The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
Vol. 318, No. 2
August 2006
Contents
PERSPECTIVES IN PHARMACOLOGY
Neuroproteomics of the Synapse and Drug Addiction
BEHAVIORAL PHARMACOLOGY
Pharmacological Characterization of Hydrolysis-Resistant
Analogs of Oleoylethanolamide with Potent Anorexiant
Properties
Antinociceptive and Hypothermic Effects of Salvinorin A Are
Abolished in a Novel Strain of K-Opioid Receptor-1 Knockout
Mice
Efficacy and the Discriminative Stimulus Effects of Negative
GABAA Modulators, or Inverse Agonists, in DiazepamTreated Rhesus Monkeys
CARDIOVASCULAR
Chronic /3-Adrenergic Receptor Stimulation Induces Cardiac
Apoptosis and Aggravates Myocardial Ischemia/Reperfusion
Injury by Provoking Inducible Nitric-Oxide SynthaseMediated Nitrative Stress
Amphetamine Analogs Increase Plasma Serotonin:
Implications for Cardiac and Pulmonary Disease
Ethanol Consumption Enhances Endothelin-1-Induced
Contraction in the Isolated Rat Carotid
CELLULAR AND MOLECULAR
Endoxifen, a Secondary Metabolite of Tamoxifen, and 4-OHTamoxifen Induce Similar Changes in Global Gene Expression
Patterns in MCF-7 Breast Cancer Cells
Interaction of Methotrexate with Organic-Anion Transporting
Polypeptide 1A2 and Its Genetic Variants
Noura S. Abul-Husn and Lakshmi A. Devi
Giuseppe Astarita, Barbara Di Giacomo,
Silvana Gaetani, Fariba Oveisi, Timothy
R. Compton, Silvia Rivara, Giorgio
Tarzia, Marco Mor, and Daniele Piomelli
Michael A. Ansonoff, Jiwen Zhang, Traci
Czyzyk, Richard B. Rothman, Jeremy
Stewart, Heng Xu, Jordan Zjwiony, Daniel J.
Siebert, Feng Yang, Bryan L. Roth, and John
E. Pintar
Lance R. McMahon, Lisa R. Gerak, and
Charles P. France
Aihua Hu, Xiangying Jiao, Erhe Gao,
Walter J. Koch, Said Sharifi-Azad, Zvi
Grunwald, Xin L, Ma, and Jian-Zhong
Sun
Dorota Zoikowska, Richard B. Rothman, and
Michael H. Baumann
Carlos R. Tirapelli, Debora A. Casolari,
Augusto C. Montezano, Alvaro Yogi, Rita C.
Tostes, Eurode Legros, Pedro D'OrleansJuste, Vera L. Lanchote, Sergio A. Uyemura,
and Ana M. de Oliveira
Young Chai Lim, Lang Li, Zeruesenay
Desta, Qianqian Zhao, James M. Rae,
David A. Flockhart, and Todd C. Skaar
Ilaria Badagnani, Richard A. Castro,
Travis R. Taylor, Claire M. Brett,
Conrad C. Huang, Douglas Slryke,
Michiko Kawamoto, Susan J. Johns,
Thomas E. Ferrin, Elaine J. Carlson,
Estcban G. Burchard, and Kathleen
M. Giacomini
461
563
641
907
469
604
819
503
521
Lysophosphatidic Acid Binds to and Activates GPR92, a G
Protein-Coupled Receptor Highly Expressed in
Gastrointestinal Lymphocytes
Knut Kotarsky, Ake Boketoft,
Jesper Bristulf, Niclas E. Nilsson,
Ake Norberg, Stefan Hansson,
Chrisler Owman, Rannar Sillard,
L. M. Fredrik Leeb-Lundberg, and
Bjorn Olde
619
Differential Coupling of Muscarinic MIS M2, and M3 Receptors
to Phosphoinositide Hydrolysis in Urinary Bladder and
Longitudinal Muscle of the lleum of the Mouse
