The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
Vol. 306, No. 1
July 2003
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-iVnormethadol (norLAAM) by the Perfused Human Placental
Lobule
Tatiana N. Nanovskaya, Sujal V. Deshmukh,
Rachel Miles, Steve Burmaster, and
Mahmoud S. Ahmed
205
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
Bryan A. Ward, J Christopher Gorski,
David R. Jones, Stephen D. Hall,
David A. Flockhart, and Zeruesenay Desta
287
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
310
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
BEHAVIORAL PHARMACOLOGY
The Cannabinoid CB1 Antagonist iV-Piperidinyl-5-(4chloropheny 1) -1 -(2,4-dichloropheny 1) -4-methylpyrazole-3carboxamide (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-tetrahydropyridineTreated Monkeys
324
332
M. Solinas, L. V. Panlilio, K. Antoniou,
L. A. Pappas, and S. R. Goldberg
93
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
116
J. S. Schneider, J. P. Tinker, F. Menzaghi,
and G. K. Lloyd
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
Helene C. Seegers, Vivienne C. Hood,
8
Bruce L. Kidd, Simon C. Cruwys, and
David A. Walsh
Robert D. Mayer, Xiaojun Wang, and
Mahin D. Maines
43
S. Rolin, M. Petein, V. Tchana-Sato,
J. M. Dogne, P. Benoit, B. Lambermont,
A. Ghuysen, P. Kolh, and B. Masereel
59
Takuya Matsumoto, Livius V. d'Uscio,
Daihiko Eguchi, Masahiko Akiyama, Leslie
A. Smith, and Zvonimir S. Katusic
103
D. L. Lee, B. R. Wamhoff, L. C. Katwa,
H. K. Reddy, D. J. Voelker, J. L. Dixon, and
M. Sturek
132
Gregory R. Ferrier and Susan E. Howletl
166
Casilde Sesti, Motohiro Koyama,
M. Johan Broekman, Aaron J. Marcus, and
Roberto Levi
238
Mahmoud M. El-Mas and
Abdel A. Abdel-Rahman
271
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
A. Banan, A. Farhadi, J. Z. Fields, E. Mutlu,
L. Zhang, and A. Keshavarzian
13
Stephen Hsu, Wendy B. Bollag, Jill Lewis,
Qin Huang, Baldev Singh, Mohamed Sharawy,
Tetsuya Yamamoto, and George Schuster
29
Christoph H. Kindler, Matthias Paul,
Hilary Zou, Canhui Liu, Bruce D. Winegar,
Andrew T. Gray, and C. Spencer Yost
84
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]-2pyrrolidinecarboxamide, a New Potent and Selective
Nonpeptide Antagonist of the Oxytocin Receptor
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
Magnus M. Berglund, Douglas A. Schober,
Michael A. Statnick, Patricia H. McDonald, and
Donald R. Gehlert
147
Rocco Cirillo, Enrico Gillio Tos,
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
253
Qi Cai, Natalia I. Dmitrieva, Luis F. Michea,
Gerson Rocha, Douglas Ferguson, and
Maurice B. Burg
35
Enrique J. Sanchez Pozzi,
Fernando A. Crocenzi, Jose M. Pellegrino,
Viviana A. Catania, Marcelo G. Luquita, Marcelo
G. Roma, Emilio A. Rodriguez Garay, and Aldo D.
Mottino
279
Glucagon-Like Peptide-2 and Common Therapeutics in a
Murine Model of Ulcerative Colitis
Marie-Claude L'Heureux and
Patricia L. Brubaker
347
Uptake of Serotonin at the Apical and Basolateral Membranes
of Human Intestinal Epithelial (Caco-2) Cells Occurs through
the Neuronal Serotonin Transporter (SERT)
Fatima Martel, Rosario Monteiro, and
Clara Lemos
355
INFLAMMATION AND IMMUNOPHARMACOLOGY
Receptor-Mediated Pharmacokinetics and Pharmacodynamics
of Interferon-/31a in Monkeys
NEUROPHARMACOLOGY
Functional Characterization of YM928, a Novel
Noncompetitive a:-Amino-3-hydroxy-5-niethyl-4isoxazolepropionic 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
Donald E. Mager, Berend Neuteboom,
Constantinos Efthymiopoulos, Alain Munafo,
and William J. Jusko
262
Kazushige Ohno, Rie Tsutsumi,
Naoyuki Matsumoto, Hiroshi Yamashita,
Yoko Amada, Jun-Ichi Shishikura,
Hiroshi Inami Shin-Ichi Yatsugi,
Masaraichi Okada, Shuichi Sakamoto, and
Tokio Yamaguchi
66
Jordi Riba, Marta Valle, Gloria Urbano,
Mercedes Yritia, Adelaida Morte, and Manel
J. Barbanoj
73
Eva V. Varga, Marc K. Rubenzik,
Dagmar Stropova, Masano Sugiyama,
Vanessa Grife, Victor J. Hruby, Kenner C.
