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Items: 17

1.

Emerging Models of Drug Metabolism, Transporters, and Toxicity.

Sawant-Basak A, Obach RS.

Drug Metab Dispos. 2018 Nov;46(11):1556-1561. doi: 10.1124/dmd.118.084293.

PMID:
30333205
2.

Physiologically Relevant, Humanized Intestinal Systems to Study Metabolism and Transport of Small Molecule Therapeutics.

Sawant-Basak A, Rodrigues AD, Lech M, Doyonnas R, Kasaian M, Prasad B, Tsamandouras N.

Drug Metab Dispos. 2018 Nov;46(11):1581-1587. doi: 10.1124/dmd.118.082784. Epub 2018 Aug 20.

PMID:
30126862
3.

Quantitative Translational Analysis of Brain Kynurenic Acid Modulation via Irreversible Kynurenine Aminotransferase II Inhibition.

Chang C, Fonseca KR, Li C, Horner W, Zawadzke LE, Salafia MA, Welch KA, Strick CA, Campbell BM, Gernhardt SS, Rong H, Sawant-Basak A, Liras J, Dounay A, Tuttle JB, Verhoest P, Maurer TS.

Mol Pharmacol. 2018 Aug;94(2):823-833. doi: 10.1124/mol.118.111625. Epub 2018 May 31.

PMID:
29853495
4.

Metabolism of a 5HT6 Antagonist, 2-Methyl-1-(Phenylsulfonyl)-4-(Piperazin-1-yl)-1H-Benzo[d]imidazole (SAM-760): Impact of Sulfonamide Metabolism on Diminution of a Ketoconazole-Mediated Clinical Drug-Drug Interaction.

Sawant-Basak A, Obach RS, Doran A, Lockwood P, Schildknegt K, Gao H, Mancuso J, Tse S, Comery TA.

Drug Metab Dispos. 2018 Jul;46(7):934-942. doi: 10.1124/dmd.118.080457. Epub 2018 Apr 25.

PMID:
29695615
5.

Estimation of Circulating Drug Metabolite Exposure in Human Using In Vitro Data and Physiologically Based Pharmacokinetic Modeling: Example of a High Metabolite/Parent Drug Ratio.

Obach RS, Lin J, Kimoto E, Duvvuri S, Nicholas T, Kadar EP, Tremaine LM, Sawant-Basak A.

Drug Metab Dispos. 2018 Feb;46(2):89-99. doi: 10.1124/dmd.117.078279. Epub 2017 Nov 17.

PMID:
29150544
6.

Kynurenine pathway in schizophrenia: Galantamine-memantine combination for cognitive impairments.

Koola MM, Sklar J, Davis W, Nikiforuk A, Meissen JK, Sawant-Basak A, Aaronson ST, Kozak R.

Schizophr Res. 2018 Mar;193:459-460. doi: 10.1016/j.schres.2017.07.005. Epub 2017 Jul 11. No abstract available.

PMID:
28705532
7.

Dopamine D3/D2 Receptor Antagonist PF-4363467 Attenuates Opioid Drug-Seeking Behavior without Concomitant D2 Side Effects.

Wager TT, Chappie T, Horton D, Chandrasekaran RY, Samas B, Dunn-Sims ER, Hsu C, Nawreen N, Vanase-Frawley MA, O'Connor RE, Schmidt CJ, Dlugolenski K, Stratman NC, Majchrzak MJ, Kormos BL, Nguyen DP, Sawant-Basak A, Mead AN.

ACS Chem Neurosci. 2017 Jan 18;8(1):165-177. doi: 10.1021/acschemneuro.6b00297. Epub 2016 Oct 21.

PMID:
27715007
8.

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.

Xenobiotica. 2017 Feb;47(2):119-126. doi: 10.3109/00498254.2016.1166531. Epub 2016 Jun 29.

PMID:
27353353
9.

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.

J Cereb Blood Flow Metab. 2017 Mar;37(3):1095-1107. doi: 10.1177/0271678X16650697. Epub 2016 Jul 20.

10.

Strategies toward optimization of the metabolism of a series of serotonin-4 partial agonists: investigation of azetidines as piperidine isosteres.

Obach RS, LaChapelle EA, Brodney MA, Vanase-Frawley M, Kauffman GW, Sawant-Basak A.

Xenobiotica. 2016 Dec;46(12):1112-1121. Epub 2016 Mar 7.

PMID:
26947511
11.

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.

Xenobiotica. 2014 May;44(5):438-54. doi: 10.3109/00498254.2013.850552. Epub 2013 Dec 4.

PMID:
24304147
12.

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.

J Pharm Sci. 2013 Sep;102(9):3277-93. doi: 10.1002/jps.23542. Epub 2013 Apr 15.

PMID:
23589342
13.

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.

J Med Chem. 2012 Nov 8;55(21):9240-54. doi: 10.1021/jm300953p. Epub 2012 Oct 5.

PMID:
22974325
14.

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.

J Pharmacol Exp Ther. 2012 Jun;341(3):681-91. doi: 10.1124/jpet.112.192351. Epub 2012 Mar 9.

15.

Pharmacodynamic model of sodium-glucose transporter 2 (SGLT2) inhibition: implications for quantitative translational pharmacology.

Maurer TS, Ghosh A, Haddish-Berhane N, Sawant-Basak A, Boustany-Kari CM, She L, Leininger MT, Zhu T, Tugnait M, Yang X, Kimoto E, Mascitti V, Robinson RP.

AAPS J. 2011 Dec;13(4):576-84. doi: 10.1208/s12248-011-9297-2. Epub 2011 Aug 26.

16.

Quantitative PK-PD model-based translational pharmacology of a novel kappa opioid receptor antagonist between rats and humans.

Chang C, Byon W, Lu Y, Jacobsen LK, Badura LL, Sawant-Basak A, Miller E, Liu J, Grimwood S, Wang EQ, Maurer TS.

AAPS J. 2011 Dec;13(4):565-75. doi: 10.1208/s12248-011-9296-3. Epub 2011 Aug 17.

17.

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.

J Pharmacol Exp Ther. 2011 Nov;339(2):555-66. doi: 10.1124/jpet.111.185108. Epub 2011 Aug 5.

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