Search Results - "ZHAO, Sabrina X"

Role of Transporters in the Disposition of the Selective Phosphodiesterase-4 Inhibitor (+)-2-[4-({[2-(Benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic Acid in Rat and Human by KALGUTKAR, Amit S, BO FENG, DUIGNAN, David B, CHOO, Edna F, ZHAO, Sabrina X, NGUYEN, Hang T, FREDERICK, Kosea S, CAMPBELL, Scott D, HATCH, Heather L, BI, Yi-An, KAZOLIAS, Diana C, DAVIDSON, Ralph E, MIRELES, Rouchelle J

“…The role of transporters in the disposition of (+)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid…”
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Metabolism of a Dopamine Receptor Partial Agonist in Rats, Including an Unusual N-Dearylation Reaction by Zhao, Sabrina X., Wang, Wendy WeiWei, Walker, Gregory S., Zhang, Liming, Scott Obach, R.

“…The metabolism of 3,4-dihydro-7-[4-(1-naphthalenyl)-1-piperazinyl]butoxy]-1,8-naphthyridin-2(1H)-one (NPBN) was investigated in rats. Animals were administered…”
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BIOACTIVATION OF THE NONTRICYCLIC ANTIDEPRESSANT NEFAZODONE TO A REACTIVE QUINONE-IMINE SPECIES IN HUMAN LIVER MICROSOMES AND RECOMBINANT CYTOCHROME P450 3A4 by KALGUTKAR, Amit S, VAZ, Alfin D. N, HOP, Cornelis E. C. A, LAME, Mary E, HENNE, Kirk R, SOGLIA, John, ZHAO, Sabrina X, ABRAMOV, Yuri A, LOMBARDO, Franco, COLLIN, Claire, HENDSCH, Zachary S

“…The therapeutic benefits of the antidepressant nefazodone have been hampered by several cases of acute hepatotoxicity/liver failure. Although the mechanism of…”
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Metabolic activation of the nontricyclic antidepressant trazodone to electrophilic quinone-imine and epoxide intermediates in human liver microsomes and recombinant P4503A4 by Kalgutkar, Amit S., Henne, Kirk R., Lame, Mary E., Vaz, Alfin D.N., Collin, Claire, Soglia, John R., Zhao, Sabrina X., Hop, Cornelis E.C.A.

“…Therapy with the antidepressant trazodone has been associated with several cases of idiosyncratic hepatotoxicity. While the mechanism of hepatotoxicity remains…”
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Can In Vitro Metabolism-Dependent Covalent Binding Data in Liver Microsomes Distinguish Hepatotoxic from Nonhepatotoxic Drugs? An Analysis of 18 Drugs with Consideration of Intrinsic Clearance and Daily Dose by Obach, R. Scott, Kalgutkar, Amit S, Soglia, John R, Zhao, Sabrina X

“…In vitro covalent binding assessments of drugs have been useful in providing retrospective insights into the association between drug metabolism and a…”
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Can In Vitro Metabolism-Dependent Covalent Binding Data Distinguish Hepatotoxic from Nonhepatotoxic Drugs? An Analysis Using Human Hepatocytes and Liver S-9 Fraction by Bauman, Jonathon N, Kelly, Joan M, Tripathy, Sakambari, Zhao, Sabrina X, Lam, Wing W, Kalgutkar, Amit S, Obach, R. Scott

“…In vitro covalent binding studies in which xenobiotics are shown to undergo metabolism-dependent covalent binding to macromolecules have been commonly used to…”
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Discovery of N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an Agonist of the α7 Nicotinic Acetylcholine Receptor, for the Potential Treatment of Cognitive Deficits in Schizophrenia:  Synthesis and Structure−Activity Relationship by Wishka, Donn G, Walker, Daniel P, Yates, Karen M, Reitz, Steven C, Jia, Shaojuan, Myers, Jason K, Olson, Kirk L, Jacobsen, E. Jon, Wolfe, Mark L, Groppi, Vincent E, Hanchar, Alexander J, Thornburgh, Bruce A, Cortes-Burgos, Luz A, Wong, Erik H. F, Staton, Brian A, Raub, Thomas J, Higdon, Nicole R, Wall, Theron M, Hurst, Raymond S, Walters, Rodney R, Hoffmann, William E, Hajos, Mihaly, Franklin, Stanley, Carey, Galen, Gold, Lisa H, Cook, Karen K, Sands, Steven B, Zhao, Sabrina X, Soglia, John R, Kalgutkar, Amit S, Arneric, Stephen P, Rogers, Bruce N

“…N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (14, PHA-543,613), a novel agonist of the α7 neuronal nicotinic acetylcholine receptor…”
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High throughput ADME screening: practical considerations, impact on the portfolio and enabler of in silico ADME models by Hop, Cornelis E C A, Cole, Mark J, Davidson, Ralph E, Duignan, David B, Federico, James, Janiszewski, John S, Jenkins, Kelly, Krueger, Suzanne, Lebowitz, Rebecca, Liston, Theodore E, Mitchell, Walter, Snyder, Mark, Steyn, Stefan J, Soglia, John R, Taylor, Christine, Troutman, Matt D, Umland, John, West, Michael, Whalen, Kevin M, Zelesky, Veronica, Zhao, Sabrina X

