30 June 2009

Rob ter Heine, Michel Hillebrand, Hilde Rosing, Eric van Gorp, Jan Willem Mulder, Jos H Beijnen, and Alwin Huitema

Identification and profiling of circulating metabolites of atazanavir, a human immunodeficiency virus protease inhibitor
Published June 30, 2009; doi: 10.1124/dmd.109.028258 [Abstract] [PDF]  

22 June 2009

Tanya Louise Hay, Rhys Marsden Jones, Kevin Beaumont, and Mark Ian Kemp

Modulation of LogD_(7.4) and pK_a to achieve the optimum balance of blood clearance and volume of distribution for a series of tetrahydropyran H₃ antagonists
Published June 22, 2009; doi: 10.1124/dmd.109.027888 [Abstract] [PDF]  

Huiqing Chen, Kyunghee Yang, Suyoung Choi, James H Fischer, and Hyunyoung Jeong

Upregulation of UDP-glucuronosyltransferase (UGT) 1A4 by 17-Estradiol: a Potential Mechanism of Increased Lamotrigine Elimination in Pregnancy
Published June 22, 2009; doi: 10.1124/dmd.109.026609 [Abstract] [PDF]  

18 June 2009

Robert S. Foti, Josh T. Pearson, Dan A. Rock, Jan L. Wahlstrom, and Larry C. Wienkers

In Vitro Inhibition of Multiple Cytochrome P450 Isoforms by Xanthone Derivatives from Mangosteen Extract
Published June 18, 2009; doi: 10.1124/dmd.109.028043 [Abstract] [PDF]  

Kazuko Inoue, Tomoyuki Ohe, Kenichi Mori, Takeshi Sagara, Yasuyuki Ishii, and Masato Chiba

Aromatic Substitution Reaction of 2-Chloropyridines Catalyzed by Microsomal Glutathione S-Transferase 1
Published June 18, 2009; doi: 10.1124/dmd.109.027698 [Abstract] [PDF]  

Christopher S. Mazur, John F. Kenneke, Michael-Rock Goldsmith, and Catherine Brown

Contrasting Influence of NADPH and a NADPH-regenerating System on the Metabolism of Carbonyl-Containing Compounds in Hepatic Microsomes
Published June 18, 2009; doi: 10.1124/dmd.109.027615 [Abstract] [PDF] [Data Supplement]  

Shinji Shimizu, Ryo Atsumi, Tsunenori Nakazawa, Yuko Fujimaki, Kenichi Sudo, and Osamu Okazaki

Metabolism of ticlopidine in rats: Identification of the main biliary metabolite as a GSH conjugate of S-oxide
Published June 18, 2009; doi: 10.1124/dmd.109.027524 [Abstract] [PDF]  

Ye Li, David Buckley, Shuang Wang, Curtis D. Klaassen, and Xiao-bo Zhong

Genetic Polymorphisms in the TATA box and Upstream Phenobarbital-Responsive Enhancer Module of the UGT1A1 Promoter Have Combined Effects on UGT1A1 Transcription Mediated by CAR, PXR, or GR in Human Liver
Published June 18, 2009; doi: 10.1124/dmd.109.027409 [Abstract] [PDF] [Data Supplement]  

Keiko Maekawa, Noriko Harakawa, Emiko Sugiyama, Masahiro Tohkin, Su-Ryang Kim, Nahoko Kaniwa, Noriko Katori, Ryuichi Hasegawa, Kazuki Yasuda, Kei Kamide, Toshiyuki Miyata, Yoshiro Saito, and Jun-ichi Sawada

Substrate-dependent functional alterations of seven CYP2C9 variants found in Japanese subjects
Published June 18, 2009; doi: 10.1124/dmd.109.027003 [Abstract] [PDF]  

11 June 2009

Antonia H Tolson, Haishan Li, Natalie D Eddington, and Hongbing Wang

Methadone Induces the Expression of Hepatic Drug-Metabolizing Enzymes Through the Activation of Pregnane X Receptor and Constitutive Androstane Receptor
Published June 11, 2009; doi: 10.1124/dmd.109.027854 [Abstract] [PDF]  

