Download 325_02_2008

The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
July 2008
Vol. 325, No. 2
Contents
PERSPECTIVES IN PHARMACOLOGY
Progress in Brain Penetration Evaluation in Drug Discovery
and Development
XJngrong Liu, Cuiping Chen, and
Bill J. Smith
349
Sara Jane Ward, Timothy W. Lefever,
Cavario Jackson, Ronald J. Tallarida, and
Ellen A. Walker
567
Gregory T. Collins, Diane M. Calinski,
Amy Hauck Newman, Peter Grundt, and
James H. Woods
691
Sonia Marti nez-Rcvelles,
Francesc Jknenez-Altayo, Laura Caracuel,
Fernando J. Perez-Asensio, Anna M. Planas,
and Elisabet Vila
363
Antiatherosclerotic Effects of Small-Molecular-Weight
Compounds Enhancing Endothelial Nitric-Oxide Synthase
(eNOS) Expression and Preventing eNOS Uncoupling
Paulus Wohlfart, Hui Xu, Alexandra Endlich,
Alice Habermeier, Ellen I. Closs,
Thomas Hiibschle, Christian Mang,
Hartmut Strobel, Ten Suzuki,
Hartmut Kleinert, Ulrich Forstermann,
Hartmut Ruetten, and Huige Li
370
Delivery of Acid Sphingomyelinase in Normal and NiemannPick Disease Mice Using Intercellular Adhesion Molecule-1Targeted Polymer Nanocarriers
Carmen Garnacho, Rajwinder Dhami,
Eric Simone, Thomas Dziubla,
John Leferovich, Edward H. Schuchman,
Vladimir Muzykantov, and Silvia Muro
400
Oxygenated Perfluorochemicals Improve Cell Survival during
Reoxygenation by Pacifying Mitochondrial Activity
In Vivo Activation of Peroxisome Proliferator-Activated
Receptor-S Protects the Heart from Ischemia/Reperfusion
Injury in Zucker Fatty Rats
Amina Arab, Klaus Kuemmerer, Jin Wang,
Christoph Bode, and Christoph Hehrlein
417
Tian-Li Yue, Sandhya S. Nerurkar,
Weike Bao, Beat M. Jucker, Lea Sarov-Blat,
Klaudia Steplewski, Eliot H. Ohlstein, and
Robert N. Willette
466
BEHAVIORAL PHARMACOLOGY
Effects of a Cannabinoid, Receptor Antagonist and
Serotonin2C Receptor Agonist Alone and in Combination on
Motivation for Palatable Food: A Dose-Addition Analysis
Study in Mice
Food Restriction Alters iV'-Propyl-4,5,6,7tetrahydrobenzothiazole-2,6-diamine dihydrochloride
(Pramipexole)-Induced Yawning, Hypothermia, and
Locomotor Activity in Rats: Evidence for Sensitization of
Dopamine D2 Receptor-Mediated Effects
CARDIOVASCULAR
Endotlielial Dysfunction in Rat Mesenteric Resistance Artery
after Transient Middle Cerebral Artery Occlusion
[s] Vascular KCNQ Potassium Channels as Novel Targets for the
Control of Mesenteric Artery Constriction by Vasopressin,
Based on Studies in Single Cells, Pressurized Arteries, and in
Vivo Measurements of Mesenteric Vascular Resistance
Alexander R. Mackie,
Lioubov I. Brueggemann, Kyle K. Henderson,
Aaron J. Shiels, Leanne L. Cribbs,
Karie E. Scrogin, and Kenneth L. Byron
475
\s} Cardioprotective and Survival Benefits of Long-Term
Combined Therapy with 0 2 Adrenoreceptor (AR) Agonist and
Pl AR Blocker in Dilated Cardiomyopathy Postmyocardial
Infarction
Ismayil Ahmet, Melissa Krawczyk,
Weizhong Zhu, Anthony Yiu-Ho Woo,
Christopher Morrell, Suresh Poosala,
Riu-ping Xiao, Edward G. Lakatta, and
Mark I. Talan
Jian-Bing Shen and Achilles J. Pappano
491
Mark A. Hallman, Shougang Zhuang, and
Rick G. SchneHmann
520
N. D. Sonawane, Olga Zegarra-Moran, Wan
Namkung, Luis J. V. Galietta, and
A. S. Verkman
529
Dennis Verzijl, Stefania StorelH, Danny J.
Scholten, Leontien Bosch, Todd A.
Reinhart, Daniel N. Streblow, Cornelis P.
Tensen, Carlos P. Fitzsimons, Guido J. R.
