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Pharmacology


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The Journal of

PHARMACOLOGY



And Experimental Therapeutics

A Publication of the American Society for Pharmacology and Experimental Therapeutics



November 2005

Vol.315, No. 2



Contents


PERSPECTIVES IN PHARMACOLOGY

In Silico Predictions of Blood-Brain Barrier Penetration: Considerations to "Keep in Mind"

ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION Functional Characterization of Rat Organic Anion Transporter 5 (Slc22al9) at the Apical Membrane of Renal Proximal Tubules

Enantiomer/Enantiomer Interactions between the S- and R-Isomers of Omeprazole in Human Cytochrome P450 Enzymes: Major Role of CYP2C19 and CYP3A4

Functional Analysis of Organic Cation Transporter 3 Expressed in Human Placenta
Jay T. Goodwin and David E. Clark 477

Naohiko Anzai, Promsuk Jutabha, 534

Atsushi Enomoto, Hirokazu Yokoyama,

Hiroshi Nonoguchi, Taku Hirata,

Katsuko Shiraya, Xin He, Seok Ho Cha,

Michio Takeda, Hiroki Miyazaki,

Takeshi Sakata, Kimio Tomita,

Takashi Igarashi, Yoshikatsu Kanai, and

Hitoshi Endou

Xue-Qing Li, Lars Weidolf, 777

Roger SJmonsson, and Tommy B. Andersson

Ryoko Sata, Hisakazu Ohtani, 888

Masayuki Tsujimoto, Hideyasu Murakami,

Noriko Koyabu, Takanori Nakamura,

Takeshi Uchiumi, Michihiko Kuwano,

Hideaki Nagata, Kiyomi Tsukimori,

Hitoo Nakano, and Yasufumi Sawada


BEHAVIORAL PHARMACOLOGY

Assessment of the Influence of Histaminergic Actions on Cocaine-Like Effects of 3a-Diphenylmethoxytropane Analogs

Chronopharmacological Study of Antidepressants in Forced Swimming Test of Mice

Characterization of a Novel Bivalent Morphinan Possessing k Agonist and [i Agonist/Antagonist Properties

Effect of GABA Agonists and GABA-A Receptor Modulators on Cocaine- and Food-Maintained Responding and Cocaine Discrimination in Rats

Vera C. Campbell, Theresa A. Kopajtic, 631

Amy Hauck Newman, and Jonathan L. Katz

Kentarou Ushijima, Hiromi Sakaguchi, 764

Yuki Sato, Hideto To, Satoru Koyanagi, Shun Higuchi, and Shigehiro Ohdo

Jennifer L. Mathews, Xuemei Peng, 821

Wennan Xiong, Ao Zhang,

S. Stevens Negus, John L. Neumeyer, and

Jean M. Bidlack

Andrew C. Barrett, S. Stevens Negus, 858



Nancy K. Mello, and S. Barak Came

Despite Similar Anxiolytic Potential, the 5-Hydroxytryptamine 2C Receptor Antagonist SB-242084 [6-Chloro-5-methyl-l-[2-(2-methylpyrid-3-yloxy)-pyrid-5-yl Carbamoyl] Indoline] and Chlordiazepoxide Produced Differential Effects on Electroencephalogram Power Spectra

CARDIOVASCULAR

The Effect of Dipyridamole on Vascular Cell-Derived Reactive Oxygen Species

Effects of Phytoestrogens Genistein and Daidzein on Prostacyclin Production by Human Endothelial Cells

Donitriptan Decreases Jugular Venous Oxygen Saturation in Rats in the Absence of Cranial Vasoconstriction: An Overlooked Mechanism of Antimigraine Action?

DAF-FM (4-Amino-5-methylamino-2',7'-difluorofluorescein) Diacetate Detects Impairment of Agonist-Stimulated Nitric Oxide Synthesis by Elevated Glucose in Human Vascular Endothelial Cells: Reversal by Vitamin C and L-Sepiapterin

CELLULAR AND MOLECULAR

In Vitro Evaluation of the Angiostatic Potential of Drugs Using an Endothelialized Tissue-Engineered Connective Tissue

Impairment of Hyperpolarization-Activated, Cyclic Nucleotide-Gated Channel Function by the Intravenous General Anesthetic Propot'ol

Differential Regulation of Cystic Eibrosis Transmembrane Conductance Regulator by Interferon y in Mast Cells and Epithelial Cells

Prevention of the Ultraviolet B-Mediated Skin Photoaging by a Nuclear Factor kB Inhibitor, Parthenolirte

Transcriptional Regulation of Activating Transcription Factor 3 Involves the Early Growth Response-1 Gene

Fibrotic Lung Fibroblasts Show Blunted Inhibition by cAMP Due to Deficient cAMP Response Element-Binding Protein Phosphorylation