Ala F Nassar, Ivan King, Brandy L Paris, Lois Haupt, Florence Ndikum-Moffor, Rebecca Campbell, Etsuko Usuki, Jennifer Skibbe, Dan Brobst, Brian W Ogilvie, and Andrew Parkinson

An in vitro evaluation of the victim and perpetrator potential of the anti-cancer agent laromustine (VNP40101M), based on reaction phenotyping and inhibition and induction of cytochrome P450 (CYP) enzymes
Published June 11, 2009; doi: 10.1124/dmd.109.027516 [Abstract] [PDF]  

Megumi Iwai, Tsuyoshi Minematsu, Shinichi Narikawa, Takashi Usui, and Hidetaka Kamimura

Involvement of Human Organic Cation Transporter 1 (OCT1) in the Hepatic Uptake of YM155 Monobromide, 1-(2-Methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazolium Bromide, a Novel, Small Molecule Survivin Suppressant
Published June 11, 2009; doi: 10.1124/dmd.109.027359 [Abstract] [PDF]  

Emese Kis, Eniko Ioja, Tunde Nagy, Lajos Szente, Krisztina Heredi-Szabo, and Peter Krajcsi

Effect of membrane cholesterol on BSEP/Bsep activity - species specificity studies for substrates and inhibitors
Published June 11, 2009; doi: 10.1124/dmd.108.024778 [Abstract] [PDF]  

Hidekazu Ooe, Junko Kon, Hideki Oshima, and Toshihiro Mitaka

Thyroid Hormone Is Necessary for Expression of Constitutive Androstane Receptor in Rat Hepatocytes
Published June 11, 2009; doi: 10.1124/dmd.108.022905 [Abstract] [PDF]  

8 June 2009

Emi Kamiyama, Daisuke Sugiyama, Daisuke Nakai, Shin-ich Miura, and Osamu Okazaki

Culture period-dependent change of function and expression of ABC transporters in Caco-2 cells
Published June 8, 2009; doi: 10.1124/dmd.109.027490 [Abstract] [PDF]  

Baskar Mannargudi, David McNally, William Reynolds, and Jack Uetrecht

Bioactivation of Minocycline to Reactive Intermediates by Myeloperoxidase, Horseradish Peroxidase and Hepatic Microsomes: Implications for Minocycline-Induced Lupus and Hepatitis
Published June 8, 2009; doi: 10.1124/dmd.109.027292 [Abstract] [PDF]  

1 June 2009

Oranun Kerdpin, Peter I Mackenzie, Kushari Bowalgaha, Moshe Finel, and John O Miners

Influence of N-terminal domain histidine and proline residues on the substrate selectivties of human UDP-glucuronosyltransferase (UGT) 1A1, 1A6, 1A9, 2B7 and 2B10
Published June 1, 2009; doi: 10.1124/dmd.109.028225 [Abstract] [PDF]  

Hao-Jie ZHU, David Appel, Yan Jiang, and John S. Markowitz

Age and sex-related expression and activity of carboxylesterase 1 and 2 in mouse and human liver
Published June 1, 2009; doi: 10.1124/dmd.109.028209 [Abstract] [PDF]  

Aik Jiang Lau and Thomas K. H. Chang

Inhibition of Human CYP2B6-Catalyzed Bupropion Hydroxylation by Ginkgo biloba Extract: Effect of Terpene Trilactones and Flavonols
Published June 1, 2009; doi: 10.1124/dmd.109.028118 [Abstract] [PDF]  

Shintaro Nakayama, Ryo Atsumi, Hideo Takakusa, Yoshimasa Kobayashi, Atsuhi Kurihara, Yoko Nagai, Daisuke Nakai, and Osamu Okazaki

A zone classification system for risk assessment of idiosyncratic drug toxicity using daily dose and covalent binding
Published June 1, 2009; doi: 10.1124/dmd.109.027797 [Abstract] [PDF]  

