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The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
Vol 312, No. 3
March 2005
Contents
O6OB%fl3K
PERSPECTIVES IN PHARMACOLOGY
Cannabinoid CBX Receptor Antagonists as PromisingOBIrtR
New
Bernard Le Foil and Steven R. Goldberg
875
Medications for Drug Dependence
ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION
Predictive Models of CYP3A4 Heteroactivation: In Vitro-in Vivo Ann-Charlotte Egtiell, J. Brian Houston, and
Scaling and Pharmacophore Modeling
C. Scott Boyer
Immunogenicity and Rapid Blood Clearance of Liposomes
Sean C. Semple, Troy O. Harasym, Kathy
Containing Polyethylene Glycol-Lipid Conjugates and Nucleic
A. Clow, Steven M. Ansell, Sandra K.
Acid
Klimuk, and Michael J. Hope
926
1020
Renal D-Amino Acid Oxidase Mediates Chiral Inversion of
A^-Nitro-D-arginine
Two Major Grapefruit Juice Components Differ in Time to
Onset of Intestinal CYP3A4 Inhibition
Yan-Fei Xin, Xiang-Jun Zhou, Xi Cheng,
and Yong-Xiang Wang
Mary F. Paine, Anne B. Criss, and
Paul B. Watkins
P-Glycoprotein and Mutlidrug Resistance-Associated Proteins
Limit the Brain Uptake of Saquinavir in Mice
Seonghee Park and Patrick J. Sinko
1249
Carrie K. Jones, Elizabeth Lutz Eberle,
David B. Shaw, David L. McKinzie, and
Harlan E. Shannon
1055
E. L. Lane, S. Cheetham, and P. Jenner
1124
Sharon Bingham, Paul J. Beswick,
Chas Bountra, Terry Brown,
Ian B. Campbell, Iain P. Chessell,
Nick Clayton, Sue D. Collins,
Philip T. Davey, Helen Goodland,
Norman Gray, Claudine Haslam,
Jonathan P. Hatcher, A. Jacqueline Hunter,
Fiona Lucas, Graham Murkitt, Alan Naylor,
Elizabeth Pickup, Becky Sargent,
Scott G. Summerfield, Alexander Stevens,
Sharon C. Stratton, and Joanne Wiseman
1161
BEHAVIORAL PHARMACOLOGY
Pharmacologic Interactions between the Muscarinic
Cholinergic and Dopaminergic Systems in the Modulation of
Prepulse Inhibition in Rats
Dopamine Uptake Inhibitor-Induced Rotation in 6Hydroxydopamine-Lesioned Rats Involves Both D, and D 2
Receptors but Is Modulated through 5-Hydroxytryptamine
and Noradrenaline Receptors
The Cyclooxygenase-2 Inhibitor GW406381X [2-(4EthoxyphenyI)-3-[4-(methylsulfonyl)phenyl]-pyrazolo[l,5ijpyridazine] Is Effective in Animal Models of Neuropathic
Pain and Central Sensitization
Attenuation of Behavioral Effects of Cocaine by the
Metabotropic Glutamate Receptor 5 Antagonist 2-MethyI-6(phenylethynyl)-pyridine in Squirrel Monkeys: Comparison
with Dizocilpine
Buyean Lee, Donna M. Platt,
James K. Rowlett, Adepero S. Adewale, and
Roger D. Spealman
1090
1151
1232
Self-Administration of Cocaine-Opioid Combinations by
Rhesus Monkeys: Evaluation of the Role of jx Receptor
Efficacy Using Labor Supply Analysis
CARDIOVASCULAR
Poly(ADP-Ribose) Polymerase Promotes Cardiac Remodeling,
Contractile Failure, and Translocation of Apoptosis-Inducing
Factor in a Murine Experimental Model of Aortic Banding
and Heart Failure
Cyclooxygenase-2 Inhibition Improves Vascular Endothelial
Dysfunction in a Rat Model of Endotoxic Shock: Role of
Inducible Nitric-Oxide Synthase and Oxidative Stress
James K. Rowlett, Joshua S. Rodefer, and
Roger D. Spealman
1289
Chun-Yang Xiao, Min Chen,
Zsuzsanna Zsengeller, Hongshan Li, Levente
Kiss, Mark Kollai, and Csaba Szabo
891
Agostino Virdis, Rocchina Colucci,
Matteo Fornai, Corrado Blandizzi,
Emiliano Duranti, Stefania Pinto,
