The Journal of PHARMACOLOGY And Experimental Therapeutics A Publication of the American Society for Pharmacology and Experimental Therapeutics November 2004 Vol. 311, No. 2 Contents PERSPECTIVES IN PHARMACOLOGY Corticotropin-Releasing Factor in Brain: A Role in Activation, Arousal, and Affect Regulation Stephen C. Heinrichs and George F. Koob ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION Plasma Membrane Localization of Multidrug ResistanceYan Zhang, John D. Schuetz, Associated Protein Homologs in Brain Capillary Endothelial William F. Elmquist, and Donald W. Miller Cells The Role of Advanced Glycation in Reduced Organic Cation Merlin C. Thomas, Christos Tikellis, Transport Associated with Experimental Diabetes Phillip Kantharidis, Wendy C. Burns, Mark E. Cooper, and Josephine M. Forbes 427 449 456 Differential Multidrug Resistance-Associated Protein 1 through 6 Isoform Expression and Function in Human Intestinal Epithelial Caco-2 Cells Hannah M. Prime-Chapman, Richard A. Fearn, Anne E. Cooper, Vanessa Moore, and Barry H. Hirst 476 G-Adrenergic Blockade Affects Initial Drug Distribution Due to Decreased Cardiac Output and Altered Blood Flow Distribution Michael J. Avrarn, Tom C. Krejrie, Thomas K. Henthorn, and Claus U. Niemann 617 Pharmacokinetics of Novel Dipeptide Ester Prodrugs of Acyclovir after Oral Administration: Intestinal Absorption and Liver Metabolism Banmeet S. Anand, Suresh Katragadda, and Ashim K. Mitra 659 Estrogen Regulation of the Cytochrome P450 3A Subfamily in Humans Eric T. Williams, Malgorzata Leyk, Steven A. Wrighton, Peter J. A. Davies, David S. Loose, Gregory L. Shipley, and Henry W. Strobel 728 Expression of Constitutive Androstane Receptor Splice Variants- in Human Tissues and Their Functional Consequences Jatinder K. Lamba, Vishal Lamba, Kazuto Yasuda, Yvonne S. Lin, Mahfoud Assem, Emma Thompson, Stephen Strom, and Erin Schuetz 811 Aron H. Lichtman, Donmienne Leung, Christopher C. Shelton, Alan Saghatelian, Christophe Hardouin, Dale L. Boger, and Benjamin F. Cravatt 441 Alexander R. Kosowski and Sture Liljequist 560 BEHAVIORAL PHARMACOLOGY Reversible Inhibitors of Fatty Acid Amide Hydrolase That Promote Analgesia: Evidence for an Unprecedented Combination of Potency and Selectivity The NR2B-Selective W-Methyl-D-aspartate Receptor Antagonist Ro 25-6981 [(±)-(R*,5*)-a-(4-HydroxyphenyI)-pmethyI-4-(phenyImethyl)-l-piperidine Propanol] Potentiates the Effect of Nicotine on Locomotor Activity and Dopamine Release in the Nucleus Accumbens The Opioid Receptor Like-1 Receptor Agonist Ro 64-6198 (lS,3aS-8-2,3,3a,4,5,6-Hexahydro-m-phcnalen-l-yl-l-phenyll,3j8-triaza-spiro[4.51decan-4-onc) Produces a Discriminative Stimulus in Rats Distinct from That of a jx, K, and 5 Opioid Receptor Agonist Cue Matthew D. Recker and Guy A. Higgins 652 Memantine Improves Spatial Learning in a Transgenic Mouse Model of Alzheimer's Disease Rimante Minkcviciene, Pradeep Banerjee, and Heikki Tanila 677 Drug Discrimination in Methamphetamine-Trained Monkeys: Effects of Monoamine Transporter Inhibitors Paul W. Czoty, Chinnasamy