The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
Vol. 319, No. 2
November 2006
Contents
507
PERSPECTIVES IN PHARMACOLOGY
Preclinical Assessment of Candidate Analgesic Drugs: Recent
Advances and Future Challenges
S. S. Negus, T. W. Vanderah, M. R. Brandt, E. J.
Bilsfcy, L. Becerra, and D. Borsook
BEHAVIORAL PHARMACOLOGY
Effect of Duration and Pattern of Chronic Ethanol Exposure
on Tolerance to the Discriminative Stimulus Effects of
Ethanol in C57BL/6J Mice
Howard C. Becker and Alicia M. Baros
871
Nathalie Turle-Lorenzo, Beatrice Maurin, Carole
Puma, Claire Chezaubernard, Philippe
Morain, Christelle Baunez, Andre
Nieoullon, and Marianne Amalric
914
Sandra Donnini, Raffaella Solito, Antonio
Giachetti, Harris J. Granger, Marina Ziche,
and Lucia Morbidelli
515
Anastasia Pyriochou, Dimitris Beis,
Vasiliki Koika, Christos Potytarchou,
Evangelia Papadimitriou, Zongmin Zhou,
and Andreas Papapetropoulos
663
Role of Myocardial Nitric Oxide in Diabetic IschemiaReperfusion Dysfunction: Studies in Mice with MyocyteSpecific Overexpression of Endothelial Nitric-Oxide Synthase
Beatriz Pozo-Navas, Heike Stessel, Gerald
Wolkart, and Friedrich Brunner
729
Pharmacological Characterization of Novel a-Calcitonin
Gene-Related Peptide (CGRP) Receptor Peptide Antagonists
That Are Selective for Human CGRP Receptors
Christopher K. Taylor, D. David Smith,
Martin Hulce, and Peter W. Abel
749
The Serotonin 5-Hydroxytryptaphan,A Receptor Agonist, (+)8Hydroxy-2-(di-n-propylamino)-tetralin, Stimulates
Sympathetic-Dependent Increases in Venous Tone during
Hypovolemic Shock
Ruslan Tiniakov and Karie E. Scrogin
776
Enhanced Thromboxane Receptor-Mediated Responses and
Impaired Endothelium-Dependent Relaxation in Human
Corpus Cavernosum from Diabetic Impotent Men: Role of
Protein Kinase C Activity
Javier Angulo, Pedro Cuevas, Argentina
Fernandez, Antonio Allona, Ignacio
Moncada, Antonio Martin-Morales, Jose
Maria La Fuente, and lingo Saenz de
Tejada
783
Properties of a Time-Dependent Potassium Current in Pig
Atrium: Evidence for a Role of K ¥1.5 in Repolarization
Joachim R. Ehrlich, Christin Hoche, Pierre
Coutu, Christiane Metz-Weidmann, Werner
Dittrich, Stefan H. Hohnloser, Stanley
Nattel, and Heinz Gb'gelein
The Dopamine Agonist Piribedil with L-DOPA Improves
Attentional Dysfunction: Relevance for Parkinson's Disease
CARDIOVASCULAR
Fibroblast Growth Factor-2 Mediates Angiotensin-Converting
Enzyme Inhibitor-Induced Angiogenesis in Coronary
Endothelium
\sj Soluble Guanylyl Cyclase Activation Promotes Angiogenesis
CELLULAR AND MOLECULAR
Valproic Acid Inhibits Invasiveness in Bladder Cancer but
Not in Prostate Cancer Cells
Chien-Lun Chen, Jennifer Sung,
Michael Cohen, Wasim H. Chowdhury,
Markus D. Sachs, Ying Li,
Yegappan Lakshmanan,
Benjamin Y. M. Yung, Shawn E. Lupold,
and Ronald Rodriguez
533
Busulfan Selectively Induces Cellular Senescence but Not
Apoptosis in WI38 Fibroblasts via a p53-Independent but
Extracellular Signal-Regulated Kinase-p38 Mitogen-Activated
Protein Kinase-Dependent Mechanism
Virginia Probin, Yong Wang, Aiping Bai,
and Daohong Zhou
551
Nitric Oxide Production by the Vacuolar-Type (H+)-ATPase
Inhibitors Bafilomycin Al and Concanamycin A and Its
Possible Role in Apoptosis in RAW 264.7 Cells
JangJa Hong, Yasuhiro Nakano,
Aya Yokomakura, Kenji Ishihara,
Soonjoo Kim, Young-Sook Kang, and
Kazuo Ohuchi
672
Determining the Potency and Molecular Mechanism of Action
of Insurmountable Antagonists
Terry Kenakin, Stephen Jenkinson, and
Christian Watson
710
Tethered Yohimbine Analogs as Selective Human a2CAdrenergic Receptor Ligands
Supriya A. Bavadekar, Guoyi Ma,
Suni M. Mustafa, Bob M. Moore,
Duane D. Miller, and Dennis R. Feller
Vicenta Salvador-Recatala, Yonjung Kim,
Elena Zaks-Makhina, and Edwin S. Levitan