Nunzia Bernardini, Cristina Segnani,
Luca Antonioli, Stefano Taddei,
Antonio Salvetti, and Mario Del Tacca
945
Blood Clearance and Activity of Erythrocyte-Coupled
Fibrinolytics
Kumkum Ganguly, Tatiana Krasik,
Sandra Medinilla. Khali! Bdeir,
Douglas B. Cines, Vladimir R. Mnzykantov,
and Juan Carlos Murciano
1106
The Effects of Tamoxifen and Its Metabolites on Platelet
Function and Release of Reactive Oxygen Intermediates
Olga Vitseva, David A. Flockhart, Yan Jin,
Sonia Varghese, and Jane E. Freedman
1144
Epidermal Growth Factor Receptor-Dependent and Independent Pathways in Hydrogen Peroxide-Induced
Mitogen-Activated Protein Kinase Activation in
Cardiomyocytes and Heart Fibroblasts
Sally Purdom and Qin M. Chen
] 179
Raloxifcne Relaxes Rat Pulmonary Arteries and Veins: Roles
of Gender, Endothelium, and Antagonism of Ca 2+ Influx
Yau-Chi Chan, Fung-Ping Leung,
Xiaoqiang Yao, Chi-Wai Lau, Paul
M. Vanhoutte, and Yu Huang
1266
Differences in Tail Vascular Bed Reactivity in Rats with and
without Heart Failure following Myocardial Infarction
Raquel Binda Pereira,
Carmem Luiza Sartorio, Daiton
Valentim Vassallo, and Ivanita
Slefanon
1321
A New ATP-Sensitive Potassium Channel Opener Reduces
Blood Pressure and Reverses Cardiovascular Remodeling in
Experimental Hypertension
Hai Wang, Cbao-Liang Long, and
Ying-Li Zhang
1326
CELLULAR AND MOLECULAR
Green Tea PolyphenoMnduced Epidermal Keratinocyte
Differentiation Is Associated with Coordinated Expression of
p57/KIP2 and Caspase 14
Stephen Hsu, Tetsuya Yamamoto,
James Borke, Douglas S. Walsh,
Baldev Singh, Sushma Rao,
Kamatani Takaaki, Nam Nah-Do,
Carol Lapp, David Lapp, Emily Foster,
Wendy B. Bollag, Jill Lewis, John Wataha,
Tokio Osaki, and George Schuster
884
Induction of Nitric Oxide Production by the Cytostatic
Macrolide Apicularen A [2,4-Heptadienamide, N-[{lE)-3[(3S,5R,7R,9S)-3,4,5,6,7,8,9,10-octahydro-7,14Dihydroxy-l-oxo5,9-epoxy-l//-2-benzoxacyclododecin-3-yl]-1 propenyl]-,
(2Z,4Z)-(9CI)] and Possible Role of Nitric Oxide in Apicularen
A-Induced Apoptosis in RAW 264.7 Cells
JangJa Hong, Aya Yokomakura,
Yasuhiro Nakano, Hyun Seung Ban,
Kenji Ishihara, Jong-Woong Ahn,
OkPyo Zee, and Kazuo Ohuchi
968
Positional Isomerism Markedly Affects the Growth Inhibition
of Colon Cancer Cells by Nitric Oxide-Donating Aspirin in
Vitro and in Vivo
Khosrow Kashfi, Simona Borgo,
Jennie L. Williams, Jie Chen, Jianjun Gao,
Athanasios Glekas, Francesca Benedini,
Piero del Soldato, and Basil Rigas
978
In Vitro Metabolism of Nitric Oxide-Donating Aspirin: The
Effect of Positional Isomerism
Jianjun Gao, Khosrow Kashfi, and
Basil Rigas
989
Angiotensin II-Induced Akt Activation through the Epidermal
Growth Factor Receptor in Vascular Smooth Muscle Cells Is
Mediated by Phospholipid Metabolites Derived by Activation
of Phospholipase D
Fang Li and Kafait U. Malik
1043
Evidence for Pleiotropic Signaling at the Mouse /3 3Adrcnoceptor Revealed by SR59230A [3-(2-Ethylphenoxy)-l-[(1
,S)-1,2,3,4-tetrahy dronapth-1 -ylamino] -2S-2-propanol Oxalate]
Dana S. Hutcbinson, Masaaki Salo,
Bronwyn A. Evans, Arthur Christopoulos,
and Roger J. Summers
1064
Phospholipase D Signaling and Extracellular Signal-Regulated
Kinase-1 and -2 Phosphorylation (Activation) Are Required
for Maximal Phorbol Ester-Induced Transglutaminase
Activity, a Marker of Keratinocyte Differentiation
Wendy B. Bollag, Xiaofeng Zhong.