R. Ramanathan, Nicole H. Mutschler, Alexandras Makriyannis, and Jack Bergman 720 Effect of the D3 Dopamine Receptor Partial Agonist BP897 [Af-[4-(4-(2-Methoxyphenyl)piperazinyl)butyl]-2-naphthamide] on 1,-3,4-Dihydroxyphenylalanine-Induced Dyskinesias and Parkinsonism in Squirrel Monkeys Albert Hsu, Daniel M. Togasaki, Erwan Bezard, Pierre Sokoloff, J. William Langston, Donato A. Di Monte, and Maryka Quit 770 Yves Rival, Aline Stennevin, Laurence Puech, Anne Rouquette, Claudie Cathala, Fabrice Lestienne, Elisabeth Dupont-Passelaigue, Jean-Francois Patoiseau, Thierry Wurch, and Didier Junquero Pal Pacber, Anne Vaslin, Rita BenkS, Jon G. Mabley, Lucas Liaudet, Gyorgy Hasko, Anita Marton, Sandor Batkai, Mark Kollai, and Csaba Szabo 467 CARDIOVASCULAR Human Adipocyte Fatty Acid-Binding Protein (aP2) Gene Promoter-Driven Reporter Assay Discriminates Nonlipogenic Peroxisome Proliferator-Activated Receptor y Ligands A New, Potent Poly(ADP-ribosc) Polymerase Inhibitor Improves Cardiac and Vascular Dysfunction Associated with Advanced Aging 485 The Preparation and Characterization of Novel Peptide Antagonists to Thrombin and Factor Vila and Activation of Protease-Activated Receptor 1 Marvin T. Nieman, Mark Warnock, Ahmed A. K. Hasan, Fakhri Mahdi, Benedict R. Lucchesi, Nancy J. Brown, Laine J. Murphey, and Alvin H. Schmaier 492 Role of Prostaglandins in Mediating Differences in Human Internal Mammary and Radial Artery Relaxation Elicited by Hypoxia Sachin A. Gupte, Elias A. Zias, Mohan R. Sarabu, and Michael S. Wolin 510 Perillyl Alcohol Is an Angiogenesis Inhibitor Heleni Loutrari, Maria Hatziapostolou, Vassoula Skouridou, Evangelia Papadimitriou, Charis Roussos, Fragiskos N. Kolisis, and Andreas Papapetropoulos 568 Role of Protein Kinase CS in Endothelin-Induced Type I Collagen Expression in Cardiac Myofibroblasts Isolated from the Site of Myocardial Infarction Vishnu Chintalgattu and Laxmansa C. Katwa 691 . Changes in Phospholipid Content and Myocardial CalciumIndependent Phospholipase A2 Activity during Chronic Anthracycline Administration Jane McHowat, Luther M. Swift, Kimberly N. Crown, and Narine A. Sarvazyan 736 The Role of Rho Kinase and Extracellular Regulated KinaseMitogen-Activated Protein Kinase in a 2-AdrenoceptorMediated Vasoconstriction in the Porcine Palmar Lateral Vein Richard E. Roberts 742 Inhibitory Profile of SEA0400 [2-[4-[(2,5Difluorophenyl)methoxyjphenoxy]-5-ethoxyaniline] Assessed on the Cardiac Na+-Ca2+ Exchanger, NCX1.1 Candace Lee, Neeraj S. Visen, Naranjan S. Dhalla, Hoa Dinh Le, Michael Isaac, Platon Choptiany, Gil Gross, Alexander Omelchenko, Toshio Matsuda, Akemichi Baba, Kenzo Takahashi, Mark Hnatowich, and Larry V. Hryshko 748 Atsushi Fukunari, Ken Okamoto, Takeshi Nishino, Bryan T. Eger, Emil F. Pai, Miho Kamezawa, Ichimaro Yamada, and Norihisa Kato Alison J. Smith, Beth Oxley, Sallie Malpas, Gopalan V. Pillai, and Peter B. Simpson 519 CELLULAR AND MOLECULAR Y-700 [l-[3-Cyano-4-(2,2-dimethylpropoxy)phenyl]-lffpyrazole-4-carboxylic Acid]: A Potent Xanthine Oxidoreductase Inhibitor with Hepatic Excretion