Zaman, James E. Pease, Iwan J. P. de Esch,
Martine J. Smit, and Rob Leurs
544
An Estrogen Metabolite, 2-Methoxyestradiol, Disrupts Cardiac
Microtubules and Unmasks Muscarinic Inhibition of Calcium
Current
CELLULAR AND MOLECULAR
Regulation of Dedifferentiation and Redifferentiation in Renal
Proximal Tubular Cells by the Epidermal Growth Factor
Receptor
[s] a-Aminoazaheterocyclic-Methylglyoxal Adducts Do Not
Inhibit Cystic Fibrosis Transmembrane Conductance
Regulator Chloride Channel Activity
Noncompetitive Antagonism and Inverse Agonism as
Mechanism of Action of Nonpeptidergic Antagonists at
Primate and Rodent CXCR3 Chemokine Receptors
UDP Is a Competitive Antagonist at the Human P2Y!
Receptor
CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY
Statin-Induced Inhibition of 3-Hydroxy-3-MethyI Glutaryl
Coenzyme A Reductase Sensitizes Human Osteosarcoma Cells
to Anticancer Drugs
Cytokeratin-RNA Cross-Linking Mediated by the Antitumor
Aminoflavone, 5-Amino-2,3-fluorophenyl-6,8-difluoro-7-methyl4if-l-benzopyran-4-one
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL
Is] Thioredoxin-1 Ameliorates Cigarette Smoke-Induced Lung
Inflammation and Emphysema in Mice
\s\ Drug-Induced Alterations to Gene and Protein Expression in
Intestinal Epithelial Cell 6 Cells Suggest a Role for Calpains in
the Gastrointestinal Toxicity of Nonsteroidal AntiInflammatory Agents
Tetrathiomolybdate Protects against Bile Duct LigationInduced Cholestatic Liver Injury and Fibrosis
Isoflavones Promote Mitochondrial Biogenesis
INFLAMMATION, IMMUNOPHARMACOLOGY, AND ASTHMA
MF498 [AM[4-(5,9-Diethoxy-6-oxo-6,8-dihydro-7Jf-pyrrolo[3,4-g]
quinolin-7-yl)-3-methylbenzyl]su!fonyl}-2-(2-methoxyphenyl)
acetamide], a Selective E Prostanoid Receptor 4 Antagonist,
Relieves Joint Inflammation and Pain in Rodent Models of
Rheumatoid and Osteoarthritis
Ingrid P. Fricks, Savitri Maddileti, Rhonda
L. Carter, Eduardo R. Lazarowski, Robert
A. Nicholas, Kenneth A. Jacobson, and T.
Kendall Harden
507
588
Olivia Fromigue, Zahia Hamidouche, and
Pierre J. Marie
595
Ling-hua Meng, Zhaojing Meng,
Ze-hong Miao, Timothy D. Veenstra, and
Yves Pommier
674
Atsuyasu Sato, Yuma Hoshino,
Tomijiro Hara, Shigeo Muro,
Hajime Nakamura, Michiaki Mishima, and
Junji Yodoi
380
N. N. Raveendran, K. Silver, L. C. Freeman,
D. Narvaez, K. Weng, S. Ganta, and J.
D. Lillich
389
Ming Song, Zhenyuan Song, Shirish Barve,
Jingwen Zhang, Theresa Chen, Marcia Liu,
Gavin E. Arteel, George J. Brewer, and Craig
J. McClain
Kyle A. Rasbach and Rick G. Schnellmann
409
Patsy Clark, Steven E. Rowland,
Danielle Denis, Marie-Claude Mathieu,
Rino Stocco, Hugo Porrier, Jason Burch,
Yongxin Han, Laurent Audoly, Alex G.
Therien, and Daigen Xu
425
536
Prostaglandin I2 Plays a Key Role in Zymosan-Induced Mouse
Pleurisy
Koh-ichi Yuhki, Fumitaka Ushikubi,
Hiroaki Naraba, Akinori Ueno, Hirotsugu
Kato, Fumiaki Kojima, Shuh Narumiya,
Yukihiko Sugimoto, Misao Matsushita, and
Sachiko Oh-ishi
601
Relation between mRNA Expression Level of Muttidrug
Resistance 1/ABCB1 in Blood Cells and Required Level of
Tacrolimus in Pediatric Living-Donor Liver Transplantation
Maki Goto, Satohiro Masuda,
Tetsuya Kiuchi, Yasuhiro Ogura,
Fumitaka Oike, Koichi Tanaka,
Shinji Uemoto, and Ken-ichi Inui
610
Structural Requirements for Activation of the 5-Oxo6£,8Z,llZ,14Z-eicosatetraenoic Acid (5-Oxo-ETE) Receptor:
Identitication of a Mead Acid Metabolite with Potent Agonist
Activity
Pranav Patel, Chantal Cossette,
Jaganrnohan R. Anumolu, Sylvie Gravel,
Alain Lesimple, Orval A. Mamer, Joshua
Rokach, and William S. Powell
698
Jason M. Gow, Laura M. Hodges,
Leslie W. Chinn, and Deanna L. Kroetz
435
Yuji Tanaka, Lauren M. Aleksunes,
Ronnie L. Yeager, Maxwell A. Gyamfi,
Noriko Esterly, Grace L. Guo, and
Curtis D. Klaassen
655
Nobuko Matsumura, Kazue Kikuchi-Utsumi,
and Toshio Nakaki
357
Xavier Rovira, David Roche, Juan Serra,
Julie Kniazeff, Jean-Philippe Pin, and
Jesus Giraldo
443
Activation of Muscarinic Cholinergic Receptors on Human
SH-SY5Y Neuroblastoma Cells Enhances Both the Influx and
Efflux of K + under Conditions of Hypo-Osmolarity
Daniel J. Foster, Anne M. Heacock,
Richard F. Keep, and Stephen K. Fisher
457
Unexceptional Seizure Potential of Tramadol or Its
Enantiomers or Metabolites in Mice
Robert B. Raffa and Dennis J. Stone, Jr.