M. Ernest Dodd, David M. Hardy, Xiangjian
Zheng, and W. Thomas AUred
1223
Protease Inhibitor Treatments Reveal Specific Involvement of
Matrix MetaIloproteinase-9 in Human Adipocyte
Differentiation
CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY
YC-1 [3-(5'-Hydroxymethyl-2'-furyl)-l-benzyl Indazole]
Exhibits a Novel Antiproliferative Effect and Arrests the Cell
Cycle in G 0-Gi in Human Hepatocellular Carcinoma Cells
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL
Effect of Neocuproine, a Copper(I) Chelator, on Rat Bladder
Function
Endogenous Interleukin-6 Enhances the Renal Injury,
Dysfunction, and Inflammation Caused by
Ischemia/Reperfusion
INFLAMMATION AND IMMUNOPHARMACOLOGY
Effect of E6060 [4-{5-[7-Fluoro-4{trifluoromethyl)benzo[/>]furan-2-yl]-l/^2-pyrrolyI}benzoic
Acid], a Novel Subtype-Selective Retinoid, on Lupus-Like
Nephritis in Female (NZBxNZW)Fl Mice
Virginie Bourlier, Alexia Zakaroff-Girard,
Sandra De Barms, Christophe Pizzacalla,
Veronique Durand de Saint Front, Max
Lafonlan, Anne Bouloumie, and Jean
Galitzky
Shih-Wei Wang, Shiow-Lin Pan,
Jih-Hwa Guh, Hui-Iing Chen, DongMing Huang, Ya-Ling Chang, ShengChu Kuo. Fang-Yu Lee, and Che-Ming
Teng
1272
917
Cemil Gocmen, Ben Giesselman, and
William C. de Groat
1138
Nimesh S. A. Patel, Prabal K. Chatterjee,
Rosanna Di Paola, Emanuela Mazzon,
Domenico Britti, Angelina De Sarro,
Salvalore Cuzzocrea, and Chris toph
Thiemermann
1 170
Prostaglandin D2-Induced Eosinophilic Airway Inflammation Is
Mediated by CRTH2 Receptor
Toshihiko Yamauchi, Akira Ishibashi,
Kohdoh Shikata, Naoki Tokuhara, Kenichiro Seine. Seiichi Kobayashi, and Mitsuo
Nagai
Yoshiki Shiraishi, Koichiro Asano,
Takeshi Nakajima, Tsuyoshi Oguma,
Yusuke Suzuki, Tctsuya Shiomi,
Koichi Sayama, Kyoko Niimi, Misa Wakaki,
Junko Kagyo, Eiji Ikeda, Hiroyuki Hirai,
Kazuhiro Yamaguchi, and Akitoshi Ishizaka
Ethyl Pyruvate Inhibits Nuclear Factor-KB-Dependent
Signaling by Directly Targeting p65
Yusheng Han, Joshua A. Englert,
Runkuan Yang, Russell L. Delude, and
Mitchell P. Fink
1097
Glabridin, an Isoflavan from Licorice Root, Inhibits Inducible
Nitric-Oxide Synthase Expression and Improves Survival of
Mice in Experimental Model of Septic Shock
Valdecoxib: Assessment of Cyclooxygenase-2 Potency and
Selectivity
Jong Soon Kang, Yeo Dae Yoon,
Ig Jun Cho, Mi Hwa Han, Chang Woo Lee,
Song-Kyu Park, and Hwan Mook Kim
1187
James K. Gierse, Yan Zhang,
William F. Hood, Mark C. Walker,
Jennifer S. Trigg, Timothy J. Maziasz,
Carol M. Koboldt, Jerry L. Muhammad,
Ben S. Zweifel, Jaime L. Masferrer,
Peter C. Isakson, and Karen Seibcrt
1206
