The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
July 2003
Vol. 306, No. 1
Contents
PERSPECTIVES IN PHARMACOLOGY
Ontogenesis of /3-Adrenoceptor Signaling: Implications for Perinatal Physiology and for Fetal Effects of Tocolytic Drugs
Theodore A. Slotkin, J. Todd Auman, and Frederic J. Seidler
ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION
Contribution of Organic Anion Transporter 3 (Slc22aS) to the Ryota Kikuchi, Hiroyuki Kusuhara,
Elimination of /j-Aminohippuric Acid and Benzylpenicillin Daisuke Sugiyama, and Yuichi Sugiyama
across the Blood-Brain Barrier
51
Transfer of L-a-Acetylmethadol (LAAM) and L-a-Acetyl-iV-normethadol (norLAAM) by the Perfused Human Placental Lobule
The Cytochrome P450 2B6 (CYP2B6) Is the Main Catalyst of Efavirenz Primary and Secondary Metabolism: Implication for HIV/AIDS Therapy and Utility of Efavirenz as a Substrate Marker of CYP2B6 Catalytic Activity
The Site-Specific Transport and Metabolism of Tacrolimus in Rat Small Intestine
Pliarmacokinetic and Pharmacodynamic Modeling of Recombinant Human Erythropoietin after Intravenous and Subcutaneous Dose Administration in Cynomolgus Monkeys
Effect of Atorvastatin on Apolipoprotein B100 Containing Lipoprotein Metabolism in Type-2 Diabetes
Tatiana N. Nanovskaya, Sujal V. Deshmukh, Rachel Miles, Steve Burmaster, and Mahmoud S. Ahmed
Bryan A. Ward, J Christopher Gorski,
David R. Jones, Stephen D. Hall,
David A. Flockhart, and Zeruesenay Desta
Shigeki Tamura, Yuji Tokunaga, Rinta Ibuki, Gordon L. Amidon, Hitoshi Sezaki, and Shinji Yamashita
Rohini Ramakrishnan, Wing K. Cheung, Francis Farrell, Linda Joffee, and William J. Jusko
Khadija Ouguerram, Thierry Magot, Yassine Zai'r, J. S. Marchini, Bernard Charbonnel, Herve Laouenan, and Michel Krempf
205
287
310
324
332
BEHAVIORAL PHARMACOLOGY
The Cannabinoid CB1 Antagonist iV-Piperidinyl-5-(4-
chloropheny 1) -1 -(2,4-dichloropheny 1) -4-methylpyrazole-3-carboxamide (SR-141716A) Differentially Alters the Reinforcing Effects of Heroin under Continuous Reinforcement, Fixed Ratio, and Progressive Ratio Schedules of Drug Self-Administration in Rats
Metabotropic Glutamate Subtype 5 Receptors Modulate Locomotor Activity and Sensorimotor Gating in Rodents
Risperidone Attenuates the Discriminative-Stimulus Effects of ^-Amphetamine in Humans
5-Hydroxytryptamine (5-HT)2 Receptor Involvement in Acute 5-HT-Evoked Scratching but Not in Allergic Pruritus Induced by Dinitrofluorobenzene in Rats
The Subtype-Selective Nicotinic Acetylcholine Receptor Agonist SIB-1553A Improves Both Attention and Memory Components of a Spatial Working Memory Task in Chronic Low Dose l-Methyl-4-phenyl-l,2,3,6-tetrahydropyridine-Treated Monkeys
M. Solinas, L. V. Panlilio, K. Antoniou, L. A. Pappas, and S. R. Goldberg
Gene G. Kinney, Maryann Burno, Una C. Campbell, Lisa M. Hernandez, Dana Rodriguez, Linda J. Bristow, and P. Jeffrey Conn
Craig R. Rush, William W. Stoops, Lon R. Hays, Paul E. A. Glaser, and Lon S. Hays
Hiroshi Nojima and E. Carstens
J. S. Schneider, J. P. Tinker, F. Menzaghi, and G. K. Lloyd
93
116
195
245
401
CARDIOVASCULAR
Enhancement of Angiogenesis by Endogenous Substance P Release and Neurokinin-1 Receptors During Neurogenic Inflammation
