The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
November 2003
Vol. 307, No. 2
Contents
PERSPECTIVES IN PHARMACOLOGY
Protease-Activated Receptors: New Concepts in Regulation of
G Protein-Coupled Receptor Signaling and Trafficking
JoAnn Trejo
ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION
Developmental Expression of the Major Human Hepatic
CYP3A Enzymes
Altered Diurnal Rhythm of Intestinal Peptide Transporter by
Fasting and Its Effects on the Pharmacokinetics of Ceftibuten
Cellular Uptake and Efflux of the Tea Flavonoid (-)Epicatechin-3-gallate in the Human Intestinal Cell Line Caco2
Evaluation of the Blood-Brain Barrier Transport, Population
Pharmacokinetics, and Brain Distribution of Benztropine
Analogs and Cocaine Using in Vitro and in Vivo Techniques
Interaction of Imatinib Mesilate with Human P-Glycoprotein
Jeffrey C. Stevens, Ronald
N. Hines, " Chungang Gu,
Sevasti B. Koukouritaki,
Jason R. Manro, Peler J. Tandler, and
Matthew J. Zaya
Xiaoyue Pan, Tomohiro Terada,
Masahiro Okuda, and Ken-Ichi Inui
Jaya Bharathi Vaidyanathan and
Thomas Walle
Sangceta Raje, Jianjing Cao,
Amy Hauck Newman, Huanling Gao, and
Natalie D. Eddingtoo
Akinobu Hamada, Hideto Miyano,
Hiroshi Watanabe, and Hideyuki Saito
BEHAVIORAL PHARMACOLOGY
An Assessment of the Effects of Serotonin 6 (5-HT6) Receptor
Antagonists in Rodent Models of Learning
The Competitive iV-Methyl-D-aspartate Receptor Antagonist
(—)-6-Phosphonomethyl-deca-hydroisoquinoline-3-carboxylic
Acid (LY235959) Potentiates the Antinociceptive Effects of
Opioids That Vary in Efficacy at the /t-Opioid Receptor
CARDIOVASCULAR
Semicarbazide-Sensitive Amine Oxidase Substrates Potentiate
Hydralazine Hypotension: Possible Role of Hydrogen Peroxide
Hypothalamic Leptin Receptor and Signaling Molecule
Expressions in Cafeteria Diet-Fed Rats
A Subset of Highly Effective Propafenone-Type Multidrug
Resistance Modulators Lacks Effects on Cardiac Action
Potential and Mechanical Twitch Parameters of Rat Papillary
Muscles
Protective Effect of Amiodarone but Not NDesethylamiodarone on Postischemic Hearts through the
Inhibition of Mitochondrial Permeability Transition
The Aminotetraline Derivative (±)-(i?,1S)-5,6-Dihydroxy-2methylamino-1,2,3,4-tetrahydro-naphthalene Hydrochloride
(CHF-1024) Displays Cardioprotection in Postischemic
Ventricular Dysfunction of the Rat Heart
Mark D. Lindner, Donald B. Hodges Jr.,
John B. Hogan, Anitra F. Orie,
Jason A. Corsa, Donna M. Barten,
Craig Poison, Barbara J. Robertson,
Valerie L. Guss, Kevin W. Gillman,
John E. Starrett Jr., and Valentin K. Gribkoff
Richard M. Allen, Arthur L. Granger, and
Linda A. Dykstra
437
573
626
745
801
824
682
785
Horacio Vidrio, Martha Medina,
Pilar Gonzalez-Romo,
Marte Lorenzana-Jimenez,
Patricia Diaz-Arista, and Alejandro Baeza
Charles Plut, Catherine Ribiere,
Yves GJudicelli, and Jean-Pierre Dausse
497
Diethart Schmid, Dawid L. Staudacher,
Hans G. Loew, Paui G. Spieckermann,
Gerhard F. Ecker, Stephan Kopp, and
Peter Chiba
589
Gabor Varbiro, Ambrus Toth, Antal Tapodi,
Zita Bognar, Balazs Veres, Baiazs Sumegi,
and Ferenc Gallyas, Jr.
