The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
December 2004
Vol.311, No. 2
Contents
ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION
The Functional Role of Threonine-205 in the Mechanism-Based
Inactivation of P450 2B1 by Two Ethynyl Substrates: The
Importance of the F Helix in Catalysis
Physiological Capacity of the Reticuloendothelial System for
the Degradation of Hemoglobin Vesicles (Artificial Oxygen
Carriers) after Massive Intravenous Doses by Daily Repeated
Infusions for 14 Days
Mechanism-Based Inactivation of Human Cytochrome
P4502C8 by Drugs in Vitro
A'-Glucuronidation of Carbamazepine in Human Tissues Is
Mediated by UGT2B7
Population Pharmacokinetic Modeling of Blood-Brain Barrier
Transport of Synthetic Adenosine A1 Receptor Agonists
Involvement of Multiple Transporters in the Efflux of 3Hydroxy-3-methyIglutaryl-CoA Reductase Inhibitors across the
Blood-Brain Barrier
NADH Cytochrome b5 Reductase and Cytochrome bs Catalyze
the Microsomal Reduction of Xenobiotic Hydroxylamines and
Amidoximes in Humans
Haplotype-Oriented Genetic Analysis and Functional
Assessment of Promoter Variants in the MDRl (ABCBl) Gene
Hepatobiliary Disposition of the Metabolically Stable Opioid
Peptide [D-Pen3,D-Pen5]-Enkephalin (DPDPE): Pharmacokinetic
Consequences of the Interplay between Multiple Transport
Systems
BEHAVIORAL PHARMACOLOGY
Effects of Dopamine D, Ligands on Eye Blinking in Monkeys:
Efficacy, Antagonism, and D1/D2 Interactions
Opioid Receptor Involvement in Food Deprivation-Induced
Feeding: Evaluation of Selective Antagonist and Antisense
Oligodeoxynucleotide Probe Effects in Mice and Rats
Hsia-Lien Lin, Ute M. Kent,
Haoming Zhang, Lucy Waskell, and
Paul F. Hollenberg
Hiromi Sakai, Yohei Masada,
Hirohisa Horinouchi, Eiji Ikeda, Keitaro Sou,
Shinji Takeoka, Makoto Suematsu, Masuhiko
Takaori, Koichi Kobayashi, and Eishun
Tsuchida
855
Thomas M. Polasek, David J. Elliot,
Benjamin C. Lewis, and John O. Miners
996
874
Adam G. Staines, Michael W. H. Coughtrie,
and Brian Burchell
1131
M. P. Schaddelee, D. Groenendaal,
J. DeJongh, C. G. J. Cleypool,
A. P. Uzerman, A. G. De Boer, and
M. Danhof
1138
Ryota Kikuchi, Hiroyuki Kusuhara,
Takaaki Abe, Hitoshi Endou, and
Yuichi Sugiyama
1147
Joseph R. Kurian, Sunil U. Bajad,
Jackie L. Miller, Nathaniel A. Chin, and
Lauren A. Trepanier
1171
Hiroshi Takane, Daisuke Kobayashi,
Takeshi Hirota, Junzo Kigawa,
Naoki Terakawa, Kenji Otsubo, and
Ichiro leiri
1179
Keith A. Hoffmaster,
Maciej J. Zamek-Gliszczynski,
Gary M. Pollack, and Kim L. R. Brouwer
1203
Emily M. Jutkiewicz and Jack Bergman
1008
M. M. Hadjimarkou, A. Sin,
Y. Israel, Y.-X. Pan, G. C. J
G. W. Pasternak, and R. J. Bodna
1188
CARDIOVASCULAR
Anti-Inflammatory Effects of ATI Receptor Blockade Provide
End-Organ Protection in Stroke-Prone Rats Independently
from Blood Pressure Fall
Luigi Sironi, Paolo Gelosa, Uliano Guerrini,
Cristina Banfi, Veronica Crippa,
Maura Brioschi, Elisabetta Gianazza,
Elena Nobili, Anita Gianella,
Marc dc Gasparo, and Elena Tremoli
989
Volatile Anesthetics Inhibit Calcitonin Gene-Related Peptide
Receptor-Mediated Responses in Pithed Rats and Human
Neuroblastoma Cells