739
Yong Chen, Chongguang Chen, Yulin Wang,
and Lee-Yuan Liu-Chen
765
Rodolfo Bianchini, Giuseppe Nocentini,
Ludovic Tibor Krausz, Kalia Fettucciari,
Stefano Coaccioli, Simona Ronchetti, and
Carlo Riccardi
887
Mallotoxin Is a Novel Human Ether-a-go-go -Related Gene
(hERG) Potassium Channel Activator
Haoyu Zeng, Irina M. Lozinskaya,
Zuojim Lin, Robert N. Willette,
David P. Brooks, and Xiaoping Xu
957
Prostanoid Receptors Regulate the Volume-Sensitive Efflux of
Osmolytes from Murine Fibroblasts via a Cyclic AMPDependent Mechanism
Anne M. Heacock, Daniel J. Foster, and
Stephen K. Fisher
963
Pal K. Selbo, Anette Weyergang,
Anette Bonsted. Stephen G. Bown, and
Kristian Berg
604
H. Alec Ross, Petra J. van Gurp,
Jacques J. Willemsen,
Jacques W. M. Lenders, Cecs J. Tack, and
Fred C. G. J. Sweep
840
Carolin Daniel, Heinfried H. Radeke,
Nico A. Sartory, Nadine Zahn,
Ulrich Zuegel, Andreas Steinmeyer, and
Jiirgen Stein
622
Renoprotective Effects of /-Carnosine on Ischemia/
Reperfusion-Induced Renal Injury in Rats
Hayato Kurata, Toshihide Fujii,
Hidenobu Tsutsui, Tomoaki Katayama,
Mamoru Ohkita, Masanori Takaoka,
Nobuo Tsuruoka, Yoshinobu Kiso,
Yukihiro Ohno, Yoshihide Fujisawa,
Takatoshi Shokoji, Akira Nishiyaraa,
Youichi Abe, and Yasuo Matsumura
640
Role of Cyclooxygenase Isoforms and Nitric-Oxide Synthase in
the Modulation of Tracheal Motor Responsiveness in Normal
and Antigen-Sensitized Guinea Pigs
Paola Nieri, Cinzia Martinelli,
Corrado Blandizzi, Nunzia Bernardini,
Rosamiria Greco, Chiara Ippolito,
Mario Del Tacca, and Maria Cristina Breschi
648
Melatonin Treatment Reverts Age-Related Changes in Guinea
Pig Gallbladder Neuromuscular Transmission and
Contractility
Pedro J. Gomez-Pinilla,
Cristina Camello-Almaraz, Rosario Moreno,
Pedro J. Camello, and Maria J. Pozo
847
Voltage-Gated K+ Channel Block by Catechol Derivatives:
Defining Nonselective and Selective Pharmacophores
Ligands Regulate Cell Surface Level of the Human K Opioid
Receptor by Activation-Induced Down-Regulation and
Pharmacological Chaperone-Mediated Enhancement:
Differential Effects of Nonpeptide and Peptide Agonists
H] Modulation of Pro- and Antiapoptotic Molecules in DoublePositive (CD4+CD8+) Thymocytes following Dexamethasone
Treatment
CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY
Photochemical Internalization of Therapeutic Macromolecular
Agents: A Novel Strategy to Kill Multidrug-Resistant Cancer
Cells
ENDOCRINE AND DIABETES
Transport within the Interstitial Space, Rather Than
Membrane Permeability, Determines Norepinephrine
Recovery in Microdialysis
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL
The New Low Calcemic Vitamin D Analog 22-Ene-25-OxaVitamin D Prominently Ameliorates T Helper Cell Type 1Mediated Colitis in Mice
758
Identification of Bombesin Receptor Subtype-Specific Ligands:
Effect of iV-Methyl Scanning, Truncation, Substitution, and
Evaluation of Putative Reported Selective Ligands
Samuel A. Mantey, Nieves Gonzalez,
Michael Schumann, Tapas K. Pradhan,
Lin Shen, David H. Coy, and Robert
T. Jensen
980
Sum Yee Leung, Akio Niimi, Alistair Noble,
Timothy Oates, Alison S. Williams,
Satyanarayana Medicherla,
Andrew A. Protter, and Kian Fan Chung
586
Yun-Feng Fu, Yi-Na Zhu, Jia Ni,
Xiang-Gen Zhong, Wei Tang, Yu-Dan Re,
Li-Ping Shi, Jin Wan, Yi-Fu Yang,
Chong Yuan, Fa-Jun Nan, Brian R. Lawson,
and Jian-Ping Zuo
799
Soledad Negrotto, Elisa Malaver,
Marfa Eugenia Alvarez, Natalia Pacienza,
Lina Paola D'Atri, Roberto Gabriel Pozner,
Ricardo Martfn Gomez, and Mirta Schattner
972
Andrea Gaedigk, Darren W. Baker,
Rheem A. Totah, Roger Gaedigk,
Robin E. Pearce, Carrie A. Vyhlidal,
Darryl C. Zeldin, and J. Steven Leeder
Elisabet Gullberg, Asa V. Keita,
Sa'ad Y. Salim, Margaretha Andersson, Karin D.
