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The Journal of PHARMACOLOGY And Experimental Therapeutics A Publication of the American Society for Pharmacology and Experimental Therapeutics October 2004 Vol. 311, No. 1 Contents ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION Multiple Novel Nonsynonymous CYP2B6 Gene Polymorphisms Thomas Lang, Kathrin Klein, Tanja Richter, in Caucasians: Demonstration of Phenotypic Null Alleles Arne Zibat, Reinhold Kerb, Michel Eichelbaum, Matthias Schwab, and Ulrich M. Zanger GHB (y-Hydroxybutyrate) Carrier-Mediated Transport across the Blood-Brain Barrier Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the Hepatic Uptake of Pitavastatin in Humans Gemfibrozil and Its Glucuronide Inhibit the Organic Anion Transporting Polypeptide 2 (OATP2/OATP1B1:SLC2JA6)Mediated Hepatic Uptake and CYP2C8-Mediated Metabolism of Cerivastatin: Analysis of the Mechanism of the Clinically Relevant Drug-Drug Interaction between Cerivastatin and Gemfibrozil Indranil Bhattacharya and Kathleen M. K. Boje Masaru Hirano, Kazuya Maeda, Yoshihisa Shitara, and Yuichi Sugiyama Yoshihisa Shitara, Masaru Hirano, Hitoshi Sato, and Yuichi Sugiyama 34 92 139 228 Pharmacokinetics of Erythromycin in Rabbit Corneas after Single-Dose Infusion: Role of P-Glycoprotein as a Barrier to in Vivo Ocular Drug Absorption Surajit Dey, Sriram Gunda, and Ashim K. Mitra 246 Effect of Quinidine on the 10-Hydroxylation of fi-Warfarin: Species Differences and Clearance Projection Qing Chen, Eugene Tan, John R. Strauss, Zhoupeng Zhang, Judith E. Fenyk-Melody, Catherine Booth-Genthe, Thomas H. Rushmore, Ralph A. Stearns, David C. Evans, Thomas A. Baillie, and Wei Tang 307 XP13512 [(±)-l-([(a-Isobutanoyloxyethoxy)carbonyl]aniinomethyl)1-cyclohexane Acetic Acid], A Novel Gabapcntin Prodrug: I. Design, Synthesis, Enzymatic Conversion to Gabapentin, and Transport by Intestinal Solute Transporters XP13512 [(±)-l-([(a-Isobutanoyloxyethoxy)carbonyl]aminomethyl) 1-cyclohexane Acetic Acid], A Novel Gabapentin Prodrug: II. Improved Oral Bioavailability, Dose Proportionality, and Colonic Absorption Compared with Gabapentin in Rats and Monkeys , Kenneth C. Cundy, Russell Branch, Tania Chernov-Rogan, Tracy Dias, Tono Estrada, Karin Hold, Kerry Koller, Xiaoli Liu, Adam Mann, Matt Panuwat, Stephen P. Raillard, Shubhra Upadhyay, Quincey Q. Wu, Jia-Ning Xiang, Hui Yan, Noa Zerangue, Cindy X. Zhou, Ronald W. Barrett, and Mark A. Gallop Kenneth C. Cundy, Thamil Annamalai, Lin Bu, Josephine De Vera, Jenny Estrela, Wendy Luo, Payal Shirsat, Allan Torneros, Fenmei Yao, Joan Zou, Ronald W. Barrett, mdMfli'kA.iGallop 315 324 BEHAVTORAL PHARMACOLOGY Antiallodynic Effects of Loperamide and Fentanyl against Topical Capsaicin-Induced Allodynia in Unanesthetized Primates Antinociceptive Structure-Activity Studies with EnkephalinBased Opioid Glycopeptides CARDIOVASCULAR iV-Methyi-D-aspartate Receptor Blockade Inhibits Cardiac Inflammation in the Mg2+-Deficient Rat The Protective Effect of Superoxide Dismutase Mimetic M40401 on Balloon Injury-Related Neointima Formation: Role of the Lectin-Like Oxidized Low-Density Lipoprotein Receptor-1 Regulation of Gene Expression in Cardiomyocytes by Thyroid Hormone and Thyroid Hormone Analogs 3,5Diiodothyropropionic Acid and CGS 23425 [iV-[3,5-Dimetliyl4-(4'-hydroxy-3'-isopropylphenoxy)-phenyl]-oxamic