Giuseppe Rossoni, Barbara Manfredi,
Viviana Cavalca, Roberta Razzetti, Stefano
Bongrani, Gian Luca Polvani, and Ferruccio
Berti
615
544
633
Up-Regulation of Endothelial Nitric-Oxide Synthase by
Endothelium-Derived Hyperpolarizing Factor Involves
Mitogen-Activated Protein Kinase and Protein Kinase C
Signaling Pathways
Hong Wang, Li Lin, Jiangang Jiang,
Yan Wang, Zai Ying Lu, J. Alycc Bradbury,
Fred Bj0rn Lih, Dao Wen Wang, and Darryl
C. Zeldin
753
Electrophysiological Safety of Sertindole in Dogs with Normal
and Remodeled Hearts
Morten B. Thomsen, Paul G. A. Volders,
Milan Stengl, Roel L. H. M. G. Spiitjens, Jet
D. M. Beekman, Ulrike Bischoff, Morten A.
Kail, Kristen Frederiksen, J0rgen Matz, and
Marc A. Vos
776
Katherine G. Moss, Guy C. Toner,
Julie M. Cherrington, Dirk B. Mendel, and
A. Douglas Laird
476
Blockade of G Protein-Coupled Receptors and the Dopamine
Transporter by a Transmembrane Domain Peptide: Novel
Strategy for Functional Inhibition of Membrane Proteins in
Vivo
Susan R. George, Gordon Y. K. Ng,
Samuel P. Lee, Theresa Fan, George
Varghese, Chen Wang, Charles M. Dcber,
Philip Seeman, and Brian F. O'Dowd
481
Eun Joung Kim, Ki Sook Park,
Soo Youn Chung, Yhun Yhong Sheen,
Dong Chuol Moon, Yeun Sook Song,
Kyong Soon Kim, Sukgi] Song,
Yeo Pyo Yun, Myung Koo Lee, Ki Wan Oh,
Do Young Yoon, and Jin Tae Hong
505
Peroxisome Proliferator-Activated Receptor-y Activator 15Deoxy-A12')4-Prostaglandin J2 Inhibits Neuroblastoma Cell
Growth through Induction of Apoptosis: Association with
Extracellular Signal-Regulated Kinase Signal Pathway
Petrus J, Pauwels and Francis C. Colpaert
608
Robert E. Carraway, Xianyong Gui, and
David E. Cochrane
640
Tim D. Werry, Graeme F. Wilkinson, and
Gary B. Wiliars
661
Erding Hu, Edward Dul, Chiu-Mei Sung,
Zunxuan Chen, Robert Kirkpatriek,
Gui-Feng Zhang, Kyung Johanson.
Ronggang Liu, Amparo Lago,
Glenn Hofmann, Ricardo Macarron,
Maite de los Frailes, Paloma Perez,
John Krawiee, James Winkler, and
Michael Jaye
720
Limen Chi and Maarten E. A. Reith
729
Isabelle Passagne, Alexandra Evrard,
Jean-Yves Winum, Philippe Dcpeille,
Pierre Cuq. Jean-Louis Montero,
Didler Cupissol, and Laurence Vian
816
Tom Stover and Mark Kcster
468
Christian Thorkildsen, S0ren Neve,
Bjarne Due Larsen, Eddi Meier, and
J0rgen Ssberg Petersen
490
Xiaonan Han, Takashi Uchiyama,
Penny L. Sappington, Arino Yaguchi,
Runkuan Yang, Mitchell P. Fink, and
Russell L. Delude
443
CELLULAR AND MOLECULAR
Hair Depigmentation Is a Biological Readout for
Pharmacological Inhibition of KIT in Mice and Humans
Ca2+ Responses in Chinese Hamster Ovary-Kl Cells
Demonstrate an Atypical Pattern of Ligand-Induced 5-HT1A
Receptor Activation
Ca2+ Channel Blockers Enhance Neurotensin (NT) Binding
and Inhibit NT-Induced Inositol Phosphate Formation in
Prostate Cancer PC3 Cells
Cross Talk between P2Y2 Nucleotide Receptors and CXC
Chemokine Receptor 2 Resulting in Enhanced Ca 2+ Signaling
Involves Enhancement of Phospholipase C Activity and Is
Enabled by Incremental Ca2+ Release in Human Embryonic
Kidney Cells
Identification of Novel Isoform-Selective Inhibitors within
Class I Histone Deacetvlases
Substrate-Induced Trafficking of the Dopamine Transporter
in Heterologously Expressing Cells and in Rat Striatal
Synaptosomal Preparations
Cytotoxicity, DNA Damage, and Apoptosis Induced by New
Fotemustine Analogs on Human Melanoma Cells in Relation
to 06-Methylguanine DNA-Methyltransferase Expression
CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY
Liposomal Delivery Enhances Short-Chain Ceramide-Induced
Apoptosis of Breast Cancer Cells
ENDOCRINE AND REPRODUCTIVE
Glucagon-Like Peptide 1 Receptor Agonist ZP10A Increases
Insulin mRNA Expression and Prevents Diabetic Progression
in db/db Mice
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL
NAD+ Ameliorates Inflammation-Induced Epithelial Barrier
Dysfunction in Cultured Enterocytes and Mouse Heal Mucosa
Ncurotransmitters Mediating the Intestinal Peristaltic Reflex
in the Mouse
Importance of Amino Acids of the Central Portion of the
Second Intracellular Loop of the Gastrin-Releasing Peptide
Receptor for Phospholipase C Activation, Internalization, and
Chronic Down-Regulation
John R. Grider
460
Michael Schumann, Tomoo Nakagawa,
Samuel A. Mantey, Kenji Tokita, David J.
Verizon, Simon J. Hocart, Richard V.