Nitric Oxide Inhibitor iV'-Nitro-L-arginine Methyl Ester Potentiates Induction of Heme Oxygenase-1 in Kidney Ischemia/Reperfusion Model; A Novel Mechanism for Regulation of the Oxygenase
BM-573, a Dual Thromboxane Synthase Inhibitor and Thromboxane Receptor Antagonist, Prevents Pig Myocardial Infarction Induced by Coronary Thrombosis
Protective Effect of Chronic Vitamin C Treatment on Endothelial Function of Apolipoprotein E-Detlcient Mouse Carotid Artery
Increased Endothelin-Induced Ca2+ Signaling, Tyrosine Phosphorylation, and Coronary Artery Disease in Diabetic Dyslipidemic Swine Are Prevented by Atorvastatin
Differential Effects of Phosphodiesterase-Sensitive and -Resistant Analogs of cAMP on Initiation of Contraction in Cardiac Ventricular Myocytes
Ectonucleotidase in Sympathetic Nerve Endings Modulates ATP and Norepinephrine Exocytosis in Myocardial Ischemia
Effects of Chronic Ethanol Feeding on Clonidine-Evoked Reductions in Blood Pressure, Heart Rate, and Their Variability: Time-Domain Analyses
CELLULAR AND MOLECULAR
Evidence That Nuclear Factor-icB Activation Is Critical in Oxidant-Induced Disruption of the Microtubule Cytoskeleton and Barrier Integrity and That Its Inactivation Is Essential in Epidermal Growth Factor-Mediated Protection of the Monolayers of Intestinal Epithelia
Green Tea Polyphenols Induce Differentiation and Proliferation in Epidermal Keratinocytes
Amide Local Anesthetics Potently Inhibit the Human Tandem Pore Domain Background K+ Channel TASK-2 (KCNK5)
The Use of Bioluminescence Resonance Energy Transfer 2 to Study Neuropeptide Y Receptor Agonist-Induced /3-Arrestin 2 Interaction
ENDOCRINE AND REPRODUCTIVE
Pharmacology of (2S,4Z)-iV-[(2S)-2-Hydroxy-2-phenyletliyl]-4-(methoxy imino)-1- [ (2' -methy 1[ 1,1' -biphenyl] -4-yl)carbonyl]-2-pyrrolidinecarboxamide, a New Potent and Selective Nonpeptide Antagonist of the Oxytocin Receptor
Helene C. Seegers, Vivienne C. Hood, 8
Bruce L. Kidd, Simon C. Cruwys, and David A. Walsh
Robert D. Mayer, Xiaojun Wang, and 43
Mahin D. Maines
S. Rolin, M. Petein, V. Tchana-Sato, 59
J. M. Dogne, P. Benoit, B. Lambermont, A. Ghuysen, P. Kolh, and B. Masereel
Takuya Matsumoto, Livius V. d'Uscio, 103
Daihiko Eguchi, Masahiko Akiyama, Leslie A. Smith, and Zvonimir S. Katusic
D. L. Lee, B. R. Wamhoff, L. C. Katwa, 132
H. K. Reddy, D. J. Voelker, J. L. Dixon, and M. Sturek
Gregory R. Ferrier and Susan E. Howletl 166
Casilde Sesti, Motohiro Koyama, 238
M. Johan Broekman, Aaron J. Marcus, and Roberto Levi
Mahmoud M. El-Mas and 271
Abdel A. Abdel-Rahman
A. Banan, A. Farhadi, J. Z. Fields, E. Mutlu, 13
L. Zhang, and A. Keshavarzian
Stephen Hsu, Wendy B. Bollag, Jill Lewis, 29
Qin Huang, Baldev Singh, Mohamed Sharawy, Tetsuya Yamamoto, and George Schuster
Christoph H. Kindler, Matthias Paul, 84
Hilary Zou, Canhui Liu, Bruce D. Winegar, Andrew T. Gray, and C. Spencer Yost
Magnus M. Berglund, Douglas A. Schober, 147
Michael A. Statnick, Patricia H. McDonald, and Donald R. Gehlert
Rocco Cirillo, Enrico Gillio Tos, 253
Matthias K, Schwarz, Anna Quattropani, Alexander Scheer, Marc Missotten, Jerome Dorbais, Anthony Nichols, Francesco Borrelli, Claudio Giachetti, Lucia Golzio, Paolo Marinelli, Russell J. Thomas, Claude Chevillard, Florence Laurent, Karitie Portet, Claude Barberis, and Andre Chollet
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL Toxicity of Acetaminophen, Salicylic Acid, and Caffeine for First-Passage Rat Renal Inner Medullary Collecting Duct