Acid] Pharmacology of the Urotensin-II Receptor Antagonist Palosuran (ACT-058362; l-[2-(4-Benzyl-4-hydroxy-piperidin-lyl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea Sulfate Salt): First Demonstration of a Pathophysiological Role of the Urotensin System Characterization of Cannabinoid Modulation of Sensory Neurotransmission in the Rat Isolated Mesenteric Arterial Bed Effects of Pravastatin on the Expression of ATP-Binding Cassette Transporter Al CELLULAR AND MOLECULAR p53-Dependent Apoptotic Mechanism of a New Designer Bimetallic Compound Tri-phenyl Tin Benzimidazolethiol Copper Chloride (TPT-CuCI2): In Vivo Studies in Wistar Rats as Well as in Vitro Studies in Human Cervical Cancer Cells Identification of Amino Acid Residues Involved in the Inactivation of Cytochrome P450 2B1 by Two Acetylenic Compounds: The Role of Three Residues in Nonsubstrate Recognition Sites Insulin Signaling Regulates y-Glutamyleysteine Ligase Catalytic Subunit Expression in Primary Cultured Rat Hepatocytes Fenofibrate Impairs Rat Mitochondrial Function by Inhibition of Respiratory Complex I Domain Swapping in the Human Histamine H, Receptor Ligand-Directed Functional Heterogeneity of Histamine H, Receptors: Novel Dual-Function Ligands Selectively Activate and Block H rMediated Phospholipase C and Adenylyl Cyclase Signaling Eduardo R. Butelman, Todd J. Harris, and Mary Jeanne Kreek 155 Nura O. Elmagbari, Richard D. Egleton, Michael M. Palian, John J. Lowery, Wendi R. Schmid, Peg Davis, Edita Navratilova, Muthu Dhanasekaran, Charles M. Keyari, Henry I. Yamarnura, Frank Porreca, Victor J. Hruby, Robin Polt, and Edward J. Bilsky 290 M. Isabel Tejero-Taldo, 8 Joanna J. Chmielinska, Grace Gonzalez, I. Tong Mak, and William B. Weglicki Carolina Muscoli, Iolanda Sacco, Wanessa Alecce, Ernesto Palma, Robert Nisticb, Nicola Costa, Fabrizio Clementi, Domenicantonio Rotiroti, Francesco Romeo, Daniela Salvemini, Jawahar L. Mchta, and Vincenzo Mollace Cynthia Adamson, Niranjan Maitra, Joseph Bahl, Kevin Greer, Scott Klcwer, James Hoying, and Eugene Morkin Martine Clozel, Christoph Binkert, Magdalena Birker-Robaczewska, Celine Boukhadra, Shuang-Shuang Ding, Walter Fischli, Patrick Hess, Boris Mathys, Keith Morrison, Celia Miiller, Claus Miiller, Oliver Nayler, Changbin Qiu, Markus Rey, Michael W. Scherz, Jorg Velker, Thomas Weller, Jian-Fei Xi, and Patrick Ziltener Marnie Duncan, David A. Kendall, and Vera Ralevic 44 164 204 411 Hitoshi Ando, Shuichi Tsuruoka, Hisashi Yamamoto, Toshinari Takamura, Shuichi Kaneko, and Akio Fujimura 420 Naseruddin Hod, De-e Zhu, Zhiyin Song, Zhengsheng Wu, Sartaj Tabassum, and Mian Wu 22 Linda B. Von Weymarn, Chitra Sridar, and Paul F. Hollenberg 71 Sang K. Kim, Kimberley J. Woodcroft, Sarah S. Khodadadeh, and Raymond F. Novak Barbara Brunmair, Andrea Lest, Katrin Staniek, Florian Gras, Nicole Scharf, Michael Roden, Hans Nohl, Werner Waldhausl, and Clemens Fiirnsinn 99 109 Remko A. Bakker, Guido Dees, Juan J. Carriilo, Raymond G. Booth, Juan F. Lopez-Gimenez, Graeme Milligan, Philip G. Strange, and Rob Leurs 131 Nader H. Moniri, Dawn Covington-Strachan, and Raymond G. Booth 274 CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY Kaurene Diterpene Induces Apoptosis in Human Leukemia Cells Partly through a Caspase-8-Dependent Pathway Intratumoral Administration of Methotrexate Bound to