Analysis of Allosterism in Functional Assays

Curciimin Suppresses Interleukin 1/3-Mediated Microsomal Prostaglandin E Synthase 1 by Altering Early Growth Response Gene 1 and Other Signaling Pathways

Inhibition of Autoantigen Expression by (-)-Epigallocatechin-3-gaIlate (the Major Constituent of Green Tea) in Normal Human Cells

Evans Blue Is a Specific Antagonist of the Human Epithelial Na+ Channel 8-Subunit

Agonist-Directed Trafficking of Response by Endocannabinoids Acting at CB2 Receptors

Characterization of Isoprenaline- and Salmeterol-Stimulatcd Interactions between /32-Adrenoceptors and J3-Arrestin 2 Using /3-Galactosidasc Complementation in C2C12 Cells

CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY

Interaction with Blood Components Plays a Crucial Role in Asialoglycoprotein Receptor-Mediated in Vivo Gene Transfer by Galactosylated Lipoplex

Human U251 Glioma Cell Proliferation Is Suppressed by HET0016 [A'-Hydroxy-A''-(4-butyl-2-methylphenyl)formamidine], a Selective Inhibitor of CYP4A

Sandor Kantor, Rita Jakus, Eszter Molnar, 921

Norbert Gyongyosi, Attila Toth, Laszlo Detari, and Gyorgy Bagdy

Subrata Chakrabarti, Olga Vitseva, 494

David Iyu, Sonia Varghese, and Jane E. Freedman

Carlos Hermenegildo, Pilar J. Oviedo, 722

Miguel Angel Garcfa-Perez, Juan J. Tarin, and Antonio Cano

Robert Letienne, Jean-Christophe Blanchet, 849

Estellc Sole, Gareth W. John, and Bruno Le Grand

Jian-Zhong Sheng, Dianna Wang, and 931

Andrew P. Braun

Pierre-Luc Tremblay, Francois Berthod, 510

Lucie Germain, and Francois A. Auger

Luisa P. Caeheaux, Norbert Topf, 517

Gareth R. Tibbs, Ulrich R. Schaefer,

Roberto Levi, Neil L. Harrison,

Geoffrey W. Abbott, and Peter A. Goldstein

Marianna Kulka, Rene Dery, 563

Drew Nahirney, Marek Duszyk, and A. Dean Befus

Kiyotaka Tanaka. Junichi Hasegawa, 624

Kaori Asamitsu, and Takashi Okamolo

Frank G. Bottone, Jr., Yuseok Moon, 668

Brenda Alston-Mills, and Thomas E. Eling

Xiaoqiu Liu, Shu Qiang Sun, and 678

Rennolds S. Ostrom

Frederick J. Ehlert 740

Yuseok Moon, Wayne C. Glasgow, and 788

Thomas E. Eling

Stephen Hsu, Douglas P. Dickinson, 805

Haiyan Qin, Carol Lapp, David Lapp,

James Borke, Douglas S. Walsh,

Wendy B. Bollag, Hubert Stoppler,

Telsuya Yamamoto, Tokio Osaki, and

George Schuster

Hisao Yamamura, Shinya Ugawa, 965

Takashi Ueda, and Shoichi Shimada

Jennifer L. Shoemaker, Michael B. Ruckle, 828

Philip R. Mayeux, and Paul L. Pralher

Alison A. Carter and Stephen J. Hill 839

Shintaro Fumoto, Shigeru Kawakami, 484

Kosuke Shigeta, Yuriko Higuchi, Fumiyoshi Yamashita, and Mitsuru Hashida

Meng Guo, Richard J. Roman, 526

John R. Falck, Paul A. Edwards, and A. Guillermo Scicli



Synthetic Pyrrole-Imidazole Polyamide Inhibits Expression of the Human Transforming Growth Factor-01 Gene

Coformulated Af-Octanoyl-glucosylceramidc Improves Cellular Delivery and Cytotoxicity of Liposomal Doxorubicin

Pharmacoproteomic Effects of Isoniazid, Ethambutol, and JV-Geranyl-Af'-(2-adamantyl)ethane-l,2-diamine (SQ109) on Mycobacterium tuberculosis H37Rv

ENDOCRINE AND DIABETES

Acute and Chronic Effects of the Incretin Enhancer Vildagliptin in Insulin-Resistant Rats

Yu-Mu Lai, Noboru Fukuda, Takahiro Ueno, 571

Hiroyuki Matsuda, Satoshi Saito, Koichi Matsumoto, Hirohito Ayame, Toshikazu Bando, Hiroshi Sugiyama, Hideo Mugishima, and Ka/uo Serie