Cells
Ursodeoxycholate Reduces Ethinylestradiol Glucuronidation in the Rat: Role in Prevention of Estrogen-Induced Cholestasis
Glucagon-Like Peptide-2 and Common Therapeutics in a Murine Model of Ulcerative Colitis
Uptake of Serotonin at the Apical and Basolateral Membranes of Human Intestinal Epithelial (Caco-2) Cells Occurs through the Neuronal Serotonin Transporter (SERT)
Qi Cai, Natalia I. Dmitrieva, Luis F. Michea, 35
Gerson Rocha, Douglas Ferguson, and Maurice B. Burg
Enrique J. Sanchez Pozzi, 279
Fernando A. Crocenzi, Jose M. Pellegrino, Viviana A. Catania, Marcelo G. Luquita, Marcelo G. Roma, Emilio A. Rodriguez Garay, and Aldo D. Mottino
Marie-Claude L'Heureux and 347
Patricia L. Brubaker
Fatima Martel, Rosario Monteiro, and 355
Clara Lemos
INFLAMMATION AND IMMUNOPHARMACOLOGY
Receptor-Mediated Pharmacokinetics and Pharmacodynamics of Interferon-/31a in Monkeys
Donald E. Mager, Berend Neuteboom, 262
Constantinos Efthymiopoulos, Alain Munafo, and William J. Jusko
NEUROPHARMACOLOGY
Functional Characterization of YM928, a Novel Noncompetitive a:-Amino-3-hydroxy-5-niethyl-4-isoxazolepropionic Acid Receptor Antagonist
Human Pharmacology of Ayahuasca: Subjective and Cardiovascular Effects, Monoamine Metabolite Excretion, and Pharmacokinetics
Converging Protein Kinase Pathways Mediate Adenylyl Cyclase Superactivation upon Chronic 6-Opioid Agonist Treatment
Multidrug Resistance Protein MRP2 Contributes to Blood-Brain Barrier Function and Restricts Antiepileptic Drug Activity
Nocistatin and Prepro-Nociceptin/Orphanin FQ 160-187 Cause Nociception through Activation of GUo in Capsaicin-Sensitive and of Gs in Capsaicin-Insensitive Nociceptors, Respectively
Studies of fx-, k-, and S-Opioid Receptor Density and G Protein Activation in the Cortex and Thalamus of Monkeys
Effect of /V-(4-Acetyl-l-piperazinyl)-/Niluorobenzamide Monohydrate (FK960), an Antidementia Drug with a Novel Mechanism of Action, on Regional Cerebral Blood Flow and Glucose Metabolism in Aged Rhesus Macaques Studied with Positron Emission Tomography
Inhibitors of Cyclooxygenase-2, but Not Cyclooxygenase-1 Provide Structural and Functional Protection against Quinolinic Acid-Induced Neurodegeneration
Evaluation of the Ocular Hypotensive Response of Serotonin 5-HT,A and 5-HT2 Receptor Ligands in Conscious Ocular Hypertensive Cynomolgus Monkeys
Distinct Recognition of Substrates by the Human and Drosophila Serotonin Transporters
Synthesis and Characterization of NESS 0327: A Novel Putative Antagonist of the CB, Cannabinoid Receptor
Improved Brain Uptake and Pharmacological Activity of Dalargin Using a Peptide-Vector-Mediated Strategy
Af-(4-Tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-l(2//)-carbox-amide (BCTC), a Novel, Orally Effective Vanilloid Receptor 1 Antagonist with Analgesic Properties: I. In Vitro Characterization and Pharmacokinetic Properties
iV-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine-l(2#)-carbox-amide (BCTC), a Novel, Orally Effective Vanilloid Receptor 1 Antagonist with Analgesic Properties: II. In Vivo Characterization in Rat Models of Inflammatory and Neuropathic Pain
Kazushige Ohno, Rie Tsutsumi, 66
Naoyuki Matsumoto, Hiroshi Yamashita,
Yoko Amada, Jun-Ichi Shishikura,