500
Delivery of Galanin-Like Peptide to the Brain: Targeting with
Intranasal Delivery and Cyclodextrins
Naoko Nonaka, Susan A. Fair,
Haruaki Kageyama, Selji Shioda, and
William A. Banks
513
Neurotensin in the Ventral Pallidum Increases Extracellular yAminobutyric Acid and Differentially Affects Cue- and
Cocaine-Primed Reinstatement
Mary M. Torregrossa and Peter W. Kalivas
556
William J. Thomsen, Andrew J. Grottick,
Frederique Menzaghi, Hazel Reyes-Saldana,
Stephen Espitia, Diane Yuskin,
Kevin Whelan, Michael Martin,
Michael Morgan, Weichao Chen,
Hussien Al-Shamma, Brian Smith,
Derek Chalmers, and Dominic Behan
577
j3-Phenylethylamine Alters Monoamine Transporter Function
via Trace Amine-Associated Receptor 1: Implication for
Modulatory Roles of Trace Amines in Brain
Zhihua Xie and Gregory M. Miller
617
Modulation of Monoamine Transporters by Common Biogenic
Amines via Trace Amine-Associated Receptor 1 and
Monoamine Autoreceptors in Human Embryonic Kidney 293
Cells and Brain Synaptosomes
Zhihua Xie, Susan V. Westmoreland, and
Gregory M. Miller
629
First in Vivo Evidence for a Functional Interaction between
Chemokine and Cannabinoid Systems in the Brain
Khalid Benamar, Ellen B. Geller, and
Martin W. Adler
641
Cotinine Selectively Activates a Subpopulation of «3/a6/32*
Nicotinic Receptors in Monkey Striatum
Kathryn O'Leary, Neeraja Parameswaran,
J. Michael Mclntosh, and Maryka Quik
646
Diclofenac Attenuates the Regional Effect of A-Carrageenan on
Blood-Brain Barrier Function and Cytoarchitecture
Tracy A. Brooks, Nicole Nametz,
Rachael Charles, and Thomas P. Davis
665
METABOLISM, TRANSPORT, AND PHARMACOGENOMICS
Substrate-Dependent Effects of Human ABCB1 Coding
Polymorphisms
[s] NF-E2-Related Factor 2 Inhibits Lipid Accumulation and
Oxidative Stress in Mice Fed a High-Fat Diet
NEUROPHARMACOLOGY
Activities of 7-Nitroindazole and l-(2-(TrifluoromethyIphenyl}imidazole Independent of Neuronal Nitric-Oxide Synthase
Inhibition
[sj Modeling the Binding and Function of Metabotropic
Glutamate Receptors
[s] Lorcaserin, a Novel Selective Human 5-Hydroxytryptamine3C
Agonist: in Vitro and in Vivo Pharmacological
Characterization
Preclinical Characterization of Selective Phosphodiesterase
10A Inhibitors: A New Therapeutic Approach to the
Treatment of Schizophrenia
TOXICOLOGY
Preclinical Toxicology (Subacute and Acute) and Efficacy of a
New SqualenoyI Gemcitabine Anticancer Nanomedicine
C. J. Schmidt, D. S. Chapin, J. Cianfrogna,
M. L. Corman, M. Hajos, J. F. Harms,
W. E. Hoffman, L. A. Lebel, S. A. McCarthy,
F. R. Nelson, C. Proulx-LaFrance,
M. J. Majchrzak, A. D. Ramirez, K. Schmidt,
P. A. Seymour, J. A. Siuciak,
F. D. Tingley HI, R. D. Williams,
P. R. Verhoest, and F. S. Menniti
681
L. Harivardhan Reddy, Pierre-Emmanuel
Marque, Catherine Dubernet, Sinda-Lepetre
Mouelhi, Didier Desmaele, and Patrick
Couvreur
484