Apolipoprotein A-IMilail<> and 1-PaImitoyl-2-oleoyl
Phosphatidylcholine Complex (ETC-216) Protects the in Vivo
Rabbit Heart from Regional Ischemia-Reperfusion Injury
Masataka Kuroda, Daisuke Yoshikawa,
Koichi Nishikawa, Shigeru Saito, and
Fumio Goto
1016
Marta Marches!, Erin A. Booth,
Treasa Davis, Charles L. Bisgaier, and
Benedict R. Lucchesi
1023
Cytoprotective Effect of Sodium Orthovanadate on Ischemia/
Reperfusion-Induced Injury in the Rat Heart Involves Akt
Activation and Inhibition of Fodrin Breakdown and Apoptosis
Yoko Takada, Masami Hashimoto,
Jiro Kasahara, Kazuyuki Aihara, and
Kohji Fukunaga
1249
CELLULAR AND MOLECULAR
Selective Nonsteroidal Anti-Inflammatory Drugs Induce
Thymosin /3-4 and Alter Actin Cytoskeletal Organization in
Human Colorectal Cancer Cells
Anshu K. Jain, Scott M. Moore,
Kiyoshi Yamaguchi, Thomas E. Eling, and
Seung Joon Baek
885
Transfection and Functional Expression of CYP4A1 and
CYP4A2 Using Bicistronic Vectors in Vascular Cells and
Tissues
Ji-Shi Wang, Fan Zhang, Miao Jiang,
Mong-Heng Wang, Barbara A. Zand, Nader
G. Abraham, Alberto Nasjlctti, and Michal
Laniado-Schwartzman
913
Rotenone Induces Apoptosis via Activation of Bad in Human
Dopaminergic SH-SY5Y Cells
Induction of Novel Agonist Selectivity for the ADP-Activated
P2Y, Receptor Versus the ADP-Activated P2Y12 and P2Y13
Receptors by Conformational Constraint of an ADP Analog
Masahiko Watabe and Toshio Nakaki
948
Mariya Chhatriwala, R. Gnana Ravi,
Roshni I. Patel, Jose L. Boyer,
Kenneth A. Jacobson, and T.
Kendall Harden
1038
Inhibition of Tumor Cell Proliferation by <r Ligands Is
Associated with K+ Channel Inhibition and p27 kipl
Accumulation
Coexpression of Yv Y2, and Y4 Receptors in Smooth Muscle
Coupled to Distinct Signaling Pathways
The Effect of the /32-Adrenoceptor Agonist Prodrug BRL47672 on Cardiovascular Function, Skeletal Muscle Myosin
Heavy Chain, and MyoD Expression in the Rat
Adrien Renaudo, Vanina Watry,
Anne-Amandine Chassot, Gilles Ponzio.
Jordi Ehrenleld, and Olivier Soriani
1105
Sudhakar Misra, Karnam S. Murthy,
Huiping Zhou, and John R. Grider
1154
S. W. Jones, D. J. Baker, S. M. Gardiner,
T. Bennett, J. A. TJmmons, and P.
L. Greenhaff
1225
Inhibition of Activator Protein 1 by Barbiturates Is Mediated
by Differential Effects on Mitogen-Activated Protein Kinases
and the Small G Proteins Ras and Rac-1
Matjaz Humar, Nikolaos Andriopoulos,
Soeren E. Pischke, Torsten Loop,
Rene Schmidt, Alexander Hoetzel,
Martin Roesslein, Heike L. Pahl,
Klaus K. Geiger, and Benedikt H. J. Pannen
1232
CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY
Epigenomic Changes during Leukemia Cell Differentiation:
Analysis of Histone Acetylation and Cytosine Methylation
Using CpG Island Microarrays
M. Nouzova, N. Holtan, M M. Oshiro,
R. B. Isett, J. L. Munoz-Rodriguez,
A. F. List, M. L. Narro, S. J. Miller,
N. C. Merchant, and B. W. Futscher
968
Involvement of Kstrone-3-Sulfate Transporters in Proliferation
of Hormone-Dependent Breast Cancer Cells
Takashi Nozawa, Masato Suzuki,
Koichi Takaliashi, Hikaru Yabuuchi,
Tomoji Maeda, Akira Tsuji, and
Ikumi Tamai
1032
Relationship between Antiapoptotic Molecules and Metastatic
Potency and the Involvement of DNA-Dependent Protein
