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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: chen l. Xenobiotica. 2017 Feb;47(2):119-126. doi: 10.3109/00498254.2016.1166531. Epub 2016 Jun 29. Xenobiotica. 2017. PMID: 27353353
Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development of a novel phosphodiesterase 2A PET ligand.
Zhang L, Villalobos A, Beck EM, Bocan T, Chappie TA, Chen L, Grimwood S, Heck SD, Helal CJ, Hou X, Humphrey JM, Lu J, Skaddan MB, McCarthy TJ, Verhoest PR, Wager TT, Zasadny K. Zhang L, et al. Among authors: chen l. J Med Chem. 2013 Jun 13;56(11):4568-79. doi: 10.1021/jm400312y. Epub 2013 May 28. J Med Chem. 2013. PMID: 23651455
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: chen l. J Med Chem. 2014 Feb 13;57(3):861-77. doi: 10.1021/jm401622k. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24392688
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: chen l. 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
Identification of a Novel Positron Emission Tomography (PET) Ligand for Imaging β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE-1) in Brain.
Zhang L, Chen L, Dutra JK, Beck EM, Nag S, Takano A, Amini N, Arakawa R, Brodney MA, Buzon LM, Doran SD, Lanyon LF, McCarthy TJ, Bales KR, Nolan CE, O'Neill BT, Schildknegt K, Halldin C, Villalobos A. Zhang L, et al. Among authors: chen l. J Med Chem. 2018 Apr 26;61(8):3296-3308. doi: 10.1021/acs.jmedchem.7b01769. Epub 2018 Feb 2. J Med Chem. 2018. PMID: 29356535
Quantitative Analysis of 18F-PF-06684511, a Novel PET Radioligand for Selective β-Secretase 1 Imaging, in Nonhuman Primate Brain.
Takano A, Chen L, Nag S, Brodney MA, Arakawa R, Chang C, Amini N, Doran SD, Dutra JK, McCarthy TJ, Nolan CE, O'Neill BT, Villalobos A, Zhang L, Halldin C. Takano A, et al. Among authors: chen l. J Nucl Med. 2019 Jul;60(7):992-997. doi: 10.2967/jnumed.118.217372. Epub 2018 Dec 7. J Nucl Med. 2019. PMID: 30530832 Free article.
PET imaging of beta-secretase 1 in the human brain: radiation dosimetry, quantification, and test-retest examination of [18F]PF-06684511.
Arakawa R, Takano A, Stenkrona P, Stepanov V, Nag S, Jahan M, Grybäck P, Bolin M, Chen L, Zhang L, He P, Villalobos A, McCarthy TJ, Halldin C, Varrone A. Arakawa R, et al. Among authors: chen l. Eur J Nucl Med Mol Imaging. 2020 Sep;47(10):2429-2439. doi: 10.1007/s00259-020-04739-5. Epub 2020 Mar 6. Eur J Nucl Med Mol Imaging. 2020. PMID: 32140803 Free PMC article.
Investigating CNS distribution of PF-05212377, a P-glycoprotein substrate, by translation of 5-HT6 receptor occupancy from non-human primates to humans.
Sawant-Basak A, Chen L, Lockwood P, Boyden T, Doran AC, Mancuso J, Zasadny K, McCarthy T, Morris ED, Carson RE, Esterlis I, Huang Y, Nabulsi N, Planeta B, Fullerton T. Sawant-Basak A, et al. Among authors: chen l. Biopharm Drug Dispos. 2023 Feb;44(1):48-59. doi: 10.1002/bdd.2351. Epub 2023 Mar 13. Biopharm Drug Dispos. 2023. PMID: 36825693
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