Cilostazol Prevents Remnant Lipoprotein Particle-Induced
Monocyte Adhesion to Endothelial Cells by Suppression of
Adhesion Molecules and Monocyte Chemoattractant Protein-1
Expression via Lectin-Like Receptor for Oxidized LowDensity Lipoprotein Receptor Activation
So Youn Park, Jeong Hyun Lee,
Yong Ki Kim, Chi Dae Kim,
Byung Yong Rhim, Won Suk Lee, and
Ki Whan Hong
1241
NEUROPHARMACOLOGY
Differential Effects on Current Kinetics by Point Mutations in
the lurcher Motif of NR1/NR2A Receptors
Corticotropin-Releasing Factor Receptor 1 and Central Heart
Rate Regulation in Mice during Expression of Conditioned
Fear
\s} Amiloride Peptide Conjugates: Prodrugs for Sodium-Proton
Exchange Inhibition
Mixed-Lineage Kinase Inhibitors Require the Activation of
Trk Receptors to Maintain Long-Term Neuronal Trophism
and Survival
Dual, Hyperalgesic, and Analgesic Effects of the High-Efficacy
5-Hydroxytryptamine 1A (5-HT1A) Agonist F 13640 [(3Chloro-4-fluoro-phenyl)-[4-fluoro-4-{[(5-methyl-pyridin-2ylmethyl)-ainino]-methyl}piperidin-l-yl]methanone, Fumaric
Acid Salt]: Relationship with 5-HT,A Receptor Occupancy and
Kinetic Parameters
938
954
Bo Hu and Fang Zheng
899
Oliver Stiedl, Michael Meyer, Olaf Jahn,
Sven Ove Ogren, and Joachim Spiess
905
Hasan Palandoken, Kolbot By, Manu Hegde,
William R. Harley, Fredric A. Gorin, and
Michael H. Nant?
Leo H. Wang, Andrew J. Paden, and
Eugene M. Johnson, Jr.
961
Laurent Bardin, Marie-Bernadette Assie,
Marline Pelissou, Isabelle Royer-Urios,
Adrian Newman-Tancredi, Jean-Paul Ribel,
Francois Sautel, Wouter Koek, and Francis
C. Colpaert
1007
1034
A Tyr-W-MIF-1 Analog Containing D-Pro2 Acts as a Selective
jLt2-Opioid Receptor Antagonist in the Mouse
Hiroyuki Watanabe, Daisuke Nakayama,
Kanenori Ito, Chizuko Watanabe,
Hirokazu Mizoguchi, Tsutomu Fujimura,
Kimie Murayama, Shunsuke Kawamura,
Takurai Sato, Chikai Sakurada,
Tsukasa Sakurada, and Shinobu Sakurada
1075
Differential GABAit Receptor Modulation of Ethanol Effects on
GABAA Synaptic Activity in Hippocampal CA1 Neurons
[(pF)Phe4,Arg14,Lys15]N/OFQ-NH2 (UFP-102), a Highly Potent
and Selective Agonist of the Nociceptin/Orphanin FQ Receptor
Peter H. Wu, Wolfgang Poelchen, and
William R. Proctor
1082
Giacomo Carra, Anna Rizzi, Remo Guerrini,
Timothy A. Barnes, John McDonald,
Christopher P. Hebbes, Flora Mela,
Velga A. Kenigs, Giuliano Marzola,
Daniela Rizzi, Elaine Gavioli,
Silvia Zucchini, Domenico Regoli,
Michele Morari, Severo Salvador!,
David J. Rowbotham, David G. Lambert,
Daniel R. Kapusta, and Girolamo Calo'
Mayuko Oda, Norihito Kitagawa,
Bang-Xiang Yang, Tadahide Totoki, and