Hiroshi Inami Shin-Ichi Yatsugi,
Masaraichi Okada, Shuichi Sakamoto, and
Tokio Yamaguchi
Jordi Riba, Marta Valle, Gloria Urbano, 73
Mercedes Yritia, Adelaida Morte, and Manel J. Barbanoj
Eva V. Varga, Marc K. Rubenzik, 109
Dagmar Stropova, Masano Sugiyama, Vanessa Grife, Victor J. Hruby, Kenner C. Rice, William R. Roeske, and Henry 1. Yamamura
Heidrun Potschka, Maren Fedrowitz, and 124
Wolfgang Loscher
Makoto Inoue, Toshiko Kawashima, 141
Richard G. Allen, and Hiroshi Ueda
M. C. H. Ko, H. Lee, C. Harrison, 179
M. J. Clark, H. F. Song, N. N. Naughton, J. H. Woods, and J. R. Traynor
Akihiro Noda, Hiroyuki Takamatsu, 213
Nobuya Matsuoka, Satosbi Koyama, Hideo Tsukada, and Shintaro Nishimura
Heather C. Salzberg-Brenhouse, 218
Er-Yun Chen, Dwaine F. Emerich,
Sam Baldwin, Ken Hogeland,
Sharon Ranelli, Denise Lafreniere,
Brigido Perdomo, Leah Novak,
Theodora Kladis, Karen Fu,
Anthony S. Basile, Jeffrey H. Kordower, and
Raymond T. Bartus
Jesse A. May, Marsha A. McLaughlin, 301
Najam A. Sharif, Mark R. Hellberg, and Thomas R. Dean
G. J. Rodriguez, D. L. Roman, K. J. White, 338
D. E. Nichols, and E. L. Barker
Stefania Ruiu, Gerard A. Pinna, 363
Giorgio Marchese, Jean-Mario Mussinu,
Pierluigi Saba, Simone Tambaro,
Paola Casti, Romina Vargiu, and Luca Pani
Christophe Rousselle, Philippe Clair, 371
Maria Smirnova, Yuri Kolesnikov,
Gavril W. Pasternak, Stephanie Gac-Breton,
Anthony R. Rees, Jean-Michel Scherrmann,
and Jamal Temsamani
Kenneth J. Valenzano, Elfrida R. Grant, 377
Gang Wu, Mohamed Hachicha, Lori Schmid, Laykea Tafesse, Qun Sun, Yakov Rotshteyn, Joseph Francis, James Limbcris, Shiazah Malik, Edward R. Whittemore, and Dianne Hodges
James D. Pomonis, James E. Harrison, 387
Lilly Mark, David R. Bristol,
Kenneth J. Valenzano, and Katharine Walker
Buprenorphine Blocks e- and jn-Opioid Receptor-Mediated Antinociception in the Mouse
SSR591813, a Novel Selective and Partial «4/32 Nicotinic Receptor Agonist with Potential as an Aid to Smoking Cessation
Hirokazu Mizoguchi, Amanda Spaulding, Randy LeHermann, Hsiang-En Wu, Hiroshi Nagase, and Leon F. Tseng
C. Cohen, O. E. Bergis, F. Galli,
A. W. Lochead, S. Jegham, B. Biton, J. Leonardon, P. Avenet, F. Sgard,
F. Besnard, D. Graham, A. Coste, A. Oblin,
O. Curet, C. Voltz, A. Gardes, D. Caille,
G. Perrault, P. George, P. Soubrie, and B. Scatton
394
407
TOXICOLOGY
Protein Kinase C Mediates Repair of Mitochondrial and Transport Functions after Toxicant-Induced Injury in Renal Cells
In Vivo Effect of PC-SPES on Prostate Growth and Hepatic CYP3A Expression in Rats
Characterization of Sulfamethoxazole and Sulfamethoxazole Metabolite-Specific T-Cell Responses in Animals and Humans
In Vitro Cytotoxicity of 4-Methylcatechol in Murine Tumor Cells: Induction of Apoptotic Cell Death by Extracellular Pro-Oxidant Action
ERRATUM
Correction to "Nitric Oxide-Donating Nonsteroidal Anti-Inflammatory Drugs Inhibit the Growth of Various Cultured Human Cancer Cells: Evidence of a Tissue Type-Independent Effect"
Grazyna Nowak
Ten Wadsworth, Hataya Poonyagariyagorn, Elinore Sullivan, Dennis Koop, and Charles E. Roselli
John Farrell, Dean J. Naisbitt, Nicola S. Drummond, Jan P. H. Depta, F. Javier Vilar, Munir Pirmohamed, and B. Kevin Park
Kyoji Morita, Hideki Arimochi, and Yoshinari Ohnishi
157
187
229
317
421