John A. Tran, Minoru Matsui, and
Frederick J. Ehlert
649
Mark G. Slomiany and
Steven A. Rosenzweig
666
Laelic A. Snook, Graeme Milligan,
Brigitte L. Kieffer, and Dominique Massotte
683
Ya-Ling Hsu, Chien-Yu Cho, Po-Lin Kuo,
Yu-Ting Huang, and Chun-Ching Lin
484
Antitumor Activity of Sphingosine Kinase Inhibitors
Kevin J. French, John J. Upson,
Slaci N. Keller, Yan Zhuang, Jong K. Yun,
and Charles D. Smith
596
Efficient Gene Transfer into Macrophages and Dendritic Cells
by in Vivo Gene Delivery with Mannosylated Lipoplex via the
Intraperitoneal Route
Yoshiyuki Hattori, Shigeru Kawakami,
Kazumi Nakamura, Fumiyoshi Yamashita,
and Mitsuru Hashida
Jeanelle M. Martinez, Tina Sali,
Ryuji Okazaki, Colleen Anna,
Mclinda Hollingshead, Curtis Hose,
Anne Monks, Nigel J. Walker,
Seung Joon Baek, and Thomas E. Eling
828
\s\ Hypoxia-Inducible Factor-1-Dependent and -Independent
Regulation of Insulin-Like Growth Factor-1-Stimulated
Vascular Endothelial Growth Factor Secretion
fx-S Opioid Receptor Functional Interaction: Insight Using
Receptor-G Protein Fusions
CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY
Plumbagin (5-Hydroxy-2-methyl-l,4-naphthoquinone) Induces
Apoptosis and Cell Cycle Arrest in A549 Cells through p53
Accumulation via c-Jun NH2-Terminal Kinase-Mediated
Phosphorylation at Serine 15 in Vitro and in Vivo
Drug-Induced Expression of Nonsteroidal Anti-Inflammatory
Drug-Activated Gene/Macrophage Inhibitory Cytokine-1/
Prostate-Derived Factor, a Putative Tumor Suppressor,
Inhibits Tumor Growth
ENDOCRINE AND DIABETES
Antihyperglycemic and Antioxidant Properties of Caffeic Acid
in db/db Mice
899
Un Ju Jung, Mi-Kyung Lee, Yong Bok Park,
Seon-Min Jeon, and Myung-Sook Choi
476
High-Glucose-Altered Endothelial Cell Function Involves Both
Disruption of Cell-to-Cell Connection and Enhancement of
Force Development
Koji Nobe, Mari Miyatake, Tomoko Sone,
and Kazuo Honda
530
An Orally Active Cathepsin K Inhibitor, Furan-2-Carboxylic
Acid, OST-4077 [l-{J-[4-Fluoro-2-(2-oxo-pyrrolidin-l-yl)-'
phenyl] -3-oxo-piperidin-4-ylcarbamoyl }-cy clohexy 1) -am ide],
Inhibits Osteoclast Activity in Vitro and Bone Loss in
Ovariectomized Rats
M. K. Kim, H. D. Kim, J. H. Park. J. I. Urn,
J. S. Yang, W. Y. Kwak, S. Y. Sung,
H. J. Kim, S. H. Kim, C. H. Lee,
J. Y. Shim, M. H. Bae, Y. A. Shin, Y. Huh,
T. D. Han, W, Chong, H. Choi, B. N. Ahn,
S. O. Yang, and M. H. Son
555
A Selective Peroxisome Prolifera tor-Activated Receptor y
Modulator with Distinct Fat Cell Regulation Properties
Takao Fujimura, Chiaki Kimura,
Tomoya Oe, Yoko Takata,
Hiroyuki Sakuma, Ichiro Aramori, and
Seitaro Mutoh
863
Novel Glucagon-Like Peptide-1 (GLP-1) Analog (Val8)GLP-l
Results in Significant Improvements of Glucose Tolerance and
Pancreatic )3-Cell Function after 3-Week Daily Administration
in Obese Diabetic (ob/ob) Mice
Brian D. Green, Kerry S. Lavery,