Benya, and Robert T. Jensen
597
Non-Ulcerogenic Dose of Dexamethasone Delays Gastric Ulcer
Healing in Rats
Jiing C. Luo, Vivian Y. Shin,
Edgar S. L. Liu, Wallace H. L. So,
Yi N. Ye, Full Y. Chang, and Chi H. Cho
692
Cyclooxygenase Isozymes Involved in Adaptive Functional
Responses in Rat Stomach after Barrier Disruption
Masanori Takeeda, Masanori Yamato,
Shinichi Kalo, and Koji Takeuchi
713
INFLAMMATION AND IMMUNOPHARMACOLOGY
Chemoattractant Receptor-Homologous Molecule Expressed on
Th2 Cells Activation in Vivo Increases Blood Leukocyte
Counts and Its Blockade Abrogates 13,14-Dihydro-15-ketoprostaglandin D2-Induced Eosinophilia in Rats
Michitaka Shichijo, Hiromi Sugimoto,
Koichi Nagao, Hisayo In be,
Jeffrey A. Encinas, Keisuke Takeshita,
Kevin B. Bacon, and Florian Gantner
518
Mitsuteru Ishiwara, Yasuo Aoki,
Hidetsugu Takagaki, Michio Ui, and
Fumikazu Okajima
583
Chanlal Beumer, Marty Wulferink,
Willem Raaben, Danielle Fiechter,
Ruud Brands, and Willem Seinen
737
Norma C. Alonzo and Barbara M. Bayer
793
Eric Backes and Scott E. Hemby
450
Characterization of Spontaneous and Precipitated Nicotine
Withdrawal in the Mouse
M. I. Damaj, W. Kao, and B. R. Martin
526
Acetylcholinesterase Inhibitors Activate Septohippocampal
GABAergic Neurons via Muscarinic but Not Nkotinic
Receptors
Min Wu, Samuel S. Newton,
Joshua B. Atkins, Changqing Xu, Ronald S.
Duman, and Meenakshi Alreja
535
Adam W. Hendricson, Mark P. Thomas,
Mclanie J. Lippmann, and
Richard A. Morrisett
550
D. A. Drakulich, A. M. Walls, M. L. Toews,
and T. D. Hexum
559
Ethanol Withdrawal Reduces the Number of Spontaneously
Active Ventral Tegmental Area Dopamine Neurons in
Conscious Animals
Roh-Yu Shen
566
Effect of (i-Amyloid Peptide 1-42 on the Cytoprotective Action
Mediated by oH Nicotinic Acetylcholine Receptors in Growth
Factor-Deprived Differentiated PC-12 Cells
Xinyu D. Li and Jerry J. Buccafusco
670
Up-Regulation of Spinal Muscarinic Receptors and Increased
Antinociceptive Effect of Intrathccal Muscarine in Diabetic
Rats
Antinociceptive Synergy, Additivity, and Subadditivity with
Combinations of Oral Glucosamine Plus Nonopioid Analgesics
in Mice
Shao-Rui Chen and Hui-Lin Pan
676
TA-270 [4-Hydroxy-l-methyl-3-octyloxy-7-sinapinoylamino2(l/f)-quinolinone], an Anti-Asthmatic Agent, Inhibits
Leukotriene Production Induced by IgE Receptor Stimulation
in RBL-2H3 Cells
Calf Intestinal Alkaline Phosphatase, a Novel Therapeutic
Drug for Lipopolysaccharide (LPS)-Mediated Diseases,
Attenuates LPS Toxicity in Mice and Piglets
Antagonism of iV-Methyl-D-aspartate Receptors Reduces the
Vulnerability of the Immune System to Stress after Chronic
Morphine
NKUROPHARMACOLOGY
Discrete Cell Gene Profiling of Ventral Tegmental Dopamine
Neurons after Acute and Chronic Cocaine Self-Administration
Suppression of L-Type Voltage-Gated Calcium ChannelDependent Synaptic Plasticity by Ethanol: Analysis of
Miniature Synaptic Currents and Dendritic Calcium
Transients
Neuropeptide Y Receptor-Mediated Sensitization of ATP•Stimulated Inositol Phosphate Formation
Protein Kinase C-Dependent Potentiation of Intracellular
Calcium Influx by tr1 Receptor Agonists in Rat Hippocampal
Neurons
Mechanism-Based Modeling of the Pharmacodynamic
Interaction of Alphaxalone and Midazolam in Rats
ATP Modulates Noradrenaline Release by Activation of
Inhibitory P2Y Receptors and Facilitatory P2X Receptors in
the Rat Vas Deferens
699
Ronald J. Tallarida, Alan Cowan, and
Robert B. Raff a
F. P. Monnet, M. P. Morin-Surun, J. Leger, and L.
Combeltes
708
S. A. G. Visser, D. R. H. Huntjcns, P. H. van der
Graaf, L. A. Peletier, and M. Danhof
765
Gloria Queiroz, Carlos Talaia, and
Jorge Goncalves
TOXICOLOGY
Repeated Exposures to Heroin and/or Cadmium Alter the
Rate of Formation of Morphine Giucuronides in the Rat
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"
Letizia Antonilli, Carmen Suriano,
Giovanna Paolone, Aldo Badiani, and
Paolo Nencini
651
829