Anand K Deo and Stelvio M Bandiera

3-Ketocholanoic Acid Is The Major In Vitro Human Hepatic Microsomal Metabolite of Lithocholic Acid
Published June 1, 2009; doi: 10.1124/dmd.109.027763 [Abstract] [PDF]  

Anne-Sophie Belanger, Patrick Caron, Mario Harvey, Peter A. Zimmerman, Rajeev K. Mehlotra, and Chantal Guillemette

Glucuronidation of the antiretroviral drug efavirenz (EFV) by UGT2B7 and an in vitro investigation of drug-drug interaction with zidovudine (AZT)
Published June 1, 2009; doi: 10.1124/dmd.109.027706 [Abstract] [PDF] [Data Supplement]  

Kacper A Wojtal, Jyrki J Eloranta, Petr Hruz, Heike Gutmann, Juergen Drewe, Christoph Beglinger, Michael Fried, Gerd A Kullak-Ublick, and Stephan R Vavricka

Changes in mRNA expression levels of solute carrier transporters in inflammatory bowel disease patients
Published June 1, 2009; doi: 10.1124/dmd.109.027367 [Abstract] [PDF] [Data Supplement]  

Jin Kyung Lee, Koji Abe, Arlene S. Bridges, Nita J. Patel, Thomas J. Raub, Gary M. Pollack, and Kim L. R. Brouwer

Sex-dependent Disposition of Acetaminophen Sulfate and Glucuronide in the In Situ Perfused Mouse Liver
Published June 1, 2009; doi: 10.1124/dmd.109.026815 [Abstract] [PDF]  

28 May 2009

Yasufumi Fukano and Kouichi Kawazu

Disposition and Metabolism of a Novel Prostanoid Antiglaucoma Medication, Tafluprost, Following Ocular Administration to Rats
Published May 28, 2009; doi: 10.1124/dmd.108.024885 [Abstract] [PDF]  

21 May 2009

Angelique Stalmach, William Mullen, Denis Barron, Kenichi Uchida, Takao Yokota, Christophe Cavin, Heike Steiling, Gary Williamson, and Alan Crozier

Metabolite Profiling of Hydroxycinnamate Derivatives in Plasma and Urine Following the Ingestion of Coffee by Humans: Identification of Biomarkers of Coffee Consumption
Published May 21, 2009; doi: 10.1124/dmd.109.028019 [Abstract] [PDF]  

Chad M Thompson, Babasaheb Sonawane, and Roland C Grafstrom

The Ontogeny, Distribution and Regulation of Alcohol Dehydrogenase 3: Implications for Pulmonary Physiology
Published May 21, 2009; doi: 10.1124/dmd.109.027904 [Abstract] [PDF]  

Jie Cheng, Xiaochao Ma, Kristopher W. Krausz, Jeffery R. Idle, and Frank J. Gonzalez

Rifampicin-Activated Human PXR and CYP3A4 Induction Enhance Acetaminophen-Induced Toxicity
Published May 21, 2009; doi: 10.1124/dmd.109.027565 [Abstract] [PDF] [Data Supplement]  

Shuko Tachibana, Kouichi YOSHINARI, Tsubasa Chikada, Takayoshi Toriyabe, Kiyoshi Nagata, and Yasushi Yamazoe

Involvement of vitamin D receptor in the intestinal induction of human ABCB1
Published May 21, 2009; doi: 10.1124/dmd.109.027219 [Abstract] [PDF]  

19 May 2009

Shu-Ying Chang, Cliff Chen, Zheng Yang, and A. David Rodrigues

Further Assessment of 17-Ethinyl Estradiol as an Inhibitor of Different Human Cytochrome P450 Forms in Vitro
Published May 19, 2009; doi: 10.1124/dmd.109.026997 [Abstract] [PDF]  

18 May 2009

Vijaya M. Lakshmi, Fong-Fu Hsu, and Terry V. Zenser

Identification of new 2-amino-3-methylimidazo[4,5-f]quinoline urinary metabolites from beta-naphthoflavone-treated mice
Published May 18, 2009; doi: 10.1124/dmd.109.027342 [Abstract] [PDF]  