Caldwell, Johan D. Soderholm, and Per
Artursson
523
Nuclear Trafficking of a Gadolinium Conjugate in Nude Mice
Xenografted with Human LN-229 Glioma
Stefan Heckl and Ulrich Vogel
657
Induction of Human CYP2A6 Is Mediated by the Pregnane X
Receptor with Peroxisome Proliferator-Activated Receptor-y
Coactivator la
Masahiro Itoh, Miki Nakajima,
Eriko Higashi, Ryoko Yoshida, Kiyoshi
Nagata, Yasushi Yamazoe, and
Tsuyoshi Yokoi
693
iV-Acetyltransferase (Nat) 1 and 2 Expression in Nat2
Knockout Mice
Jennifer A. Loehle, Valerie Cornish,
Larissa Wakefield, Mark A. Doll,
Jason R. Neale, Yu Zang, Edith Sim, and
David W. Hein
724
Molecular Determinants in the Transport of a Bile AcidDerived Diagnostic Agent in Tumoral and Nontumoral Cell
Lines of Human Liver
Antonin Libra, Cristina Fernetti,
Vito Lorusso, Massimo Visigalli, Pier
Lucio Anelli, Frantisek Staud, Claudio
Tiribelli, and Lorella Pascolo
809
Increased Estrogen Sulfation of Estradiol 17j3-D-Glucuronide in
Metastatic Tumor Rat Livers
Huadong Sun, Lichuan Liu, and
K. Sandy Pang
818
Elucidating the Effect of Final-Day Dosing of Rifampin in
Induction Studies on Hepatic Drug Disposition and
Metabolism
Cisplatin and Oxaliplatin, but Not Carboplatin and
Nedaplatin, Are Substrates for Human Organic Cation
Transporters (SLC22A1-3 and Multidrug and Toxin
Extrusion Family)
Justine L. Lam, Sarah B. Shugarts,
Hideaki Okochi, and Leslie Z. Benet
864
Atsushi Yonezawa, Satohiro Masuda,
Sachiko Yokoo, Toshiya Katsura, and
Ken-ichi Inui
879
Effects of Trimethoprim on the Clearance of Apricitabine, a
Deoxycytidine Analog Reverse Transcriptase Inhibitor, and
Lamivudine in the Isolated Perfused Rat Kidney
Tomoko Nakalani-Freshwater,
Mariana Babayeva, Aruna Dontabhaktuni, and
David R. Taft
941
Marianna E. Jung, Andrew M. Wilson, and
James W. Simpkins
543
Bertha K. Madras, Zhihua Xie,
Zhicheng Lin, Amy Jassen, Helen Panas,
Laurie Lynch, Ryan Johnson, Eli Livni,
Thomas J. Spencer, Ali A. Bonab, Gregory
M. Miller, and Alan J. Fischman
561
INFLAMMATION, IMMUNOPHARMACOLOGY, AND ASTHMA
Effect of Transforming Growth Factor-/? Receptor I Kinase
Inhibitor 2,4-Disubstituted Pteridine (SD-208) in Chronic
Allergic Airway Inflammation and Remodeling
\s\ A Reversible S-Adenosyl-L-Homocysteine Hydrolase Inhibitor
Ameliorates Experimental Autoimmune Encephalomyelitis by
Inhibiting T Cell Activation
Aspirin and Salicylate Suppress Polymorphonuclear Apoptosis
Delay Mediated by Proinflammatory Stimuli
METABOLISM, TRANSPORT, AND PHARMACOGENOMICS
Variability of CYP2J2 Expression in Human Fetal Tissues
Identification of Cell Adhesion Molecules in the Human
Follicle-Associated Epithelium That Improve Nanoparticle
Uptake into the Peyer's Patches
NEUROPHARMACOLOGY
A Nonferainizing Estrogen Analog Protects against Ethanol
Withdrawal Toxicity in Immortalized Hippocampal Cells
Modafinil Occupies Dopamine and Norepinephrine
Transporters in Vivo and Modulates the Transporters and