Activated Carbon Particles: Antitumor Effectiveness against Human Colon Carcinoma Xenografts and Acute Toxicity in Mice GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL Interleukin 1/3-Induced Production of H2O2 Contributes to Reduced Sigmoid Colonic Circular Smooth Muscle Contractility in Ulcerative Colitis Masuo Kondoh, Ikue Suzuki, Masao Sato, Fumihiro Nagashima, Siro Simizu, Motoki Harada, Makiko Fujii, Hiroyuki Osada, Yoshinori Asakawa, and Yoshiteru Watanabe Yuen Nakase, Akeo Hagiwara, Syuichi Kin, Ken-ichirou Fukuda, Tadao Ito, Tsuyoshi Takagi, Jyunshin Fujiyama, Chohei Sakakura, Eigo Otsuji, and Hisakazu Yamagishi Weibiao Cao, Matthew D. Vrees, Fabio M. Potenti, Karen M. Harnett, Claudio Fiocchi, and Victor E. Pricolo 115 382 60 The Modulating Role of Nuclear Factor-/dt in the Action of a7-Nicotinic Acetyteholine Receptor and Cross-Talk between 5-Lipoxygenase and CycIooxygenase-2 in Colon Cancer Growth Induced by 4-(iV-Methyl-iV-nitrosamino)-l-{3-pyridyl)1-butanone Yi N. Ye, Edgar S. L. Liu, Vivian Y. Shin, William K. K. Wu, and Chi H. Cho 123 Effect of Omeprazole on Gastric Adenosine A2 and A2A Receptor Gene Expression and Function Linda Yip, Henry Chi Hang Leung, and Yin Nam Kwok 180 Effect of Prolyl Endopeptidase on Digestive-Resistant Gliadin Peptides in Vivo Justin L. Piper, Gary M. Gray, and Chaitan Khosla 213 Regulation of Rat Hepatocyte Function by P2Y Receptors: Focus on Control of Glycogen Phosphorylase and Cyclic AMP by 2-Methylthioadenosine 5'-Diphosphate C. Jane Dixon, John F. Hall, Tania E. Webb, and Michael R. Boarder 334 Charles S. Bockman, Michael R. Bruchas, Wanyun Zeng, Kelly A. O'Connell, Peter W. Abel, Margaret A. Scofield, and Frank J. Dowd 364 Marcio A. F. de Godoy, Ana Maria de Oliveira, and Satish Rattan 394 Atsufumi Kawabata, Satoko Kubo, Tsuyoshi Ishiki, Naoyuki Kawao, Fumiko Sekiguchi, Ryotaro Kuroda, Morley D. Hollenberg, Toru Kanke, and Naohiro Saito 402 Alfredo Vannacci, Lucia Giannini, Maria Beatrice Passani, Annamaria Di Felice, Simone Pierpaoli, Giovanni Zagli, Ornella Fantappie, Roberto Mazzanti, Emanuela Masini, and Pier Francesco Mannaioni 256 Submandibular Gland Acinar Cells Express Multiple a xAdrenoceptor Subtypes Angiotensin II-Induced Relaxation of Anococcygeus Smooth Muscle via Desensitization of ATj Receptor, and Activation of AT2 Receptor Associated with Nitric-Oxide Synthase Pathway Proteinase-Activated Receptor-2-Mediated Relaxation in Mouse Tracheal and Bronchial Smooth Muscle: Signal Transduction Mechanisms and Distinct Agonist Sensitivity INFLAMMATION AND IMMUNOPHARMACOLOGY The Endocannabinoid 2-Arachidonylglycerol Decreases the Immunological Activation of Guinea Pig Mast Cells: Involvement of Nitric Oxide and Eicosanoids NEUROPHARMACOLOGY Methamphetamine Neurotoxicity in Dopamine Nerve Endings of the Striatum Is Associated with Microglial Activation The ./V-Methyl-D-aspartate Receptor Inhibitory Potencies of Aromatic Inhaled Drugs of Abuse: Evidence for Modulation by Cation-7r Interactions Serofendic Acid, a Sulfur-Containing Diterpenoid Derived from Fetal Calf Serum, Attenuates Reactive Oxygen SpeciesInduced Oxidative Stress in Cultured Striatal Neurons Electrophysiological, Pharmacological, and Molecular Evidence for a7-Nicotinic Acetylcholine Receptors in Rat Midbrain Dopamine Neurons ■y-Hydroxybutyrate Increases a Potassium Current and