Albert (Al) Li

Evaluation of Luciferin-IPA as a CYP3A4 Substrate for Human Hepatocytes: Effects of Organic Solvents, P450 Inhibitors, and P450 Inducers
Published May 18, 2009; doi: 10.1124/dmd.109.027268 [Abstract] [PDF]  

15 May 2009

Albert Braeuning and Albrecht Buchmann

The glycogen synthase kinase inhibitor SB216763 is a partial agonist of the aryl hydrocarbon receptor
Published May 15, 2009; doi: 10.1124/dmd.109.027821 [Abstract] [PDF]  

Murali Subramanian, Michael Low, Charles W Locuson, and Timothy S. Tracy

CYP2D6-CYP2C9 Protein-Protein Interactions and Isoform-Selective Effects on Substrate Binding and Catalysis
Published May 15, 2009; doi: 10.1124/dmd.109.026500 [Abstract] [PDF]  

Sophie C Turfus, Mark C Parkin, David A Cowan, John M Halket, Norman W Smith, Robin A Braithwaite, Simon P Elliott, Glyn B Steventon, and Andrew T Kicman

Use of Human Microsomes and Deuterated Substrates; An Alternative Approach for the Identification of Novel Metabolites of Ketamine by Mass Spectrometry
Published May 15, 2009; doi: 10.1124/dmd.108.026328 [Abstract] [PDF]  

14 May 2009

Dirk R de Waart, Maria L Vlaming, Cindy Kunne, Alfred H. Schinkel, and R.P.J. Oude Elferink

Complex pharmacokinetic behaviour of ezetimibe depends on Abcc2, Abcc3 and Abcg2
Published May 14, 2009; doi: 10.1124/dmd.108.026146 [Abstract] [PDF]  

13 May 2009

R. Scott Obach

GLYCEROLYSIS OF ACYL GLUCURONIDES AS AN ARTIFACT OF IN VITRO DRUG METABOLISM INCUBATIONS
Published May 13, 2009; doi: 10.1124/dmd.109.027953 [Abstract] [PDF]  

Takeshi Izukawa, Miki Nakajima, Ryoichi Fujiwara, Hiroyuki Yamanaka, Tatsuki Fukami, Masataka Takamiya, Yasuhiro Aoki, Shin-ichi Ikushiro, Toshiyuki Sakaki, and Tsuyoshi Yokoi

Quantitative analysis of UGT1A and UGT2B expression levels in human livers
Published May 13, 2009; doi: 10.1124/dmd.109.027227 [Abstract] [PDF] [Data Supplement]  

Takuo Ogihara, Takashi Kano, Tamae Wagatsuma, Sho Wada, Hikaru Yabuuchi, Shigeki Enomoto, Kaori Morimoto, Yoshiyuki Shirasaka, Shoko Kobayashi, and Ikumi Tamai

Oseltamivir (Tamiflu^TM) is a substrate of PEPT1
Published May 13, 2009; doi: 10.1124/dmd.109.026922 [Abstract] [PDF]  

Abhishek Gulati, Douglas Boudinot, and Phillip M Gerk

BINDING OF LOPINAVIR TO HUMAN ₁-ACID GLYCOPROTEIN AND SERUM ALBUMIN
Published May 13, 2009; doi: 10.1124/dmd.109.026708 [Abstract] [PDF]  

Ken-ichi Umehara, Nobuaki Shirai, Takafumi Iwatsubo, Kiyoshi Noguchi, Takashi Usui, and Hidetaka Kamimura

Identification of human metabolites of YM758, a novel If channel inhibitor, and investigation of the transporter-mediated renal and hepatic excretion of these metabolites
Published May 13, 2009; doi: 10.1124/dmd.108.026294 [Abstract] [PDF]  

Laura P James, Lynda G Letzig, Pippa M Simpson, Edmund Capparelli, Dean W Roberts, Jack A Hinson, Timothy J Davern, and William M Lee

Pharmacokinetics of Acetaminophen Protein Adducts in Adults with Acetaminophen Overdose and Acute Liver Failure
Published May 13, 2009; doi: 10.1124/dmd.108.026195 [Abstract] [PDF]  