Trace Amine Activity in Vitro
632
Dopamine Transporter (DAT) Inhibitors Alleviate Specific
Parkinsonian Deficits in Monkeys: Association with DAT
Occupancy in Vivo
Bertha K. Madras, Michele A. Fahey,
Martin Goulet, Zhicheng Lin, Jacob Bendor,
Claudia Goodrich, Peter C. Meltzer, David
R. Elmaleh, Eli Livni, Ali A. Bonab, and
Alan J. Fisehman
570
Pituitary Adenylate Cyclase-Activating Polypeptide (PACAP)
38 and PACAP4-6 Are Neuroprotective through Inhibition of
NADPH Oxidase: Potent Regulators of Microglia-Mediated
Oxidative Stress
Sufen Yang, Jun Yang, Zhengqin Yang,
Posee Chen, Alison Fraser, Wei Zhang, Hao
Pang, Xi Gao, Belinda Wilson, Jau-Shyong
Hong, and Michelle L. Block
595
Mechanism-Based Pharniacokinetic-Pharmacodynamic
Modeling of the Respiratory-Depressant Effect of
Buprenorphine and Fentanyl in Rats
The Mechanism of Carbamazepine Aggravation of Absence
Seizures
Ashraf Yassen, Jingmin Kan, Erik Olofsen,
Ernst Suidgeest, Albert Dahan, and
Meindert Danhof
682
Lige Liu, Thomas Zheng,
Margaret J. Morris, Charlolt Wallengren,
Alison L. Clarke, Christopher A. Reid,
Steven Petrou, and Terence J. O'Brien
790
Effects of Glycogen Synthase Kinase 3/3 and CyclinDependent Kinase 5 Inhibitors on Morphine-Induced
Analgesia and Tolerance in Rats
Jan Rodriguez Parkitna, Ilona Obara,
Agnieszka Wawrzczak-Bargiela,
Wioletta Makuch, Barbara Przewlocka, and
Ryszard Przewlocki
832
Effects of Prenatal Ethanol Exposure on the Excitability of
Ventral Tegmental Area Dopamine Neurons in Vitro
Functional Selectivity of NKX Receptor Signaling: Peptide
Agonists Can Preferentially Produce Receptor Activation or
Desensitization
Jue Wang, Samir Haj-Dahmane, and
Roh-Yu Shen
857
Mark A. Simmons
907
Concentration-Dependent Modulation of Amyloid-|3 in Vivo
and in Vitro Using the 7-Secretase Inhibitor, LY-450139
Thomas A. Lanz, Michael J. Karmilowicz,
Kathleen M. Wood, Nikolay Pozdnyakov,
Ping Du,Mary A. Piotrowski,
Tracy M. Brown, Charles E. Nolan,
Karl E. G. Richter, James E. Finley,
Qing Fei, Charles F. Ebbinghaus,
Yuhpyng L. Chen, Douglas K. Spracklin,
Barbara Tate, Kieran F. Geoghegan,
Lit-Fui Lau, David D. Auperin, and
Joel B. Schachter
924
Jin Yan and Barbara F. Hales
613
Paul S. Fitzmaurice, Junchao Tong,
Mehrdad Yazdanpanah, Peter P. Liu,
Kathryn S. Kalasinsky, and Stephen J. Kish
Kevyn E. Merten, Youchun Jiang,
Wenke Feng, and Y. James Kang
703
Christy C. Bridges and Rudolfs K. Zalups
948
TOXICOLOGY
Depletion of Glutathione Induces 4-Hydroxynonenal Protein
Adducts and Hydroxyurea Teratogenicity in the
Organogenesis Stage Mouse Embryo
Levels of 4-Hydroxynonenal and Malondialdehyde Are
Increased in Brain of Human Chronic Users of
Methamphetamine
Calcineurin Activation Is Not Necessary for DoxorubicinInduced Hypertrophy in H9c2 Embryonic Rat Cardiac Cells:
Involvement of the Phosphoinositide 3-Kinase-Akt Pathway
System B°'+ and the Transport of Thiol-S-Conjugates of
Methylmercury
934