The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
Vol. 308, No. 1
January 2004
Contents
EDITORIAL
PERSPECTIVES IN PHARMACOLOGY
Pharmacological and Physiological Functions of the
Polyspecific Organic Cation Transporters: OCT1, 2, and 3
(SLC22A1-3)
Johan W. Jonker and Alfred H. Schinkel
ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION
Effect of Interferon-y on the Pharmacokinetics of Digoxin, a
Hiroko Kawaguchi, Yumi Matsui,
P-glycoprotein Substrate, Intravenously Injected into the
Yoshihiko Watanabe, and
Mouse
Yoshinobu Takakura
91
CYP3A4-Transfected Caco-2 Cells as a Tool for
Understanding Biochemical Absorption Barriers: Studies with
Sirolimus and Midazolam
Carolyn L. Cummins, Wolfgang Jacobsen,
Uwe Christians, and Leslie Z. Benet
143
Potent Mechanism-Based Inhibition of Human CYP2B6 by
Clopidogrel and Ticlopidine
Tanja Richter, Thomas E. Miirdter, Georg
Heinkele, Jiirgen Pleiss, Stephan Tatzel,
Matthias Schwab, Michel Eichelbaum, and
Ulrich M. Zanger
189
Ion-Trapping, Microsomal Binding, and Unbound Drug
Distribution in the Hepatic Retention of Basic Drugs
Sis Novel Nonsynonymous CYP1A2 Gene Polymorphisms:
Catalytic Activities of the Naturally Occurring Variant
Enzymes
Gerhard A. Siebert, Daniel Y. Hung,
Ping Chang, and Michael S. Roberts
228
Norie Murayama, Akiko Soyama, Yoshiro
Saito, Yukiko Nakajima, Kazuo Komamura,
Kazuyuki Ueno, Shiro Kamakura, Masafumi
Kitakaze, Hideo Kimura, Yu-ichi Goto,
Osamu Saitoh, Masaaki Katoh, Teiichi
Ohnuma, Mitsuru Kawai, Kenji Sugai,
Taisuke Ohtsuki, Chieko Suzuki, Narihiro
Minami, Shogo Ozawa, and Jun-ichi
Sawada
300
Lance R. McMahon, Stacy L. Sell, and
Charles P. France
111
Lawrence P. Carter, Huifang Wu, Weibin
Chen, Christopher M. Cruz, R. J. Lamb,
Wouter Koek, Andy Coop, and Charles P.
France
182
BEHAVIORAL PHARMACOLOGY
Cocaine and Other Indirect-Acting Monoamine Agonists
Differentially Attenuate a Naltrexone Discriminative Stimulus
in Morphine-Treated Rhesus Monkeys
Effects of y-Hydroxybutyrate (GHB) on Schedule-Controlled
Responding in Rats: Role of GHB and GABA B Receptors
Modification by Dopaminergic Drugs of Choice Behavior
under Concurrent Schedules of Intravenous Saline and Food
Delivery in Monkeys
Maciej Gasior, Carol A. Paronis, and
Jack Bergman
249
Antkociceptive Effects of Novel A2B Adenosine Receptor
Antagonists
Osama M. Abo-Salem, Alaa M. Hayallah,
Andras Bilkei-Gorzo, Barbara Filipek,
Andreas Zimmer. and Christa E. Miiller
358
CARDIOVASCULAR
Propafenone and Its Metabolites Preferentially Inhibit IKr in
Rabbit Ventricular Myocytes
Cardiovascular Effects of Nicotine, Chlorisondamine, and
Mecamylamine in the Pigeon
Synthetic High-Density I,ipoproteins Exert Cardioprotective
Effects in Myocardial Ischemia/Reperfusion Injury
Potent Antioxidant. Properties, t$ 4-Hydroxykpitopfanolol
Inhibition of G Protein-Coupled and ATP-Sensitive Potassium
Currents by 2-Methyl-3-(3,5-diiodo-4carboxymethoxybenzyl)benzofuran (KB130015), an
Amiodarone Derivative
Sean A. Cahill and Gil J. Gross
59
Kathryn K. Chadman and James H. Woods
73
Giuseppe Rossoni, Monica Gomaraschi,
Ferrucrio Berti, Cesare R. Sirlori, Guido
