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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.


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.


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.


In vitro metabolism of BIIB021, an inhibitor of heat shock protein 90, in liver microsomes and hepatocytes of rats, dogs, and humans and recombinant human cytochrome P450 isoforms.

Xu L, Woodward C, Khan S, Prakash C.

Drug Metab Dispos. 2012 Apr;40(4):680-93. doi: 10.1124/dmd.111.043000. Epub 2012 Jan 4.


In vitro and in vivo metabolism of a selective δ-opioid receptor.

Guo J, Gu C, Zhou D, Elmore CS, Bui KH, Grimm SW.

Drug Metab Dispos. 2011 Oct;39(10):1883-94. doi: 10.1124/dmd.111.040980. Epub 2011 Jul 13.


Biotransformation of 6-methoxy-3-(3',4',5'-trimethoxy-benzoyl)-1H-indole (BPR0L075), a novel antimicrotubule agent, by mouse, rat, dog, and human liver microsomes.

Yao HT, Wu YS, Chang YW, Hsieh HP, Chen WC, Lan SJ, Chen CT, Chao YS, Chang L, Sun HY, Yeh TK.

Drug Metab Dispos. 2007 Jul;35(7):1042-9. Epub 2007 Apr 2.


Metabolism of a dopamine receptor partial agonist in rats, including an unusual N-dearylation reaction.

Zhao SX, Wang WW, Walker GS, Zhang L, Obach RS.

Drug Metab Pharmacokinet. 2011 Jun;26(3):266-79. doi: 10.2133/dmpk.DMPK-10-RG-109. Epub 2011 Mar 4.


Metabolism of MK-0524, a prostaglandin D2 receptor 1 antagonist, in microsomes and hepatocytes from preclinical species and humans.

Dean BJ, Chang S, Silva Elipe MV, Xia YQ, Braun M, Soli E, Zhao Y, Franklin RB, Karanam B.

Drug Metab Dispos. 2007 Feb;35(2):283-92. Epub 2006 Nov 28.


In vitro metabolism of rivaroxaban, an oral, direct factor Xa inhibitor, in liver microsomes and hepatocytes of rats, dogs, and humans.

Lang D, Freudenberger C, Weinz C.

Drug Metab Dispos. 2009 May;37(5):1046-55. doi: 10.1124/dmd.108.025551. Epub 2009 Feb 5.


Biotransformation of tolterodine, a new muscarinic receptor antagonist, in mice, rats, and dogs.

Andersson SH, Lindgren A, Postlind H.

Drug Metab Dispos. 1998 Jun;26(6):528-35.


In vitro and in vivo metabolism of a gamma-secretase inhibitor BMS-299897 and generation of active metabolites in milligram quantities with a microbial bioreactor.

Zhang D, Hanson R, Roongta V, Dischino DD, Gao Q, Sloan CP, Polson C, Keavy D, Zheng M, Mitroka J, Yeola S.

Curr Drug Metab. 2006 Dec;7(8):883-96.


Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties.

McKinnell RM, Armstrong SR, Beattie DT, Fatheree PR, Long DD, Marquess DG, Shaw JP, Vickery RG.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4210-5. doi: 10.1016/j.bmcl.2013.05.018. Epub 2013 May 16.


Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent.

Park JS, Im W, Choi S, Park SJ, Jung JM, Baek KS, Son HP, Sharma S, Kim IS, Jung YH.

Eur J Med Chem. 2016 Feb 15;109:75-88. doi: 10.1016/j.ejmech.2015.12.006. Epub 2015 Dec 10.


In vitro metabolism of α7 neuronal nicotinic receptor agonist AZD0328 and enzyme identification for its N-oxide metabolite.

Zhou D, Zhang M, Ye X, Gu C, Piser TM, Lanoue BA, Schock SA, Cheng YF, Grimm SW.

Xenobiotica. 2011 Mar;41(3):232-42. doi: 10.3109/00498254.2010.536855. Epub 2011 Jan 13.


In vitro bioactivation of dihydrobenzoxathiin selective estrogen receptor modulators by cytochrome P450 3A4 in human liver microsomes: formation of reactive iminium and quinone type metabolites.

Zhang Z, Chen Q, Li Y, Doss GA, Dean BJ, Ngui JS, Silva Elipe M, Kim S, Wu JY, Dininno F, Hammond ML, Stearns RA, Evans DC, Baillie TA, Tang W.

Chem Res Toxicol. 2005 Apr;18(4):675-85.


Plasma stability-dependent circulation of acyl glucuronide metabolites in humans: how circulating metabolite profiles of muraglitazar and peliglitazar can lead to misleading risk assessment.

Zhang D, Raghavan N, Wang L, Xue Y, Obermeier M, Chen S, Tao S, Zhang H, Cheng PT, Li W, Ramanathan R, Yang Z, Humphreys WG.

Drug Metab Dispos. 2011 Jan;39(1):123-31. doi: 10.1124/dmd.110.035048. Epub 2010 Sep 28.


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.


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