Kinase in the Chemosensitization of Metastatic Human
Cancer Cells by Epidermal Growth Factor Receptor Blockade
Jee Hyun Um, Joong Keun Kwon,
Chi-Dug Kang, Mi Ju Kim, Dong Sik Ju,
Jae Ho Bae, Dong Wan Kim,
Byung Seon Chung, and Sun Hee Kim
Stephanie L. Matheson, James P. McNamee,
Taiqui Wang, Moulay A. Alaoui-Jamali, Ana
M. Tari, and Bertrand J. Jean-Claude
1062
The Com bi-Targeting Concept: Dissection of the Binary
Mechanism of Action of the Combi-Triazene SMA41 in Vitro
and Antitumor Activity in Vivo
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL
Contribution of Angiotensin II to Alcohol-Induced Pancreatic
Fibrosis in Rats
Takehiko Uesugi, Matthias Froh,
Erwin Gabele, Fuyumi Isayama,
Blair U. Bradford, Iwao Ikai,
Yoshio Yamaoka, and Gavin E. Arteel
1163
921
Evaluation of Second Generation Amiloride Analogs as
Therapy for Cystic Fibrosis Lung Disease
Gene Therapy with Adenoviral Plasmids or Naked DNA of
Vascular Endothelial Growth Factor and Platelet-Derived
Growth Factor Accelerates Healing of Duodenal Ulcer in Rats
Increased Expression of the Sodium Transporter BSC-1 in
Spontaneously Hypertensive Rats
Genetic Variants of the Human H +/Dipeptide Transporter
PEPT2: Analysis of Haplotype Functions
Andrew J. Hirsh, Juan R. Sabater,
Andra Zamurs, Rick T. Smith,
Anthony M. Paradiso, Sam Hopkins,
William M. Abraham, and Richard
C. Boucher
Xiaoming Deng, Sandor Szabo,
Tetyana Khomenko, Martin R. Jadus, and
Masashi Yoshida
929
982
Prajakta A. Sonalkcr, Stevan P. Tofovic, and
Edwin K. Jackson
1052
Julia Pinsonneault, Carslen Uhd Nielsen, and
Wolfgang Sadee
1088
P2X Receptor-Stimulated Calcium Responses in
Preglomerular Vascular Smooth Muscle Cells Involves 20Hydroxyeicosatetraenoic Acid
Xueying Zhao, John R. Falck, V. Raj Gopal,
Edward W. Inscho, and John D. Imig
121 I
Nitric Oxide (NO)-Releasing Naproxen (HCT-3012 [(S)-6Methoxy-tt-methyl-2-naphthaleneacetic Acid 4-(Nitrooxy)butyl
Ester]) Interactions with Aspirin in Gastric Mucosa of
Arthritic Rats Reveal a Role for Aspirin-Triggered Lipoxin,
Prostaglandins, and NO in Gastric Protection
Stefano Fiorucci, Annarita Di Lorenzo,
Barbara Renga, Silvana Farneti, Antonio
Morelli, and Giuseppe Cirino
1264
INFLAMMATION AND IMMUNOPHARMACOLOGY
ABT-963 [2-(3,4-Difluoro-phenyl)-4-(3-hydroxy-3-methylbutoxy)-5-(4-methaiiesulfonyl-phenyl)-2//-pyridazin--3-one], A
Highly Potent and Selective Disubstituted Pyridazinone
Cyclooxygenase-2 Inhibitor
A Novel Nonpeptide Antagonist of the Kinin B, Receptor:
Effects at the Rabbit Receptor
Richard R. Harris, Lawrence Black,
Sekhar Surapaneni, Teodozyj Kolasa,
Sandra Majest. Marian T. Namovic,
George Grayson, Victoria Komater,
Denise Wilcox, Linda King, Kennan Marsh,
Michael F. Jarvis, Merrill Nuss,
Hugh.Nellans, Lee Pruesser,
Glenn A. Reinhart, Bryan Cox,
Peer Jacobson, Andrew Stewart,
Michael Coghlan, George Carter, and
Randy L. Bell
904
Guillaume Morissettc, Jean-Philippe Fortin,
Sophie Otis, Johanne Bouthillier, and
Francois Marceau
Koh-ichi Yuhki, Akinori Ueno,
Hiroaki Naraba, Fumiaki Kojima,
Fumitaka Ushikubi, Shuh Narumiya, and
Sachiko Oh-ishi
1121
Inhibition of Poly(ADP-Ribose) Polymerase Prevents AllergenInduced Asthma-Like Reaction in Sensitized Guinea Pigs