Rice, William R. Roeske, and Henry 1.
Yamamura
109
Multidrug Resistance Protein MRP2 Contributes to BloodBrain Barrier Function and Restricts Antiepileptic Drug
Activity
Heidrun Potschka, Maren Fedrowitz, and
Wolfgang Loscher
124
Nocistatin and Prepro-Nociceptin/Orphanin FQ 160-187
Cause Nociception through Activation of GUo in CapsaicinSensitive 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
Makoto Inoue, Toshiko Kawashima,
Richard G. Allen, and Hiroshi Ueda
141
M. C. H. Ko, H. Lee, C. Harrison,
M. J. Clark, H. F. Song, N. N. Naughton, J.
H. Woods, and J. R. Traynor
179
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
Akihiro Noda, Hiroyuki Takamatsu,
Nobuya Matsuoka, Satosbi Koyama, Hideo
Tsukada, and Shintaro Nishimura
213
Inhibitors of Cyclooxygenase-2, but Not Cyclooxygenase-1
Provide Structural and Functional Protection against
Quinolinic Acid-Induced Neurodegeneration
Heather C. Salzberg-Brenhouse,
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
218
Evaluation of the Ocular Hypotensive Response of Serotonin 5HT,A and 5-HT2 Receptor Ligands in Conscious Ocular
Hypertensive Cynomolgus Monkeys
Jesse A. May, Marsha A. McLaughlin,
Najam A. Sharif, Mark R. Hellberg, and
Thomas R. Dean
301
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
G. J. Rodriguez, D. L. Roman, K. J. White,
D. E. Nichols, and E. L. Barker
338
Stefania Ruiu, Gerard A. Pinna,
Giorgio Marchese, Jean-Mario Mussinu,
Pierluigi Saba, Simone Tambaro,
Paola Casti, Romina Vargiu, and Luca Pani
363
Christophe Rousselle, Philippe Clair,
Maria Smirnova, Yuri Kolesnikov,
Gavril W. Pasternak, Stephanie Gac-Breton,
Anthony R. Rees, Jean-Michel Scherrmann,
and Jamal Temsamani
371
Kenneth J. Valenzano, Elfrida R. Grant,
Gang Wu, Mohamed Hachicha, Lori Schmid,
Laykea Tafesse, Qun Sun, Yakov Rotshteyn,
Joseph Francis, James Limbcris, Shiazah Malik,
Edward R. Whittemore, and Dianne Hodges
377
James D. Pomonis, James E. Harrison,
Lilly Mark, David R. Bristol,
Kenneth J. Valenzano, and Katharine Walker
387
Improved Brain Uptake and Pharmacological Activity of
Dalargin Using a Peptide-Vector-Mediated Strategy
Af-(4-Tertiarybutylphenyl)-4-(3-chloropyridin-2yl)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-2yl)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
Buprenorphine Blocks e- and jn-Opioid Receptor-Mediated
Antinociception in the Mouse
Hirokazu Mizoguchi, Amanda Spaulding,
Randy LeHermann, Hsiang-En Wu, Hiroshi
Nagase, and Leon F. Tseng
394
SSR591813, a Novel Selective and Partial « 4/32 Nicotinic
Receptor Agonist with Potential as an Aid to Smoking
Cessation
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
407
Grazyna Nowak
157
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
187
229
Kyoji Morita, Hideki Arimochi, and
Yoshinari Ohnishi
317
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 ProOxidant Action
ERRATUM
Correction to "Nitric Oxide-Donating Nonsteroidal AntiInflammatory Drugs Inhibit the Growth of Various Cultured
Human Cancer Cells: Evidence of a Tissue Type-Independent
Effect"
421