Decreases the H-Current in Hippocampal Neurons via GABAB Receptors David M. Thomas, Paul D. Walker, 1 Joyce A. Benjamins, Timothy J. Geddes, and Donald M. Kuhn Douglas E. Raines, Fredrick Gioia, Robert J. Claycomb, and Renna J. Stevens 14 Fumitaka Osakada, Yuka Kawato, Toshiaki Kume, Hiroshi Katsuki, Hachiro Sugimoto, and Akinori Akaike 51 Jie Wu, Andrew A. George, Katherine M. Schroeder, Lin Xu, Syndia MarxerMiller, Linda Lucero, and Ronald J. Lukas Paul Schweitzer, Marisa Roberto, Samuel G. Madamba, and George Robert Siggins 80 172 The Serotonin1A Receptor Partial Agonist S15535 [4(Benzodioxan-5-yl)l-(indan-2-yl)piperazine] Enhances Cholinergic Transmission and Cognitive Function in Rodents: A Combined Neurochemical and Behavioral Analysis Antiepileptic Drug Treatment of Nonconvulsive Seizures Induced by Experimental Focal Brain Ischemia /3-Estradiol, Dehydroepiandrosterone, and Dehydroepiandrosterone Sulfate Protect against iV-Methyl-Daspartate-Induced Neurotoxicity in Rat Hippocampal Neurons by Different Mechanisms Chronic Morphine Treatment Alters A'-Methyl-D-aspartate Receptors in Freshly Isolated Neurons from Nucleus Accumbens Ethanol Suppression of Ventral Tegmental Area GABA Neuron Electrical Transmission Involves A'-Methyl-D-aspartate Receptors Negative Feedback Regulation of Nigrostriatal Dopamine Release: Mediation by Striatal Dl Receptors Short-Term Cocaine Treatment Causes Neuroadaptive Changes in Gaq and G«n Proteins in Rats Undergoing Withdrawal Intrathecal Protease-Activated Receptor Stimulation Produces Thermal Hyperalgesia through Spinal Cyclooxygenase Activity Edaravone Protects against Hypoxia/Ischemia-Induced Endoplasmic Reticulum Dysfunction TOXICOLOGY Expression and Induction of Cytochromes P450 in Rat White Adipose Tissue Thioether Metabolites of 3,4-Methylenedioxyamphetamine and 3,4-Methylenedioxymethamphetamine Inhibit Human Serotonin Transporter (hSERT) Function and Simultaneously Stimulate Dopamine Uptake into hSERT-Expressing SK-NMC Cells Development of a Real-Time Polymerase Chain ReactionBased Method for the Measurement of Relative Allelic Expression and Identification of CYP2A13 Alleles with Decreased Expression in Human Lung Mark J. Millan, Alain Gobert, Sylvain Roux, Roger Porsolt, Alfredo Meneses, Mirjana Carli, Benjamin Di Cara, Robert Jaffard, Jean-Michel Rivet, Pierre Lestage, Elisabeth Mocaer, Jean-Louis Peglion, and Anne Dekeyne A. J. Williams, F. C. Tortella, X. M. Lu, J. E. Moreton, and J. A. Hartings 190 220 Kenichi Kurata, Minoru Takebayashi, Shigeru Morinobu, and Shigeto Yamawaki 237 Gilles Martin, Ana Guadano-Ferraz, Beatriz Morte, Serge Ahmed, George F. Koob, Luis de Lecea, and George R. Siggins 265 Sarah H. Stobbs, Allison J. Ohran, Matthew B. Lassen, David W. Allison, J. Elliott Brown, and Scott C. Steffensen 282 Sanjida S. Saklayen, Omar S. Mabrouk, and Elizabeth A. Pehek 342 Gonzalo A. Carrasco, Katerina J. Damjanoska, Deborah N. D'Souza, Yahong Zhang, Francisca Garcia, George Battaglia, Nancy A. Muma, and Louis D. Van de Kar 349 Lee Koetzner, Joshua A. Gregory, and Tony L. Yaksh 356 Xin Qi, Yasunobu Okuma, Torn Hosoi, and Yasuyuki Nomura 388 Kouichi Yoshinari, Takeshi Sato, Nao Okino, Junko Sugatani, and Masao Miwa 147 Douglas C. Jones, Serrine S. Lau, and Terrence J. Monks 298 Xiuling Zhang, Michele Caggana, Tracey L. Cutler, and Xinxin Ding 373