Masatoshi Morimoto
1114
Quantitative and Fiber-Selective Evaluation of DoseDependent Nerve Blockade by Intrathecal Lidocaine in Rats
Memantine Blocks a7* Nicotinic Acetylcholine Receptors
More Potently Than A'-Methyl-D-aspartate Receptors in Rat
Hippocampal Neurons
;
The Selective a7 Nicotinic Acetylcholine Receptor Agonist
PNU-282987[A4(3tf)-l-Azabicyclo[2.2.2]oct-3-yl]-4chlorobenzamide Hydrochloride] Enhances GABAergic
Synaptic Activity in Brain Slices and Restores Auditory
Gating Deficits in Anesthetized Rats
Differential Mechanisms of Antianalgesia Induced by
Endomorphin-1 and Endomorphin~2 in the Ventral
Periaqueductal Gray of the Rat
Postnatal Inorganic Lead Exposure Reduces Midbrain
Dopaminergic Impulse Flow and Decreases Dopamine Dl
Receptor Sensitivity in Nucleus Accumbens Neurons
Nicotinic Acetylcholine Receptor-Mediated [3H]Dopamine
Release from Hippocampus
Repeated Cocaine Administration Increases Membrane
Excitability of Pyramidal Neurons in the Rat Medial
Prefrontal Cortex
Comparison of Peptidic and Nonpeptidic 5-Opioid Agonists on
Guanoshie 5'-0-(3-[35S]thio)triphosphate ([35S]GTPyS) Binding
in Brain Slices from Sprague-Dawley Rats
TOXICOLOGY
Protein Kinase C Signaling as a Survival Pathway against
CYP2E1-Derived Oxidative Stress and Toxicity in HepG2
Cells
Ciglitazone-Induced Lenticular Opacities in Rats: In Vivo and
Whole Lens Explant Culture Evaluation
ERRATUM
Correction to "DiPOA ([8-(3,3-Diphenyl-propyl)-4-oxo-lphenyl-1,3,8-triazaspiro[4,5]dec-3-yI]-acetic Acid), a Novel,
Systematically Available, and Peripherally Restricted Mu
Opioid Agonist with Antihyperalgesic Activity: II. In Vivo
Pharmacological Characterization in the Rat"
1132
Yasco Aracava, Edna F. R, Pereira,
Alfred Maelicke, and Edson X. Albuquerque
1195
M. Hajos, R. S. Hurst, W. E. Hoffmann,
M. Krause, T. M. Wall, N. R. Higdon, and
V. E. Groppi
1213
MaiaTerashvili, Hsiang-en Wu,
Randy J. Leitermann, Han-Sen Sun,
Andrew D. Clithero, and Leon F. Tseng
1257
Mahboubeh Tavakoli-Nezhad and
David K. Pitts
1280
Ying-Jun Cao, Carol S. Surowy, and
Pamela S. Puttfarcken
1298
Fernando J. Nasif, Kyriaki Sidiropoulou,
Xiu-Ti Hu, and Francis J. White
1305
Emily M. Julkiewicz, Nicholas P. Walker,
John E. Folk, Kenner C. Rice,
Philip S. Portoghese, James H. Woods, and
John R. Traynor
1314
Jose M. Jimenez-Lopez and
Arthur I. Cederbaum
998
Michael D. Aleo, Colleen M. Doshna, and
Kimberly A. Navetta
1027
Garth T. Whiteside, James E. Harrison,
Michelle S. Pearson, Zhengming Chen,
Paul I. Turchin, James D. Pomonis,
Lilly Mark, Katharine Walker, and
Kevin C. Brogle
1334