Search Results - "Grimm, Scott W"

The Conduct of in Vitro Studies to Address Time-Dependent Inhibition of Drug-Metabolizing Enzymes: A Perspective of the Pharmaceutical Research and Manufacturers of America by GRIMM, Scott W, EINOLF, Heidi J, TONN, George R, VAN HORN, Robert, WANG, Regina W, WONG, Y. Nancy, YANG, Tian J, OBACH, R. Scott, HALL, Steven D, KAN HE, LIM, Heng-Keang, LING, Kah-Hiing John, CHUANG LU, NOMEIR, Amin A, SEIBERT, Eleanore, SKORDOS, Konstantine W

“…Time-dependent inhibition (TDI) of cytochrome P450 (P450) enzymes caused by new molecular entities (NMEs) is of concern because such compounds can be…”
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Effects of cytochrome P450 3A modulators ketoconazole and carbamazepine on quetiapine pharmacokinetics by Grimm, Scott W., Richtand, Neil M., Winter, Helen R., Stams, Karen R., Reele, Stots B.

“…Aims To explore the potential for drug interactions on quetiapine pharmacokinetics using in vitro and in vivo assessments. Methods The CYP enzymes responsible…”
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Metabolism of a G protein-coupled receptor modulator, including two major 1,2,4-oxadiazole ring-opened metabolites and a rearranged cysteine-piperazine adduct by Gu, Chungang, Elmore, Charles S, Lin, Jianrong, Zhou, Diansong, Luzietti, Rick, Dorff, Peter, Grimm, Scott W

“…Metabolites of a G protein-coupled receptor modulator containing 1,2,4-oxadiazole and piperazine substructures were identified in vitro in human, rat, and dog…”
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COMPARISON OF METHODS FOR THE PREDICTION OF THE METABOLIC SITES FOR CYP3A4-MEDIATED METABOLIC REACTIONS by DIANSONG ZHOU, AFZELIUS, Lovisa, GRIMM, Scott W, ANDERSSON, Tommy B, ZAUHAR, Randy J, ZAMORA, Ismael

“…Predictions of the metabolic sites for new chemical entities, synthesized or only virtual, are important in the early phase of drug discovery to guide…”
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Expression and Characterization of Dog Cytochrome P450 2A13 and 2A25 in Baculovirus-Infected Insect Cells by DIANSONG ZHOU, LINNENBACH, Alban J, RUIFENG LIU, LUZIETTI, Rick A, HARRIS, Jennifer J, BOOTH-GENTHE, Catherine L, GRIMM, Scott W

“…Dog CYP2A13 and CYP2A25 were coexpressed with dog NADPH-cytochrome P450 reductase (OR) in baculovirus-infected Sf9 insect cells. CYP2A13 effectively catalyzed…”
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In Vitro Evaluation of Potential Drug-Drug Interactions with Ticagrelor: Cytochrome P450 Reaction Phenotyping, Inhibition, Induction, and Differential Kinetics by DIANSONG ZHOU, ANDERSSON, Tommy B, GRIMM, Scott W

“…Ticagrelor is an orally administered, antiplatelet agent that inhibits the prothrombotic effects of ADP on the platelet by antagonizing the P2Y(12) receptor…”
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Fusidic Acid Inhibits Hepatic Transporters and Metabolic Enzymes: Potential Cause of Clinical Drug-Drug Interaction Observed with Statin Coadministration by Gupta, Anshul, Harris, Jennifer J, Lin, Jianrong, Bulgarelli, James P, Birmingham, Bruce K, Grimm, Scott W

“…Fusidic acid (FA), which was approved in the 1960s in many European and Asian countries, has gained renewed interest due to its continued effectiveness against…”
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Pharmacokinetics, metabolism and excretion of [14C]-lanicemine (AZD6765), a novel low-trapping N-methyl-d-aspartic acid receptor channel blocker, in healthy subjects by Guo, Jian, Zhou, Diansong, Grimm, Scott W., Bui, Khanh H.