6 May 2009

Noriaki Sakai, Kentaro Q Sakamoto, Shoichi Fujita, and Mayumi Ishizuka

The importance of heterogeneous nuclear ribonucleoprotein K on Cytochrome P450 2D2 gene regulation: its binding is reduced in Dark Agouti rats
Published May 6, 2009; doi: 10.1124/dmd.109.027284 [Abstract] [PDF]  

Laddawan Senggunprai, Kouichi Yoshinari, and Yasushi Yamazoe

Selective role of SULT2A1 in the N-sulfoconjugation of quinolone drugs in human
Published May 6, 2009; doi: 10.1124/dmd.109.027441 [Abstract] [PDF]  

Sharon K Krueger, Marilyn C Henderson, Lisbeth K Siddens, Jonathan E VanDyke, Abby D Benninghoff, P Andrew Karplus, Bjarte Furnes, Daniel Schlenk, and David E Williams

Characterization of Sulfoxygenation and Structural Implications of Human Flavin-Containing Monooxygenase Isoform 2 (FMO2.1) Variants S195L and N413K
Published May 6, 2009; doi: 10.1124/dmd.109.027201 [Abstract] [PDF] [Data Supplement]  

Mario Pellegatti, Ellenia Bordini, Patrizia Fizzotti, Andy Roberts, and Brendan M Johnson

DISPOSITION AND METABOLISM OF RADIOLABELLED CASOPITANT IN HUMANS
Published May 6, 2009; doi: 10.1124/dmd.109.026781 [Abstract] [PDF]  

Xin Zhang, Sara K Quinney, J Christopher Gorski, David R. Jones, and Stephen D. Hall

Semi-physiologically-based pharmacokinetic models for the inhibition of midazolam clearance by diltiazem and its major metabolite
Published May 6, 2009; doi: 10.1124/dmd.109.026658 [Abstract] [PDF]  

Donglu Zhang, Kan He, Nirmala Raghavan, Lifei Wang, James Mitroka, Brad D Maxwell, Robert M Knabb, Charles A Frost, Alan Schuster, Feng Hao, Zheming Gu, W Griffith Humphreys, and Scott J Grossman

COMPARATIVE METABOLISM OF C-14 LABELED APIXABAN IN MICE, RATS, RABBITS, DOGS, AND HUMANS
Published May 6, 2009; doi: 10.1124/dmd.108.025981 [Abstract] [PDF] [Data Supplement]  

30 April 2009

Otito Frances Iwuchukwu, Jumoke Ajetunmobi, Din Ung, and Swati NAGAR

Characterizing the Effects of Common UGT1A6 and UGT1A1 Polymorphisms on Cis and Trans Resveratrol Glucuronidation
Published April 30, 2009; doi: 10.1124/dmd.109.027391 [Abstract] [PDF]  

Shuso Takeda, Noriyuki Usami, Ikuo Yamamoto, and Kazuhito Watanabe

Cannabidiol-2',6'-Dimethyl Ether, a Cannabidiol Derivative, Is a Highly Potent and Selective 15-Lipoxygenase Inhibitor
Published April 30, 2009; doi: 10.1124/dmd.109.026930 [Abstract] [PDF]  

Soumyajit Majumdar, Ketan Hippalgaonkar, and Ramesh Srirangam

Vitreal Kinetics of Quinidine in Rabbits in the Presence of Topically Co-administered P-gp Substrates/Modulators
Published April 30, 2009; doi: 10.1124/dmd.108.026450 [Abstract] [PDF]  

Odette A. Fahmi, Susan Hurst, David Plowchalk, Jack Cook, Feng Guo, Kuresh Youdim, Maurice Dickins, Alex Phipps, Amanda Darekar, Ruth Hyland, and Ronald Scott Obach

Investigation of Different Algorithms for Predicting Clinical Drug-Drug Interactions, Based on the Use of CYP3A4 in Vitro data; Predictions of Compounds as Precipitants of Interaction
Published April 30, 2009; doi: 10.1124/dmd.108.026252 [Abstract] [PDF] [Data Supplement]  

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