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