Robert Jan Veldman, Gerben A. Koning, 704

Albert van Hell, Shuraila Zerp,

Stefan R. Vink, Gert Storm, Marcel Verheij,

and Wim J. van Blitterswijk

Lee Jia, Lori Coward, Gregory S. Gorman, 905

Patricia E. Noker, and Joseph E. Tomaszewski

B. F. Burkey. X. Li, L. Bolognese, B. Balkan, M. Mone, M. Russell, T. E. Hughes, and P. R. Wang




GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

A New ATP-Sensitive Potassium Channel Opener Protects the Kidney from Hypertensive Damage in Spontaneously Hypertensive Rats

Signal Transduction for Proteinase-Activated Receptor-2-Triggered Prostaglandin E2 Formation in Human Lung Epithelial Cells
DPI-221 [4-((«-S)-a-((2S,5JR)-2,5-Dimethyl-4-(3-fluorobenzyl)-l-pipera7Jnyl)henzyl)-AyV-diethylbenzamide]: A Novel Nonpeptide o" Receptor Agonist Producing Increased Micturition Interval in Normal Rats

Prostanoids Secreted by Alveolar Macrophages Enhance Ionic Currents in Swine Tracheal Submucosal Gland Cells

Short-Term Exposure of Renal Proximal Tubules to Gentamicin Increases Long-Term Multidrug Resistance Protein 2 (Abcc2) Transport Function and Reduces Nephrotoxicant Sensitivity

The Effects of Extracellular Purines and Pyrimidines on Human Airway Smooth Muscle Cells

Hao Xue, Ying-Li Zhang, Gno-Shu Liu, and 501

Hai Wang

Naoyuki Kawao, Mami Nagasaki, 576

Keita Nagasawa, Satoko Kubo,

Kelly Cushing, Tetsuyuki Wada,

Fumiko Sekiguchi, Seiji Ichida,

Morley D. Hollenberg,

Wallace K. MacNaughton,

Hiroyuki Nishikawa, and

Atsufumi Kawabata

Jonathon D. S. Holt, Michael J. Watson, 601

Jane P. Chang, Scott J. O'Neill, Ke Wei, William Pendergast, Peter J. Gengo, and Kwen-Jen Chang

Huiling Liu, Abulkhair M. Mamoon, and 729

Jerry 3VL Farley, Sr.

Sylvia Notenboom, David S. Miller, 912

Leon H. Kuik, Paul Smits, Frans G. M. Russel, and Rosalinde Masereeuw

Vasanthi Govindaraju, James G. Martin. 941

Karim Maghni, Pasquale Ferraro, and Marie-Claire Michoud


INFLAMMATION AND IMMUNOPHARMACOLOGY

Anti-Inflammatory Effects of Inhibiting the Amine Oxidase Activity of Semicarbazide-Sensitive Amine Oxidase

Nociceptive Effect of Subcutaneously Injected Interleukin-12 Is Mediated by Endothelin (ET) Acting on ETB Receptors in Rats

MEN16132, a Novel Potent and Selective Nonpeptide Kinin B2 Receptor Antagonist: In Vivo Activity on Bradykinin-Induced Bronchoconstriction and Nasal Mucosa Microvascular Leakage in Anesthetized Guinea Pigs

Indirect CB2 Receptor and Mediator-Dependent Stimulation of Human Whole-Blood Neutrophils by Exogenous and Endogenous Cannabinoids

Prostaglandin E2 Enhances Neurotrophin-4 Production via EP3 Receptor in Human Keratinocytes

Gender Differences in the Endotoxin-Induced Inflammatory and Vascular Responses: Potential Role of Poly(ADP-ribose) Polymerase Activation

Luisa M. Salter-Cid, Eric Wang, 553

Anne M. O'Rourke, Andrew Miller, Hongfeng Gao, Li Huang, Arnie Garcia, and Matthew D. Linnik

Waldiceu A. Verri, Jr., Rodrigo O. Molina, 609

leda R. S. Schivo, Thiago M. Cunha,

Carlos A. Parada, Stephen Poole,

Sergio H. Ferreira, and Fernando Q. Cunha

Claudio Valenti, Cecilia Cialdai, 616

Sandro Giuliani, Alessandro Lecci, Manuela Tramontana, Stefania Meini, Laura Quartara, and Carlo Alberto Maggi

Birgit Kraft and Hans G. Kress 641

Naoko Kanda, Satsuki Koike, and 796

Shinichi Watanabe



Jon G. Mabley, Eszter M. Horvath, 812

Kanneganti G. K. Murthy,

Zsuzsanna Zsengeller, Anne Vaslin,

Rita Benko, Mark Kollai, and Csaba Szabo



NEUROPHARMACOLOGY

Human Expanded Polyglutamine Androgen Receptor Mutants in Neurodegeneration as a Novel Ligand Target

