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Page 1
Pharmacological characterization of 2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine (PF-04455242), a high-affinity antagonist selective for κ-opioid receptors.
Grimwood S, Lu Y, Schmidt AW, Vanase-Frawley MA, Sawant-Basak A, Miller E, McLean S, Freeman J, Wong S, McLaughlin JP, Verhoest PR. Grimwood S, et al. J Pharmacol Exp Ther. 2011 Nov;339(2):555-66. doi: 10.1124/jpet.111.185108. Epub 2011 Aug 5. J Pharmacol Exp Ther. 2011. PMID: 21821697
The 5-hydroxytryptamine4 receptor agonists prucalopride and PRX-03140 increase acetylcholine and histamine levels in the rat prefrontal cortex and the power of stimulated hippocampal θ oscillations.
Johnson DE, Drummond E, Grimwood S, Sawant-Basak A, Miller E, Tseng E, McDowell LL, Vanase-Frawley MA, Fisher KE, Rubitski DM, Stutzman-Engwall KJ, Nelson RT, Horner WE, Gorczyca RR, Hajos M, Siok CJ. Johnson DE, et al. J Pharmacol Exp Ther. 2012 Jun;341(3):681-91. doi: 10.1124/jpet.112.192351. Epub 2012 Mar 9. J Pharmacol Exp Ther. 2012. PMID: 22408061
Metabolism of a serotonin-4 receptor partial agonist 4-{4-[4-tetrahydrofuran-3-yloxy)-benzo[d]isoxazol-3-yloxymethyl]-piperidin-1-ylmethyl}-tetrahydropyran-4-ol (TBPT): identification of an unusual pharmacologically active cyclized oxazolidine metabolite in human.
Sawant-Basak A, Coffman KJ, Walker GS, Ryder TF, Tseng E, Miller E, Lee C, Vanase-Frawley MA, Wong JW, Brodney MA, Rapp T, Obach RS. Sawant-Basak A, et al. J Pharm Sci. 2013 Sep;102(9):3277-93. doi: 10.1002/jps.23542. Epub 2013 Apr 15. J Pharm Sci. 2013. PMID: 23589342
Metabolism and clinical pharmacokinetics of 2-methyl-n-(2'-(pyrrolidinyl-1-ylsulfonyl)-n-[1,1'-biphenyl]-4-yl)propran-1-amine: insights into monoamine oxidase- and CYP-mediated disposition by integration of in vitro ADME tools.
Sawant Basak A, Byon W, Tseng-Lovering E, Funk C, Wood L, Lin C, Delnomdedieu M, Verhoest P, Parikh V, Cox LM, Miller E, Gao H, Obach RS. Sawant Basak A, et al. Xenobiotica. 2014 May;44(5):438-54. doi: 10.3109/00498254.2013.850552. Epub 2013 Dec 4. Xenobiotica. 2014. PMID: 24304147
Determination of receptor occupancy in the presence of mass dose: [11C]GSK189254 PET imaging of histamine H3 receptor occupancy by PF-03654746.
Gallezot JD, Planeta B, Nabulsi N, Palumbo D, Li X, Liu J, Rowinski C, Chidsey K, Labaree D, Ropchan J, Lin SF, Sawant-Basak A, McCarthy TJ, Schmidt AW, Huang Y, Carson RE. Gallezot JD, et al. J Cereb Blood Flow Metab. 2017 Mar;37(3):1095-1107. doi: 10.1177/0271678X16650697. Epub 2016 Jul 20. J Cereb Blood Flow Metab. 2017. PMID: 27207170 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. Biopharm Drug Dispos. 2023 Feb;44(1):48-59. doi: 10.1002/bdd.2351. Epub 2023 Mar 13. Biopharm Drug Dispos. 2023. PMID: 36825693
Identification of multiple 5-HT₄ partial agonist clinical candidates for the treatment of Alzheimer's disease.
Brodney MA, Johnson DE, Sawant-Basak A, Coffman KJ, Drummond EM, Hudson EL, Fisher KE, Noguchi H, Waizumi N, McDowell LL, Papanikolaou A, Pettersen BA, Schmidt AW, Tseng E, Stutzman-Engwall K, Rubitski DM, Vanase-Frawley MA, Grimwood S. Brodney MA, et al. J Med Chem. 2012 Nov 8;55(21):9240-54. doi: 10.1021/jm300953p. Epub 2012 Oct 5. J Med Chem. 2012. PMID: 22974325
23 results