“…Evaluation and optimization of drug metabolism and pharmacokinetic data plays an important role in drug discovery and development and several reliable in vitro…”
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NADPH-Dependent Covalent Binding of [3H]Paroxetine to Human Liver Microsomes and S-9 Fractions: Identification of an Electrophilic Quinone Metabolite of Paroxetine by Zhao, Sabrina X, Dalvie, Deepak K, Kelly, Joan M, Soglia, John R, Frederick, Kosea S, Smith, Evan B, Obach, R. Scott, Kalgutkar, Amit S

“…The primary pathway of clearance of the methylenedioxyphenyl-containing compound and selective serotonin reuptake inhibitor paroxetine in humans involves P450…”
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Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2) : Structure-activity relationships and strategies for the elimination of reactive metabolite formation by WALKER, Daniel P, BI, F. Christopher, MCGLYNN, Molly A, OLIVER, Robert, DUNN, Matthew, LI, Jian-Cheng, RICHTER, Daniel T, COOPER, Beth A, KATH, John C, HULFORD, Catherine A, AUTRY, Christopher L, LUZZIO, Michael J, KALGUTKAR, Amit S, UNG, Ethan J, ROBERTS, W. Gregory, BONNETTE, Peter C, BUCKBINDER, Leonard, MISTRY, Anil, GRIFFOR, Matthew C, HAN, Seungil, GUZMAN-PEREZ, Angel, BAUMAN, Jonathan N, ZHAO, Sabrina X, SOGLIA, John R, ASPNES, Gary E, KUNG, Daniel W, KLUG-MCLEOD, Jacquelyn, ZAWISTOSKI, Michael P

“…The synthesis and SAR for a series of diaminopyrimidines as PYK2 inhibitors are described. Using a combination of library and traditional medicinal chemistry…”
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A Rational Chemical Intervention Strategy To Circumvent Bioactivation Liabilities Associated with a Nonpeptidyl Thrombopoietin Receptor Agonist Containing a 2-Amino-4-arylthiazole Motif by Kalgutkar, Amit S, Driscoll, James, Zhao, Sabrina X, Walker, Gregory S, Shepard, Richard M, Soglia, John R, Atherton, James, Yu, Linning, Mutlib, Abdul E, Munchhof, Michael J, Reiter, Lawrence A, Jones, Christopher S, Doty, Johnathan L, Trevena, Kristen A, Shaffer, Christopher L, Ripp, Sharon L

“…The current study examined the bioactivation potential of a nonpeptidyl thrombopoietin receptor agonist,…”
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Discovery Tactics To Mitigate Toxicity Risks Due to Reactive Metabolite Formation with 2-(2-Hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one Derivatives, Potent Calcium-Sensing Receptor Antagonists and Clinical Candidate(s) for the Treatment of Osteoporosis by Kalgutkar, Amit S, Griffith, David A, Ryder, Tim, Sun, Hao, Miao, Zhuang, Bauman, Jonathan N, Didiuk, Mary T, Frederick, Kosea S, Zhao, Sabrina X, Prakash, Chandra, Soglia, John R, Bagley, Scott W, Bechle, Bruce M, Kelley, Ryan M, Dirico, Kenneth, Zawistoski, Michael, Li, Jianke, Oliver, Robert, Guzman-Perez, Angel, Liu, Kevin K. C, Walker, Daniel P, Benbow, John W, Morris, Joel

“…The synthesis and structure−activity relationship studies on 5-trifluoromethylpyrido[4,3-d]pyrimidin-4(3H)-ones as antagonists of the human calcium receptor…”
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Simple strategies for reducing sample loads in in vitro metabolic stability high-throughput screening experiments: a comparison between traditional, two-time-point and pooled sample analyses by Zhao, Sabrina X, Forman, Darcy, Wallace, Nora, Smith, Bill J, Meyer, Daniel, Kazolias, Diana, Gao, Feng, Soglia, John, Cole, Mark, Nettleton, David

“…Higher-throughput ADME programs in early drug discovery are becoming common throughout the pharmaceutical industry as companies strive to reduce their compound…”
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Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship by Wishka, Donn G, Walker, Daniel P, Yates, Karen M, Reitz, Steven C, Jia, Shaojuan, Myers, Jason K, Olson, Kirk L, Jacobsen, E Jon, Wolfe, Mark L, Groppi, Vincent E, Hanchar, Alexander J, Thornburgh, Bruce A, Cortes-Burgos, Luz A, Wong, Erik H F, Staton, Brian A, Raub, Thomas J, Higdon, Nicole R, Wall, Theron M, Hurst, Raymond S, Walters, Rodney R, Hoffmann, William E, Hajos, Mihaly, Franklin, Stanley, Carey, Galen, Gold, Lisa H, Cook, Karen K, Sands, Steven B, Zhao, Sabrina X, Soglia, John R, Kalgutkar, Amit S, Arneric, Stephen P, Rogers, Bruce N

“…N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (14, PHA-543,613), a novel agonist of the alpha7 neuronal nicotinic acetylcholine…”
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