The Metabotropic Glutamate 5 Receptor Antagonist 3-[(2-MethyI-l,3-thiazoI-4-yl)ethynyl]-pyridine Reduces Ethanol Self-Administration in Multiple Strains of Alcohol-Preferring Rats and Regulates Olfactory Glutamatergic Systems

Prolonged Increase in the Sensitivity of the Posterior Ventral Tegmental Area to the Reinforcing Effects of Ethanol following Repeated Exposure to Cycles of Ethanol Access and Deprivation

Methyllycaconitine Prevents Methamphetamine-Induced Effects in Mouse Striatum: Involvement of al Nicotinic Receptors

Effect of Morphine on Deep Dorsal Horn Projection Neurons Depends on Spinal GABAergic and Glycinergic Tone: Implications for Reduced Opioid Effect in Neuropathic Pain

Fenobam: A Clinically Validated Nonbenzodiazepine Anxiolytic Is a Potent, Selective, and Noncompetitive mGlu5 Receptor Antagonist with Inverse Agonist Activity

Subnanomolar Concentrations of Thrombin Enhance the Volume-Sensitive Efflux of Taurine from Human 1321NI

Astrocytoma Cells

General Anesthetic-Induced Channel Gating Enhancement of 5-Hydroxytryptamine Type 3 Receptors Depends on Receptor Subunit Composition

Nicotine Regulates DARPP-32 (Dopamine- and cAMP-Regulated Phosphoprotein of 32 kDa) Phosphorylation at Multiple Sites in Neostriatal Neurons

Glycyl-Glutamine, an Endogenous j3-Endorphin-Derived Peptide, Inhibits Morphine-Induced Conditioned Place Preference, Tolerance, Dependence, and Withdrawal

Calcium-Acting Drugs Modulate Expression and Development of Chronic Tolerance to Nicotine-Induced Antinociception in Mice

TOXICOLOGY

Peroxynitrite-Induced Mitochondria! and Endonuclease-Mediated Nuclear DNA Damage in Acetaminophen

Hepatotoxicity

Handling of the Homocysteine S-Conjugate of Methylmercury by Renal Epithelial Cells: Role of Organic Anion Transporter 1 and Amino Acid Transporters

ERRATUM

Corrections to "Heine-Reversible Impairment of CYP2B1/2 Induction in Heme-Depleted Rat Hepatocytes in Primary Culture: Translational Control by a Hepatic a-Subunit of the Eukaryotic Initiation Factor Kinase?"

Takashi Furutani, Ken-ichi Takeyama, 545

Masahiko Tanabe, Hiroshi Koutoku,

Saya Ito, Nobuaki Taniguchi, Eriko Suzuki,

Masafumi Kudoh, Masayuki Shibasaki,

Hisataka Shikama, and Shigeaki Kato

Michael S. Cowen, Elvan Djouma, and 590

Andrew J. Lawrence

Zachary A. Rodd, Richard L. Bell, 648

Victoria K. McQueen, Michelle R. Davids, Cathleen C. Hsu, James M. Murphy, Ting-Kai Li, Lawrence Lumeng, and William J. McBride

Elena Escubedo, Carlos Chipana, 658

M6nica Perez-Sanchez, Jordi Camarasa, and David Pubill

Yan-Ping Chen, Shao-Rui Chen, and 696

Hui-Lin Pan

Richard H. P. Porter, Georg Jaeschke, 711

Will Spooren, Theresa M. Ballard,

Bernd Biittelmann, Sabine Kolczewski,

Jens-Uwe Peters, Eric Prinssen,

Jiirgen Wichmann, Eric Vieira,

Andreas Miihlemann, Silvia Gatti,

Vincent Mutel, and Pari Malherbe

Tooba A. Cheema, Caroline E. Ward, and 755

Stephen K. Fisher

Ken Solt, Renna J. Stevens, Paul A. Davies, 771

and Douglas E. Raines

Miho Hamada, Joseph P. Hendrick, 872

Gregory R. Ryan, Mahomi Kuroiwa, Hideho Higashi, Masatoshi Tanaka, Angus C. Nairn, Paul Greengard, and Akinori Nishi

Sinan Cavun, Gokhan Goktalay, and 949

William R. Millington

M. I. Damaj 959

Cathleen Cover, Abdellah Mansouri, 879

Tamara R. Knight, Mary Lynn Bajt,

John J. Lemasters, Dominique Pessayre, and

Hartmut Jaeschke

Rudolfs K. Zalups and Sarfaraz Ahmad 896

Xing-Mei Han, Gene Lee, Colleen Hefner, 970



Jacquelyn J. Maher, and Maria Almira Correia


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