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DRUG METABOLISM AND DISPOSITION A Publication of the American Society for Pharmacology and Experimental Therapeutics September 2009 Vol. 37, No. 9 CONTENTS SHORT COMMUNICATIONS □ S Glucuronidation of the Antiretroviral Drug Efavirenz by UGT2B7 and an in Vitro Investigation of Drug-Drug Interaction with Zidovudine. AnneSophie Bélanger, Patrick Caron, Mario Harvey, Peter A. Zimmerman, Rajeev K. Mehlotra, and Chantal Guillemette . . . . . . . . . . . . . . . . . . . 1793 In Vitro Inhibition of Multiple Cytochrome P450 Isoforms by Xanthone Derivatives from Mangosteen Extract. Robert S. Foti, Josh T. Pearson, Dan A. Rock, Jan L. Wahlstrom, and Larry C. Wienkers . . . . . . . . . . . . . . . . . . . . . . . . 1848 Aromatic Substitution Reaction of 2-Chloropyridines Catalyzed by Microsomal Glutathione S-Transferase 1. Kazuko Inoue, Tomoyuki Ohe, Kenichi Mori, Takeshi Sagara, Yasuyuki Ishii, and Masato Chiba . . . . . . . . . . . . . . . . . . . . . . . . . 1797 □ S Involvement of Human Organic Cation Transporter 1 in the Hepatic Uptake of 1-(2-Methoxyethyl)-2methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9dihydro-1H-naphtho[2,3-d]imidazolium Bromide (YM155 Monobromide), a Novel, Small Molecule Survivin Suppressant. Megumi Iwai, Tsuyoshi Minematsu, Shinichi Narikawa, Takashi Usui, and Hidetaka Kamimura . . . . . . . . . . . . . . . . 1856 Contrasting Influence of NADPH and a NADPHRegenerating System on the Metabolism of Carbonyl-Containing Compounds in Hepatic Microsomes. Christopher S. Mazur, John F. Kenneke, Michael-Rock Goldsmith, and Cather Brown . . 1801 ARTICLES Bioactivation of Minocycline to Reactive Intermediates by Myeloperoxidase, Horseradish Peroxidase, and Hepatic Microsomes: Implications for Minocycline-Induced Lupus and Hepatitis. Baskar Mannargudi, David McNally, William Reynolds, and Jack Uetrecht . . . . . . . . . . . . . 1806 Age- and Sex-Related Expression and Activity of Carboxylesterase 1 and 2 in Mouse and Human Liver. Hao-Jie Zhu, David I. Appel, Yan Jiang, and John S. Markowitz . . . . . . . . . . . . . . . . . 1819 Identification and Profiling of Circulating Metabolites of Atazanavir, a HIV Protease Inhibitor. R. ter Heine, M. J. X. Hillebrand, H. Rosing, E. C. M. van Gorp, J. W. Mulder, J. H. Beijnen, and A. D. R. Huitema . . . . . . . . . . . . . . . . . . . . . . . . . 1826 Modulation of the Partition Coefficient between Octanol and Buffer at pH 7.4 and pKa to Achieve the Optimum Balance of Blood Clearance and Volume of Distribution for a Series of Tetrahydropyran Histamine Type 3 Receptor Antagonists. Tanya Hay, Rhys Jones, Kevin Beaumont, and Mark Kemp . . . . . . . . . . . . . . . . . . . . . . . . . 1864 □ S Changes in mRNA Expression Levels of Solute Carrier Transporters in Inflammatory Bowel Disease Patients. Kacper A. Wojtal, Jyrki J. Eloranta, Petr Hruz, Heike Gutmann, Jürgen Drewe, Alex Staumann, Christoph Beglinger, Michael Fried, Gerd A. Kullak-Ublick, and Stephan R. Vavricka . . . . . . . . . . . . . . . . . . . . . . . . . . . 1871 Continued on next page Drug Metabolism and Disposition (ISSN 0090-9556) is published monthly (one volume per year) by the American Society for Pharmacology and Experimental Therapeutics, 9650 Rockville Pike, Bethesda, MD 20814-3995; e-mail: [email protected]; web site: aspet.org. Periodicals postage paid at Bethesda, MD, and at additional mailing offices. POSTMASTER: Send address changes to Drug Metabolism and Disposition, 9650 Rockville Pike, Bethesda, MD 20814-3995. Subscription rates: U.S.: $400.00; outside the U.S.: $479. Single copy: $36. GST Tax Number for Canadian subscribers: BN:13489 2330 RT, Indexed or abstracted by Biochemistry & Biophysics Citation Index®, Biological Abstracts, BIOSIS Previews Database, BioSciences Information Services, Current Awareness in Biological Sciences, Current Contents®/Life Sciences, EMBASE/Excerpta Medica, Index Medicus, International Pharmaceutical Abstracts, Medical Documentation Service®, Reference Update®, Research Alerts®, Science Citation Index®, SciSearch®, and SIIC Data Bases Copyright © 2009 by the American Society for Pharmacology and Experimental Therapeutics. All rights reserved. Printed in the U.S.A. Downloaded from dmd.aspetjournals.org at ASPET Journals on November 2, 2016 Up-Regulation of UDP-Glucuronosyltransferase (UGT) 1A4 by 17-Estradiol: A Potential Mechanism of Increased Lamotrigine Elimination in Pregnancy. Huiqing Chen, Kyunghee Yang, Suyoung Choi, James H. Fischer, and Hyunyoung Jeong . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 1841 Contents (cont’d.) Effect of Membrane Cholesterol on BSEP/Bsep Activity: Species Specificity Studies for Substrates and Inhibitors. Emese Kis, Enikő Ioja, Tunde Nagy, Lajos Szente, Krisztina Herédi-Szabó, and Péter Krajcsi . . . . . . . . . . . . . . . . . . . . . . . . 1878 Inhibition of Human CYP2B6-Catalyzed Bupropion Hydroxylation by Ginkgo biloba Extract: Effect of Terpene Trilactones and Flavonols. Aik Jiang Lau and Thomas K. H. Chang . . . . . . . . . . . . 1931 3-Ketocholanoic Acid Is the Major in Vitro Human Hepatic Microsomal Metabolite of Lithocholic Acid. Anand K. Deo and Stelvio M. Bandiera . . 1938 Methadone Induces the Expression of Hepatic DrugMetabolizing Enzymes through the Activation of Pregnane X Receptor and Constitutive Androstane Receptor. Antonia H. Tolson, Haishan Li, Natalie D. Eddington, and Hongbing Wang . . . 1887 Influence of N-Terminal Domain Histidine and Proline Residues on the Substrate Selectivities of Human UDP-Glucuronosyltransferase 1A1, 1A6, 1A9, 2B7, and 2B10. Oranun Kerdpin, Peter I. Mackenzie, Kushari Bowalgaha, Moshe Finel, and John O. Miners . . . . . . . . . . . . . . . . . . . 1948 Culture Period-Dependent Change of Function and Expression of ATP-Binding Cassette Transporters in Caco-2 Cells. Emi Kamiyama, Daisuke Sugiyama, Daisuke Nakai, Shin-ichi Miura, and Osamu Okazaki . . . . . . . . . . . . . . . . . . . . . . 1956 Metabolism of Ticlopidine in Rats: Identification of the Main Biliary Metabolite as a Glutathione Conjugate of Ticlopidine S-Oxide. Shinji Shimizu, Ryo Atsumi, Tsunenori Nakazawa, Yuko Fujimaki, Kenichi Sudo, and Osamu Okazaki . . . . . . . . . . . . . . . 1904 Thyroid Hormone Is Necessary for Expression of Constitutive Androstane Receptor in Rat Hepatocytes. Hidekazu Ooe, Junko Kon, Hideki Oshima, and Toshihiro Mitaka . . . . . . . . . . . . . . . . . . 1963 Sex-Dependent Disposition of Acetaminophen Sulfate and Glucuronide in the in Situ Perfused Mouse Liver. Jin Kyung Lee, Koji Abe, Arlene S. Bridges, Nita J. Patel, Thomas J. Raub, Gary M. Pollack, and Kim L. R. Brouwer . . . . . . . . . . . 1916 A Zone Classification System for Risk Assessment of Idiosyncratic Drug Toxicity Using Daily Dose and Covalent Binding. Shintaro Nakayama, Ryo Atsumi, Hideo Takakusa, Yoshimasa Kobayashi, Atsushi Kurihara, Yoko Nagai, Daisuke Nakai, and Osamu Okazaki . . . . . . . . . . . . . . . . . . . 1970 An in Vitro Evaluation of the Victim and Perpetrator Potential of the Anticancer Agent Laromustine (VNP40101M), Based on Reaction Phenotyping and Inhibition and Induction of Cytochrome P450 Enzymes. Alaa-Eldin F. Nassar, Ivan King, Brandy L. Paris, Lois Haupt, Florence NdikumMoffor, Rebecca Campbell, Etsuko Usuki, Jennifer Skibbe, Dan Brobst, Brian W. Ogilvie, and Andrew Parkinson . . . . . . . . . . . . . . . . . . . . 1922 □ S Genetic Polymorphisms in the TATA Box and Upstream Phenobarbital-Responsive Enhancer Module of the UGT1A1 Promoter Have Combined Effects on UDP-Glucuronosyltransferase 1A1 Transcription Mediated by Constitutive Androstane Receptor, Pregnane X Receptor, or Glucocorticoid Receptor in Human Liver. Ye Li, David Buckley, Shuang Wang, Curtis D. Klaassen, and Xiao-bo Zhong . . . . . . . . . . . . . . . . . . . . . . . . . . . . 1978 □ S Supplemental material is available online at http://dmd.aspetjournals.org. About the cover: Zone classification of IDT risk assessment in accordance with daily dose and covalent binding in human hepatocytes. See article by Nakayama et al. on page 1970 of this issue. Downloaded from dmd.aspetjournals.org at ASPET Journals on November 2, 2016 Substrate-Dependent Functional Alterations of Seven CYP2C9 Variants Found in Japanese Subjects. 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 . . . . . . . . . . 1895