Compounds Exhibiting Selective Efficacy for Different j3 Subunits of Human Recombinant y-Aminobutyric AcidA Receptors /V-Butyryl Glucosamine Increases Matrix Gene Expression by Chondrocytes ' ■ . ■ . Mark W. Poustie, John Carran, Kevin McEleney, S. Jeffrey Dixon, Tassos P. Anastassiades, and Suzanne M. Bernier 601 610 Nobuhisa Tanaka, Takao Morita, Akihiro Nezu, Akihiko Tanimura, Itaru Mizoguchi, and Yosuke Tojyo 778 Barbara Tolloczko, Petra Turkewitsch, Mustafa Al-Chalabi, and James G. Martin 787 Aarti N. Desai, Kelly M. Standifer, and Douglas C. Eikenburg 794 Flavio F. Solca, Anke Baum, Elke Langkopf, Georg Dahmann, Karl-Heinz Heider, Frank Himmelsbach, and Jacques C. A. van Meel 502 Bernd Kaina, Ute Miihihausen, Andrea Piee-Staffa, Markus Christmann, Regine Garcia Boy, Frank Rosch, and Ralf Schirrmacher 585 Donald E. Mager, Darrell R. Abernethy, Josephine M. Egan, and Dariush Elahi 830 Cesar Menor, Maria D. Fernandez-Moreno, Jesus A. Fueyo, Oscar Escribano, Tomas Olleros, Encarna Arriaza, Carlos Cara, Michele Lorusso, Marco Di Paola, Irene D. Roman, and Luis G. Guijarro 668 Daniel Y. Hung, Gerhard A. Siebert, Ping Chang, Yuri G. Anissimov, and Michael S. Roberts 822 Kcrryn McCluskie, Mark A. Birrell, Sissie Wong, and Maria G. Belvisi 625 A Cyclooxygenase Metabolite of Anandamide Causes Inhibition of Interleukin-2 Secretion in Murine Splenocytes Cheryl E. Rockwell and Norbert E. Kaminski 683 Nicotine Activates Nuclear Factor of Activated T Cells c2 (NFATc2) and Prevents Cell Cycle Entry in T Cells Ashley A. Frazer-Abel, Shairaz Baksh, Susan P. Fosmire, Derail Willis, Angela M. Pierce, Heather Meylemans, Darwin S. Linthicum, Steven J. Burakoff, Teresa Coons, Donald Bellgrau, and Jaime F. Modiano 758 Shu-Cheng Chen, Tsui-Jung Chang, and Fong-Sen Wu 529 Susan K. Sullivan, Robert E. Petroski, Gail Verge, Raymond S. Gross, Alan C. Foster, and Dimitri E. Grigoriadis Alan C. Foster, Mary Ann Pelleymounter, Mary Jane Cullen, Dacie Lewis, Margaret Joppa, Ta Kung Chen, Haig P. Bozigian, Raymond S. Gross, and Kathleen R. Gogas Smriti [yengar, Amy A. Webster, Susan K. Hemrick-Luecke, Jimmy Yu Xu, and Rosa Maria A. Simmons 537 Signaling Mechanisms Involved in Protease-Activated Receptor-1-Mediated Interleukin-6 Production by Human Gingival Fibroblasts LY-294002 [2-(4-Morpholinyl)-8-phenyI-4//-l-benzopyran-4one] Affects Calcium Signaling in Airway Smooth Muscle Cells Independently of Phosphoinositide 3-Kinase Inhibition Simultaneous a2B- and /32-Adrenoceptor Activation Sensitizes the «2n-Adrenoceptor for Agonist-Induced Down-Regulation CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY Inhibition of Epidermal Growth Factor Receptor Activity by Two Pyrimidopyrimidine Derivatives Inhibition of O6-Methylguanine-DNA Methyltransferase by Glucose-Conjugated Inhibitors: Comparison with Nonconjugated Inhibitors and Effect on Fotemustine and Temozolomide-Induced Cell Death ENDOCRINE AND REPRODUCTIVE Exendin-4 Pharmacodynamics: Insights from the Hyperglycemic Clamp Technique GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL Azathioprine Acts