“…Abstract 1. (1S)-1-phenyl-2-(pyridin-2-yl)ethanamine (lanicemine; AZD6765) is a low-trapping N-methyl-d-aspartate (NMDA) channel blocker that has been studied…”
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Absorption, distribution, metabolism and elimination of 14C-ETX0914, a novel inhibitor of bacterial type-II topoisomerases in rodents by Guo, Jian, Joubran, Camil, Luzietti, Ricardo A., Basarab, Gregory S., Grimm, Scott W., Vishwanathan, Karthick

“…1. ETX0914 is a novel bacterial topoisomerase inhibitor that has a novel mode-of-inhibition and is in clinical development for the treatment of infections…”
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Role of Human UGT2B10 in N-Glucuronidation of Tricyclic Antidepressants, Amitriptyline, Imipramine, Clomipramine, and Trimipramine by DIANSONG ZHOU, JIAN GUO, LINNENBACH, Alban J, BOOTH-GENTHE, Catherine L, GRIMM, Scott W

“…The role of human UDP glucuronosyltransferase (UGT) 2B10 in the N-glucuronidation of a number of tricyclic antidepressants was investigated and compared with…”
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A clinical study to assess CYP1A2 and CYP3A4 induction by AZD7325, a selective GABAA receptor modulator – an in vitro and in vivo comparison by Zhou, Diansong, Sunzel, Maria, Ribadeneira, Maria D., Smith, Mark A., Desai, Dhaval, Lin, Jianrong, Grimm, Scott W.

“…WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT • AZD7325 is an orally administered, potent, selective gamma‐amino‐butyric acid (GABAA) α2,3 receptor modulator…”
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Liquid chromatography–tandem mass spectrometry method for measurement of nicotine N-glucuronide: A marker for human UGT2B10 inhibition by Guo, Jian, Zhou, Diansong, Grimm, Scott W.

“…Nicotine is considered to be a specific substrate for UGT2B10, an isoform of human uridine diphosphate glucuronosyltransferase (UGT). In the present study, a…”
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Absorption, excretion, and metabolism of a potential GABA-Aα2/3 receptor modulator in rats by Guo, Jian, Davis, Patty C., Gu, Chungang, Grimm, Scott W.

“…4-Amino-8-(2,5-dimethoxyphenyl)-N-propylcinnoline-3-carboxamide (AZD6280) is a selective GABA-Aα2/3 receptor modulator under development for the treatment of…”
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In Vitro and In Vivo Metabolism of a Selective δ-Opioid Receptor by JIAN GUO, CHUNGANG GU, DIANSONG ZHOU, ELMORE, Charles S, BUI, Khanh H, GRIMM, Scott W

“…4-({4-[(2-hydroxy-ethyl)-methyl-carbamoyl]-phenyl}-quinolin-8-yl-methylene)-1-thiazol-4-ylmethyl-piperidinium (compound I) is a selective agonist of δ-opioid…”
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A clinical study to assess CYP1A2 and CYP3A4 induction by AZD7325, a selective GABA(A) receptor modulator - an in vitro and in vivo comparison by Zhou, Diansong, Sunzel, Maria, Ribadeneira, Maria D, Smith, Mark A, Desai, Dhaval, Lin, Jianrong, Grimm, Scott W

“…• AZD7325 is an orally administered, potent, selective gamma-amino-butyric acid (GABA(A) ) α2,3 receptor modulator intended for the treatment of anxiety. • The…”
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In vitro metabolism of α7 neuronal nicotinic receptor agonist AZD0328 and enzyme identification for its N-oxide metabolite by Zhou, Diansong, Zhang, Minli, Ye, Xiaomei, Gu, Chungang, Piser, Timothy M., Lanoue, Bernard A., Schock, Sara A., Cheng, Yi-Fang, Grimm, Scott W.

“…AZD0328 was pharmacologically characterized as a α7 neuronal nicotinic receptor agonist intended for treatment of Alzheimer′s disease. In vitro AZD0328 cross…”
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Inhibition of Human Drug Metabolizing Cytochromes P450 by Anastrozole, a Potent and Selective Inhibitor of Aromatase by GRIMM, S. W, DYROFF, M. C

“…Anastrozole (2,2′[5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-phenylene]bis(2-methylproprionitrile)) is a potent third-generation inhibitor of aromatase, currently…”
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Disposition and Metabolism of Ticagrelor, a Novel P2Y 12 Receptor Antagonist, in Mice, Rats, and Marmosets by Li, Yan, Landqvist, Claire, Grimm, Scott W.

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In vitro prediction of potential metabolic drug interactions for seroquel by Grimm, Scott W., Stams, Karen R., Bui, Khanh

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Disposition and Metabolism of Ticagrelor, a Novel P2Y12 Receptor Antagonist, in Mice, Rats, and Marmosets by YAN LI, LANDQVIST, Claire, GRIMM, Scott W

“…Ticagrelor is a reversibly binding and selective oral P2Y(12) antagonist, developed for the prevention of atherothrombotic events in patients with acute…”
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