Franceschini, and Laura Calabresi
79
I. Tong Mak and William B. Weglicki
85
B. Brandts, R. Borchard, R. Macianskiene,
V. Gendviliene, D. Dirkmann,
M. Van Bracht, M. Prull, M. Meine,
I. Wickenbrock, K. Mubagwa, and
H.-J. Trappe
Vangetis Karalis, Aristides Dokouraetzidis,
and Panos Macheras
134
Effect of Graded Heart Rate Reduction with Ivabradine on
Myocardial Oxygen Consumption and Diastolic Time in
Exercising Dogs
Roles of Superoxide, Peroxynitrite, and Protein Kinase C in
the Development of Tolerance to Nitroglycerin
Patrice Colin, Bijan Ghaleh, Xavier Monnet,
Luc Hittinger, and Alain Berdeaux
236
G. Abou-Mohamed, J. A. Johnson, L. Jin,
A. B. El-Remessy, K. Do,
W. H. Kaesemeyer, R. B. Caldwell, and
R. W. Caldwell
289
Saxitoxin Blocks L-Type /Ca
Zhi Su, Michael Sheets, Hideyuki Ishida,
Fenghua Li, and William H. Barry
324
Increased Reactivity of Murine Mesenteric Veins to
Adrenergic Agonists: Functional Evidence Supporting
Increased a,-Adrenoceptor Reserve in Veins Compared with
Arteries
Alex A. Perez-Rivera, Gregory D. Fink, and
James J. Galligan
350
A Physiologically Based Approach for the Estimation of
Recirculatory Parameters
CELLULAR AND MOLECULAR
Cilostazol Enhances Casein Kinase 2 Phosphorylation and
Suppresses Tumor Necrosis Factor-a-Induced Increased
Phosphatase and Tensin Homolog Deleted from Chromosome
1* Phosphorylation and Apoptotic Cell Death in SK-N-SH
Cells
Role of Receptor Protein and Membrane Lipids in
Xanomeline Wash-Resistant Binding to Muscarinic M,
Receptors
Role of Multidrug Resistance Protein 2 (MRP2, ABCC2) in
Alkylating Agent Detoxification: MRP2 Potentiates
Glutathione S-Transferase Al-1-Mediated Resistance to
Chlorambucil Cytotoxicity
Ki Young Kim, Hwa Kyoung Shin,
Jeong Hyun Lee, Chi Dae Kim, Won
Suk Lee, Byung Yong Rhim, Yung
Woo Shin, and Ki Whan Hong
198
97
Jan Jakubfk,
Stanislav Tueek, and Esam E. El-Fakahany
105
Pamela K. Smitherman, Alan J. Townsend,
Timothy E. Kute, and Charles S. Morrow
260
Roles of Catalase and Hydrogen Peroxide in Green Tea
Polyphenol-Induced Chemopreventive Effects
Tetsuya Yamamoto, Jill Lewis, John Wataha,
Douglas Dickinson, Baidev Singh,
Wendy B. Bollag, Eisaku Ueta, Tokio Osaki,
Mohammad Athar, George Schuster, and
Stephen Hsu
317
Muscarinic Agonist-Mediated Heterologous Desensitization in
Isolated Ileum Requires Activation of Both Muscarinic M 2 and
M3 Receptors
Michael T. Griffin, Minoru Matsui,
Darakhshanda Shehnaz, Khurram Z. Ansari,
Makoto M. Taketo, Toshiya Manabe, and
Frederick J. Ehlert
339
Takanori Akagi, Kazami Ushinohama,
Shoko Ikesue, Eiji Yukawa, Shun Higuchi,
Kenji Hamase, Kiyoshi Zaitsu, and
Shigehiro Ohdo
378
CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY
Chronopharmacology of Melatonin in Mice to Maximize the
Antitumor Effect and Minimize the Rhythm Disturbance
Effect
ENDOCRINE AND REPRODUCTIVE
Ovarian Steroid Hormone Modulation of the Acute Effects of
Cocaine on Luteinizing Hormone and Prolactin Levels in
Ovariectomized Rhesus Monkeys
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL
Hyperosmolar Solution Effects in Guinea Pig Airways. I.