Nigel Irwin, Finbarr P. M. O'Harte,
Patrick Harriott, Brett Greer, Clifford
J. Bailey, and Peter R. Flatt
914
Jason R. Kovac, Tom Chrones,
Harold G. Preiksaitis, and Stephen M. Sims
513
Ying H. Yang, William K. K. Wu,
Emily K. K. Tai, Helen P. S. Wong,
Emily K. Y. Lam, Wallace H. L. So,
Vivian Y. Shin, and Chi H. Cho
Ryo Hatazawa, Ryoko Ohno,
Mayu Tanigami, Akiko Tanaka, and
Koji Takeuchi
547
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL
H3 Tachykinin Receptor Expression and Function in Human
Esophageal Smooth Muscle
The Cationic Host Defense Peptide rCRAMP Promotes
Gastric Ulcer Healing in Rats
Roles of Endogenous Prostaglandins and Cyclooxygenase
Isozymes in Healing of Indomethacin-lnduced Small Intestinal
Lesions in Rats
Angiotensin-Converting Enzyme and Angiotensin II Receptor
Subtype 1 Inhibitors Restitute Hypertensive Internal Anal
Sphincter in the Spontaneously Hypertensive Rats
Marcio A. F. De Godoy and Satish Rattan
691
725
INFLAMMATION, IMMUNOPHARMACOLOGY, AND ASTHMA
Discovery and Characterization of Triaminotriazine Aniline
Amides as Highly Selective p38 Kinase Inhibitors
Tsung H. Lin, Axel Mctzger, David J. Diller,
Madhuri Desai, Ian Henderson. Gulzar
Ahmed, Earl F. Kimble, Elizabeth
Quadros, and Maria L. Webb
Tammy R. Ozment-Skelton,
Matthew P. Goldman, Siamon Gordon,
Gordon D. Brown, and David L. Williams
495
Pharmacological and Molecular Characterization of the
Mechanisms Involved in Prostaglandin E2-Induccd Mouse Paw
Edema
Rafaela F. Claudino, Candida A. L. Kassuya,
Juliano Ferreira, and Joao B. Calixto
611
Role of Matrix Metalloproteinases in the Inflammatory
Response in Human Airway Cell-Based Assays and in Rodent
Models of Airway Disease
Mark A. Bin-ell, Sissie Wong,
Abdel Dekkak, Jorge De Alba,
Saleem Haj-Yahia, and Maria G. Belvisi
741
Polymyxin B-Conjugated o^-Macroglobulin as an Adjunctive
Therapy to Sepsis: Modes of Action and Impact on Lethality
Gerd Birkcnmeier, Silke Nicklisch,
Christiane Pockelt, Andualem Mossie,
Volker Steger, Christiane Glaser,
Sunna Hauschildt, Elke Usbeck, Klaus Huse,
UUi Sack, Michael Bauer, and
Angchka Schafer
Sylvie Attucci, Alexandre Gauthier,
Brice Korkmaz, Pascal Delepine,
Michele Ferrer-Di Martino,
Francois Saudubray, Patrice Diot, and
Francis Gauthier
Victoria Boswell-Smith, Domenico Spina,
Alec W. Oxford, Mike B. Comer,
Esther A. Seeds, and Clive P. Page
762
Claudio Storini, Luigi Bergamaschini,
Raffaelia Gesuete, Emanuela Rossi,
Diana Maiocchi, and Maria Grazia De
Simoni
849
Qi Wang, Inger M. Darling, and
Marilyn E. Morris
751
CYP4 Isoform Specificity in the w-Hydroxylation of Phytanic
Acid, a Potential Route to Elimination of the Causative Agent
of Refsum's Disease
Tissue Distribution and Metabolism of the Tyrosine Kinase
Inhibitor ZD6474 (Zactima) in Tumor-Bearing Nude Mice
following Oral Dosing
Fengyun Xu, Valerie Y. Ng,
Deanna L. Kroetz, and Paul R.
