7764-7780. doi: 10.1021/acs.jmedchem.7b00604. Epub 2017 Sep 13. J Med Chem. 2017. PMID: 28817277
Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
Zhang L, Balan G, Barreiro G, Boscoe BP, Chenard LK, Cianfrogna J, Claffey MM, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Fonseca KR, Galatsis P, Grimwood S, Lazzaro JT, Mancuso JY, Miller EL, Reese MR, Rogers BN, Sakurada I, Skaddan M, Smith DL, Stepan AF, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Wright AS, Zaleska MM, Zasadny K, Shaffer CL. Zhang L, et al. Among authors: shaffer cl. J Med Chem. 2014 Feb 13;57(3):861-77. doi: 10.1021/jm401622k. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24392688
Positive allosteric modulation of AMPA receptors from efficacy to toxicity: the interspecies exposure-response continuum of the novel potentiator PF-4778574.
Shaffer CL, Hurst RS, Scialis RJ, Osgood SM, Bryce DK, Hoffmann WE, Lazzaro JT, Hanks AN, Lotarski S, Weber ML, Liu J, Menniti FS, Schmidt CJ, Hajós M. Shaffer CL, et al. J Pharmacol Exp Ther. 2013 Oct;347(1):212-24. doi: 10.1124/jpet.113.204735. Epub 2013 Jul 30. J Pharmacol Exp Ther. 2013. PMID: 23899905
Unbound Brain-to-Plasma Partition Coefficient, Kp,uu,brain-a Game Changing Parameter for CNS Drug Discovery and Development.
Loryan I, Reichel A, Feng B, Bundgaard C, Shaffer C, Kalvass C, Bednarczyk D, Morrison D, Lesuisse D, Hoppe E, Terstappen GC, Fischer H, Di L, Colclough N, Summerfield S, Buckley ST, Maurer TS, Fridén M. Loryan I, et al. Pharm Res. 2022 Jul;39(7):1321-1341. doi: 10.1007/s11095-022-03246-6. Epub 2022 Apr 11. Pharm Res. 2022. PMID: 35411506 Free PMC article.
104 results