Mechanical Responses to Relative Changes in Osmolarity
Nancy K. Mello, Jack H. Mendelson, S.
Stevens Negus, and Maureen Kelly
156
Jeffrey S. Fedan, Janet A. Dowdy,
Richard A. Johnston, and
Michael R. Van Scott
10
Hyperosmolar Solution Effects in Guinea Pig Airways. II.
Epithelial Bioelectric Responses to Relative Changes in
Osmolarity
Hyperosmolar Solution Effects in Guinea Pig Airways. III.
Studies on the Identity of Epithelium-Derived Relaxing Factor
in Isolated Perfused Trachea Using Pharmacological Agents
David X.-Y. Wu, Richard A. Johnston,
Appavoo Rengasamy, Michael R. Van Scott,
and Jeffrey S. Fedan
19
Jeffrey S. Fedan, Janet A. Dowdy,
Michael R. Van Scott, David X.-Y. Wu, and
Richard A. Johnston
30
Hyperosmolar Solution Effects in Guinea Pig Airways. IV.
Lipopolysaecharide-Induced Alterations in Airway Reactivity
and Epithelial Bioelectric Responses to Methacholine and
Hyperosmolarity
Richard A. Johnston, Michael R. Van Scott,
Choudari Kommineni, Lyndell L. Millecchia,
Juanita Dortch-Carnes, and Jeffrey S. Fedan
37
Signal Transduction Underlying Carbachol-Induced
Contraction of Rat Urinary Bladder. I. Phospholipases and
Ca2+ Sources
Tim Schneider, Peter Hein, and
Martin C. Michel
47
Signal Transduction Underlying Carbachol-Induced
Contraction of Rat Urinary Bladder. II. Protein Kinases
Marina Fleichman, Tim Schneider,
Charlotte Fetscher, and Martin C. Michel
54
Nicotine Promoted Colon Cancer Growth via Epidermal
Growth Factor Receptor, c-Src, and 5-Lipoxygenase-Mediated
Signal Pathway
Yi N. Ye, Edgar S. L. Liu, Vivian Y. Shin,
William K. K. Wu, Jiing C. Luo, and Chi
H. Cho
66
Antitumor Kffect of a Splenic Injection of 5-Fluorouracil on
Metastatic Liver Cancer in Mice
Kenichi Kanoh, Tatsuo Shimura,
Hideki Suzuki, Kenichi Nomoto,
Takayuki Asao, and Hiroyuki Kuwano
168
Oral Treatment with Recombinant Human Interleukin-11
Improves Mucosal Transport in the Colon of Human
Leukocyte Antigen-B27 Transgenic Rats
Kalina Venkova, James C. Keith, Jr., and
Beverley Greenwood-Van Meerveld
206
The Inhibitory Effect of Adrenomedullin in the Rat Ileum:
Cross-Talk with /33-Adrenoceptor in the Serotonin-Induced
Muscle Contraction
Gennadi M. Kravtsov, Isabel S. S. Hwang,
and Fai Tang
241
Interaction of Cyclooxygenase Isoenzymes, Nitric Oxide, and
Afferent Neurons in Gastric Mucosal Defense in Rats
Karlheinz Ehrlich, Christa Sicking,
Michael Respondek, and Brigitta M. Peskar
277
Characterization of Specific Opioid Binding Sites in Neural
Membranes from the Myenteric Plexus of Porcine Small
Intestine
DeWayne Townsend IV, Philip S. Portoghese,
and David R. Brown
385
Melvyn Lynn, Y. Nancy Wong,
Janice L.Wheeler, Richard J. Kao,
Carlos A. Perdomo, Robert Noveck,
Ramon Vargas, Tony D'Angelo,
Sandra Golzkowsky, F. Gilbert McMahon,
Kishor M. Wasan, and Daniel P. Rossignoi
175
Identification of a Potent and Selective Noncovalent Cathepsin
S Inhibitor
Robin L. Thurmond, Siquan Sun,
Clark A. Sehon, Sherry M. Baker, Hui Cai,
Yin Gu, Wen Jiang, Jason P. Riley, Kacy N.