Ortiz de Montellano
Daniel L. Gustafson,
Erica L. Bradshaw-Pierce, Andrea L. Merz,
and Joseph A. Zirrolli
835
Hepatobiliary Disposition of a Drug/Metabolite Pair:
Comprehensive Pharmacokinetic Modeling in SandwichCultured Rat Hepatocytes
Ryan Z. Turncnff, Keith A. Hoffmaster,
J. Cory Kalvass, Gary M. Pollack, and
Kim L. R. Brouwer
881
Takashi Mori, Terrence Town, Jun Tan,
Nobumichi Yada, Yuko Horikoshi, Junki
Yamamoto, Taiji Shimoda, Yoshihisa
Kamanaka, Narito Tateishi, and Takao
Asano
Sergei Melnik, Michael Wright,
Julian A. Tanner, Timur Tsintsadze, Vera
Tsintsadze, Andrew D. Miller, and Natalia
Lozovaya
Dustin W. DuBois, Andreas Perlegas,
Donald W. Floyd, Jeffery L. Weiner, and
Brian A. McCool
571
Prolonged Reduction of Leukocyte Membrane-Associated
Dectin-1 Levels following /3-Glucan Administration
EPI-hNE4, a Proteolysis-Resistant Inhibitor of Human
Neutrophil Elastase and Potential Anti-Inflammatory Drug for
Treating Cystic Fibrosis
The Pharmacology of Two Novel Long-Acting
Phosphodiesterase 3/4 Inhibitors, RPL554 [9,10-Dimethoxy2(2,4,6-trimethylphenyIimino)-3-(A'-carbamoyI-2-aminoethyl)3,4,6,7-tetrahydro-2//-pyrimido[6,l-a]isoquinolin-4-one] and
RPL565 [6,7-Dihydro-2-(2,6-diisopropylphenoxy)-9,10dimethoxy-4/f-pyrimido[6,l-a]isoquinolin-4-one]
Selective Inhibition of Plasma Kallikrein Protects Brain from
Reperfusion Injury
METABOLISM, TRANSPORT, AND PHARMACOGENOMICS
Transport of y-Hydroxybutyrate in Rat Kidney Membrane
Vesicles: Role of Monocarboxylate Transporters
NEUROPHARMACOLOGY
Arundic Acid Ameliorates Cerebral Amyloidosis and Gliosis
in Alzheimer Transgenic Mice
[JO Diadenosine Polyphosphate Analog Controls Postsynaptic
Excitation in CA3-CA1 Synapses via a Nitric OxideDependent Mechanism
Distinct Functional Characteristics of the Lateral/Basolateral
Amygdala GABAergic System in C57BL/6J and DBA/2J Mice
Dcsvcnlafaxine Succinate: a New Serotonin and
Norepinephrine Reuptake Inhibitor
Darlene C. Deecher, Chad E. Beyer,
Grace Johnston, Jenifer Bray, S. Shah, M.