Ylenia Suzuki, Emanuela Masini,
Cosimo Mazzocca, Salvatore Cuzzocrea,
Anna Ciampa, Hisanori Suzuki, and
Daniele Bani
1241
Comparative Study of Glucocorticoids, Cyclosporine A, and
JTE-607 l(-)-Ethyl-A'-{3,5-dichloro-2-hydroxy-4-[2-(4methylpiperazin-1 -yl)ethoxy]benzoyl }-L-phcnylalaninate
Dihydrochloride] in a Mouse Septic Shock Model
Hiroyuki Iwamura, Motohide Sato, and
Korekiyo Wakitani
1256
Erythropoietin Reduces the Development of Experimental
Inflammatory Bowel Disease
Salvatore Cuzzocrea. Emanuela Mazzon,
Rosanna Di Paola, Nimesh S. A. Patel,
Tiziana Genovese, Carmelo Muia,
Angelina De Sarro, and Christoph Thiemcrmann
1272
Prostaglandin Receptors EP2, EP3, and IP Mediate Exudate
Formation in Carrageenin-Induced Mouse Pleurisy
NEUROPHARMACOLOGY
Differential Sensitivity of N- and P/Q-Type Ca2+ Channel
Currents to a ja Opioid in Isolectin B 4-Positive and -Negative
Dorsal Root Ganglion Neurons
Interaction between Dinucleotide and Nicotinic Receptors in
Individual Cholinergic Terminals
1218
Zi-Zhen Wu, Shao-Rui Chen, and
Hui-Lin Pan
939
Miguel Diaz-Hernandez,
Jesus Sanchez-Nogueiro, Jesus Pintor, and M.
Teresa Miras-Portugal
954
Repeated Amphetamine Couples Norepinephrine Transporter
and Calcium Channel Activities in PC12 Cells
L. Kantor, M. Zhang, B. Guptaroy,
Y. H. Park, and M. E. Gnegy
1044
Long-Term Ethanol Self-Administration by Cynomolgus
Macaques Alters the Pharmacology and Expression of
GABAA Receptors in Basolateral Amygdala
Cytoprotective Efficacy and Mechanisms of the Kiposoluble
Iron Chelator 2,2'-Dipyridyl in the Rat Photothrombotic
Ischemic Stroke Model
Donald W. Floyd, David P. Friedman.
James B. Daunais, Peter J. Pierre, Kathleen
A. Grant, and Brian A. McCool
1071
C. Demougeot, M. Van Hoecke, N. Bertrand,
A. Prigent-Tessier, C. Mossiat, A. Beley, and
C. Marie
1080
Potentiation of the Osmosensitive Release of Taurine and DAspartate from SH-SY5Y Neuroblastoma Cells after
Activation of M 3 Muscarinic Cholinergic Receptors
Anne M. Heacock, Daniel Kerley,
Grzegorz T. Gurda, Aaron T.
VanTroostenberghe, and Stephen K.
Fisher
1097
Effects of y- and Hydroxypropyl-Y-cyclodextrins on the
Transport of Doxorubicin across an in Vitro Model of BloodBrain Barrier
V. Monnaert, D. Betbeder, L. Fenart, H.
Bricout, A. M. Lenfant, C. Landry, R.
Cecchelli, E. Monflier, and S. Tilloy
1115
Tanya C. McCarthy, P. Timothy Pollak,
Elyisha A. Hanniman, and Christopher J.
Sinai
864
Raoef Imamdi, Marjo de Graauw, and
Bob van de Water
892
TOXICOLOGY
Disruption of Hepatic Lipid Homeostasis in Mice after
Amiodarone Treatment Is Associated with Peroxisome
Proliferator-Activated Receptor-a Target Gene Activation
Protein Kinase C Mediates Cisplatin-Induced Loss of
Adherens Junctions Followed by Apoptosis of Renal Proximal
Tubular Epithelial Cells
ERRATUM
Correction to "p53-Dependent Apoptotic Mechanism of a New
Designer Bimetallic Compound Tri-phenyl Tin
Benzimidazolethiol Copper Chloride (TPT-CuCl2): In Vivo
Studies in Wistar Rats as Well as in Vitro Studies in Human
Cervical Cancer Cells"
Naseruddin Hoti, De-e Zhu, Zhiyin Song,
Zhengsheng Wu, Sartaj Tabassum, and
Mian Wu
1281