DRUG METABOLISM AND DISPOSITION

A Publication of the American Society for Pharmacology and Experimental Therapeutics

November 2013 Vol. 41, No. 11

CONTENTS

ARTICLES Expression of Efflux Transporters in Human Ocular

Characterization of Monocarboxylate Transporter 6: Downloaded from Expression in Human Intestine and Transport Tissues. Peng Chen, Hao Chen, Xinjie Zang, of the Antidiabetic Drug Nateglinide. Noriko Min Chen, Haoran Jiang, Shasha Han, and Kohyama, Hisae Shiokawa, Masayuki Ohbayashi, XianggenWu...... 1934 Yasuna Kobayashi, and Toshinori Yamamoto . . . .1883 Determination of Intracellular Unbound Concentra- tions and Subcellular Localization of Drugs in

s Different Hydrolases Involved in Bioactivation of dmd.aspetjournals.org Prodrug-Type Angiotensin Receptor Blockers: Rat Sandwich-Cultured Hepatocytes Compared Carboxymethylenebutenolidase and Carboxy- with Liver Tissue. Nathan D. Pfeifer, Kevin B. lesterase 1. Tomoko Ishizuka, Yasushi Yoshigae, Harris, Grace Zhixia Yan, and Kim L. R. NobuyukiMurayama,andTakashiIzumi...... 1888 Brouwer...... 1949 s Relationship between CYP1A2 Localization and Lipid A Pharmacometric Approach to Investigate the Impact Microdomain Formation as a Function of Lipid of Methylxanthine Abstinence and Caffeine Con- Composition. Lauren M. Brignac-Huber, James R. sumption on CYP1A2 Activity. Vidya Perera, at ASPET Journals on September 29, 2021 Reed,MarilynK.Eyer,andWayneL.Backes.... 1896 Annette S. Gross, Alan Forrest, Cornelia B. Landersdorfer, Hongmei Xu, Sihem Ait-Oudhia, andAndrewJ.McLachlan...... 1957 The Letrozole Phase 1 Metabolite Carbinol as a Novel Probe Drug for UGT2B7. Jana C. Precht, Werner Schroth, Kathrin Klein, Hiltrud Brauch, Evgeny Metformin Sinusoidal Efflux from the Liver Is Krynetskiy, Matthias Schwab, and Thomas E. Consistent with Negligible Biliary Excretion Mürdter...... 1906 and Absence of Enterohepatic Cycling. Maciej J. Zamek-Gliszczynski, Jing Q. Bao, Jeffrey S. Day,andJ.WilliamHiggins...... 1967 Identification and Characterization of Psoralen and Isopsoralen as Potent CYP1A2 Reversible and Time-Dependent Inhibitors in Human and Rat LETTER TO THE EDITOR Preclinical Studies. Xiao-Mei Zhuang, Yu-Huan Endogenous 4b-Hydroxycholesterol-to-Cholesterol Zhong, Wei-Bin Xiao, Hua Li, and Chuang Lu . . .1914 Ratio Is Not a Validated Biomarker for the Assessment of CYP3A Activity. Joseph D. Ma, The Nonenzymatic Reactivity of the Acyl-Linked Anne N. Nafziger, and Joseph S. Bertino, Jr. . . .1972 Metabolites of Mefenamic Acid toward Amino and Thiol Functional Group Bionucleophiles. Howard Horng and Leslie Z. Benet...... 1923

s Supplemental material is available online at http://dmd.aspetjournals.org.

About the cover: Localization of MCT6 protein in human small intestine. See article by Kohyama et al. on page 1883 of this issue.