Abou-Gharbia, and Terrance H. Andree
540
803
840
872
579
629
657
Methamphetamine Administration Reduces Hippocampal
Vesicular Monoamine Transporter-2 Uptake
Regulation of Kindling Epileptogenesis by Hippocampal
Galanin Type 1 and Type 2 Receptors: The Effects of
Subtype-Selective Agonists and the Role of G-ProteinMediated Signaling
Time-Dependent Effects of Haloperidol and Ziprasidone on
Nerve Growth Factor, Cholinergic Neurons, and Spatial
Learning in Rats
Inhibition of Paclitaxel-Induced A-Fiber Hypersensitization by
Gabapentin
Pharmacological Characterization of the Competitive GLUK5
Receptor Antagonist Decahydroisoquinoline LY46619S in
Vitro and in Vivo
The Dopamine Stabilizers (S)-(-)-(3-Methanesulf'onyl-phenyl)1-propyl-piperidine [(-)-OSU6162] and 4-(3-Methylsulfonylphenyl)-l-propyl-piperidine (ACR16) Show High in Vivo D 2
Receptor Occupancy, Antipsychotic-Like Efficacy, and Low
Potential for Motor Side Effects in the Rat
Identification of Novel Small Molecule Inhibitors of Amyloid
Precursor Protein Synthesis as a Route to Lower Alzheimer's
Disease Amyloid-/? Peptide
Effect of Vagus Nerve Stimulation on Serotonergic and
Noradrenergic Transmission
Pharmacological Stimulation of Group II Metabotropic
Glutamate Receptors Reduces Cocaine Self-Administration and
Cocaine-Induced Reinstatement of Drug Seeking in Squirrel
Monkeys
TOXICOLOGY
Proteomic Analysis of Rat Liver Phosphoproteins after
Treatment with Protein Kinase Inhibitor H89 (N-(2-\pBromocinnamylamino-]ethyl)-5-isoquinoIinesulfonamide)
Megalin-Dependent Internalization of CadmiumMetallothionein and Cytotoxicity in Cultured Renal Proximal
Tubule Cells
Alterations in the Rat Serum Proteome during Liver Injury
from Acetaminophen Exposure
Kristi S. Rau, Elisabeth Birdsall,
Trent J. Volz, James A. Riordan,
Anthony J. Baucum II. Brian P. Adair,
Rebecca Bitter, James W. Gibb, Glen R. Hanson,
and Annette E. Fleckenstein
Andrey Mazarati, Linda Lundstrom,
Ulla Sollenberg, Don Shin, Ulo Langel, and
Raman Sankar
676
Alvin V. Terry, Jr., Vinay Parikh,
Debra A. Gearhart, Anilkumar Pillai,
Elizabeth Hohnadel, Samantha Warner.
Henry A. Nasrallah, and Sahebarao P.
Mahadik
709
Misaki Matsumoto, Makoto Inoue, Andreas Hald,
Weijiao Xie, and Hiroshi Ueda
700
735
Brianne Weiss, Andrew Alt,
Ann Marie Ogden, Mary Gates,
Donna K. Dieckman, Amy Clemens-Smith,
Ken H. Ho, Keith Jarvie, Geihan Rizkalla,
Rebecca A. Wright, David O. Calligaro,
Darryle Schoepp, Edward L. Mattiuz,
Robert E. Stratford, Bryan Johnson,
Craig Salhoff, Mary Katofiasc, Lee A. Phebus.
Kathryn Schenck, Marlene Cohen,
Sandra A. Filla, Paul L. Ornstein,
Kirk W. Johnson, and David Bleakman
772
Sridhar Natesan, Kjcll A. Svensson,
Greg E. Reckless, Jose N. Nobrega, Karen
B. L. Barlow, Anette M. Johansson, and
Shitij Kapur
810
Tada Utsuki, Qian-sheng Yu,
Diane Davidson, Dcmao Chen, Harold W.
Holloway, Arnold Brossi, Kumar
Sambamurti, Debomoy K. Lahiri, Nigel H.
Greig, and Tony Giordano
855
Adrienne E. Dorr and Guy Debonnel
890
A. S. Adewale. D. M. Platt, and
R. D. Spealman
922
Myrtle A. Davis, Douglas Hinerfeld,
Sajan Joseph, Yu-Hua Hui, Naijia H. Huang, John
Leszyk, Jennifer Rutherford-Bernard, and Sun W.
Tarn
589
Natascha A. Wolff, Marouan Abouhamed,
Pierre J. Veixoust, and Frank Thevenod
782
B. Alex Merrick, Maribel E. Bruno,
Jennifer H. Madenspacher, Barbara A. Wetmore.
Julie Foley, Rembert Pieper, Ming Zhao. Anthony
J. Makusky, Andrew M. McGrath, Jeff X. Zhou,
John Taylor, and Kenneth B. Tomer
792