Williams, James P. Edwards, and Lars
Karlsson
268
Evidence That Glutathione Depletion Is a Mechanism
Responsible for the Anti-Inflammatory Effects of Ethyl
Pyruvate in Cultured Lipopolysaccharide-Stimulated RAW
264.7 Cells
Mingchen Song, John A. Kellum,
Hoda Kaldas, and Mitchell P. Fink
307
Feng Wang, Nobuya Matsuoka,
Seitaro Mutoh, and Shuji Kaneko
120
INFL'AMMATION AND IMMUNOPHARMACOLOGY
Extended in Vivo Pharmacodynamic Activity of E5564 (a-DGlucopyranose) in Normal Volunteers with Experimental
Endotoxemia
NEUROPHARMACOLOGY
Modulation of Ca2+ Channel Currents by a Novel Antidementia
Drug /V-(4-Acetyl-l-piperazinyl)-p-fluorobenzamide
Monohydrate (FK960) in Rat Hippocampal Neurons
Effects of 2-[AK4-Chlorophenyl)-iV-methylamino]-4/Jpyrido[3.2-<?]-l,3-thiazin-4-one (YM928), an Orally Active otAmino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
Receptor Antagonist, in Models of Generalized Epileptic
Seizure in Mice and Rats
Hiroshi Yamashita, Kazushige Ohno, Yoko
Amada, Hanae Hattori, Yukiko OzawaFunatsu, Takashi Toya, Hiroshi Inami, JunIchi Shishikura, Shuichi Sakamoto,
Masamichi Okada, and Tokio Yamaguchi
An Electrophysiological Model of Spinal Transmission Deficits
in Mouse Experimental Autoimmune Encephalomyelitis
Susan E. Hanak, Erin M. Reilly,
Jill Wotanis, Bin Zhu, Claudine Pulicicchio,
Kathleen McMonagle-Strucko,
Joseph G. Wettstein, and Mark D. Black
127
214
Timothy A. Vortherrns and Val J. Watts
Sensitization of Neuronal A2A Adenosine Receptors after
Persistent D2 Dopamine Receptor Activation
Central Mechanisms Regulating Penile Erection in Conscious
Rats: The Dopaminergic Systems Related to the Proerectile
Effect of Apomorphine
Nicotinic Receptor Modulation of Dopamine Transporter
Function in Rat Striatum and Medial Prefrontal Cortex
TOXICOLOGY
Suppression of Cytochrome P450 2E1 Promoter Activity by
Interferon-y and Loss of Response Due to the —71G>T
Nucleotide Polymorphism of the CYP2E1*7B Allele
In Vitro Discrimination of Fluoroquinolones Toxicity on
Tendon Cells: Involvement of Oxidative Stress
221
Gin C. Hsieh, Peter R. Hollingsworth,
Brenda Martino, Renjie Chang, Marc A.
Terranova, Alyssa B. O'Neill, James J.
Lynch, Robert B. Moreland, Diana L.
Donnelly-Roberts, Teodozyi Kolasa, Joseph
P. Mikusa, Jill M. McVey, Kennan C.
Marsh, James P. Sullivan, and Jorge D.
Brioni
Lisa S. Middleton, Wayne A. Cass, and
Linda P. Dwoskin
330
367
Ling O. Qiu, Mark W. Linder,
Deborah M. Antonino-Green, and
Roland Valdes, Jr.
284
F. Pouzaud, K. Bernard-Beau bois,
M. Thevenin, J.-M. Warnet, G. Hayem, and
P. Rat
394