upon Rat Hepatocyte Mitochondria and Stress-Activated Protein Kinases Leading to Necrosis: Protective Role of /V-Acetyl-L-cysteine Disposition Kinetics of Propranolol Isomers in the Perfused Rat Liver INFLAMMATION AND IMMUNOPHARMACOLOGY Nitric Oxide as a Noninvasive Biomarker of Lipopolysaccharide-Induced Airway Inflammation: Possible Role in Lung Neutrophilia NEUROPHARMACOLOGY Competitive Inhibition of the Capsaicin Receptor-Mediated Current by Dehydroepiandrosterone in Rat Dorsal Root Ganglion Neurons Characterization of the Interaction of Indiplon, a Novel Pyrazolopyrimidine Sedative-Hypnotic, with the GABAA Receptor In Vivo Pharmacological Characterization of Indiplon, a Novel Pyrazolopyrimidine Sedative-Hypnotic Efficacy of Duloxetine, a Potent And Balanced SerotoninNorepinephrine Reuptake Inhibitor in Persistent Pain Models in Rats Bupropion (Zyban, Wellbutrin) Inhibits Nicotine-Induced Viral Reactivation in Herpes Simplex Virus Type 1 Latent Rabbits Marvin E. Myles, Ann M. Azcuy, Ngoc T. Nguyen, Eric R. Reisch, Steven A. Barker, Hilary W. Thompson, and James M. Hill 547 576 640 Ro 64-6198 [(lS,3aS)-8-(2,3,3a,4,5,6-Hexahydro-lff-phenalen-lyl)-l-phenyl-l,3,8-triaza-spiro[4.5]decan-4-one] Acts Differently from Nociceptin/Orphanin FQ in Rat Periaqueductal Gray Slices Lih-Chu Chiou, Kuang-Chieh Chuang, Juergen Wichmann, and Geo Adam 645 Serotonin1B Receptors in the Ventral Tegmental Area Modulate Cocaine-Induced Increases in Nucleus Accumbens Dopamine Levels L. E. O'Dell and L. H. Parsons 711 The Role of 5-Hydroxytryptamine3 Receptors in the Vagal Afferent Activation-Induced Inhibition of the First Cervical Dorsal Horn Spinal Neurons Projected from Tooth Pulp in the Rat Takeshi Tanimoto, Mamoru Takeda, Tosbimi Nishikawa, and Shigeji Matsumoto 803 Endogenous u-Serine Is Involved in Induction of Neuronal Death by A'-Methyl-D-aspartate and Simulated Ischemia in Rat Cerebrocortical Slices Hiroshi Katsuki, Mild Nonaka, Hisashi Shirakawa, Toshiaki Kume, and Akinori Akaike 836 The Bile Acid Tauroursodeoxycholic Acid Modulates Phosphorylation and Translocation of Bad via Phosphatidylinositol 3-Kinase in Glutamate-Induced Apoptosis of Rat Cortical Neurons Rui E. Castro, Susana Sola, Rita M. Ramalho, Clifford J. Steer, and Cecilia M. P. Rodrigues 845 Naoya Matsunaga, Naomi Nakamura, Noriyo Yoneda, Tian Qin, Hideyuki Terazono, Hideto To, Shun Higuchi, and Shigehiro Ohdo 594 Jean-Claude Lavoie, Therese Rouleau, and Philippe Chessex 634 Maria F. M. Braga, Edna F. R. Pereira, Arpad Mike, and Edson X. Albuquerque 700 Andrea C. Simmonds, Burhan I. Ghanayem, Ashish Sharma, Christopher A. Reilly, Brandie Millen, Garold S. Yost, and Poh-Gek Forkert 853 TOXICOLOGY Influence of Feeding Schedule on 24-h Rhythm of Hepatotoxicity Induced by Acetaminophen in Mice Interaction between Ascorbate and Light-Exposed Riboflavin Induces Lung Remodeling Pb2+ via Protein Kinase C Inhibits Nicotinic Cholinergic Modulation of Synaptic Transmission in the Hippocampus ERRATUM Correction to "Bioactivation of 1,1-Dichloroethylene by CYP2E1 and CYP2F2 in Murine Lung"