The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
April 2005
Vol 313, No. 1
Contents
PERSPECTIVES IN PHARMACOLOGY
Ligand Discovery Using Small Molecule Microarrays
Xuezhong G. He,
Guillermo Gerona-Navarro, and
Sarnie R. Jaffrey
ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION
The Grapefruit Juice Effect Is Not Limited to Cytochrome
Hsia-lien Lin, Ute M. Kent, and
P450 (P450) 3A4: Evidence for Bergamottin-Dependent
Paul F. Hollenberg
Inactivation, Heme Destruction, and Covalent Binding to
Protein in P450s 2B6 and 3A5
Jim J. Xiao, Amy B. Foraker, Peter W.
Efflux of Depsipeptide FK228 (FR901228, NSC-630176) Is
Mediated by P-Glycoprotein and Multidrug ResistanceSwaan, Shujim Liu, Ying Huang, Zunyan
Associated Protein 1
Dai, Jiyun Chen, Wolfgang Sadee, John
Byrd, Guido Marcucci, and Kenneth K.
Chan
Recombinant CYP3A4*17 Is Defective in Metabolizing the
Su-Jun Lee, Douglas A. Bell,
Hypertensive Drug Nifedipine, and the CYP3A4*17 Allele May
Sherry J. Coulter, Burhan Ghanayem, and
Occur on the Same Chromosome as CYP3A5*3, Representing
Joyce A. Goldstein
a New Putative Defective CYP3A Haplotype
Lymphatic Absorption Is the Primary Contributor to the
Systemic Availability of Epoetin Alfa following Subcutaneous
Administration to Sheep
BEHAVIORAL PHARMACOLOGY
Intracranial Self-Administration of Cocaine within the
Posterior Ventral Tegmental Area of Wistar Rats: Evidence
for Involvement of Serotonin-3 Receptors and Dopamine
Neurons
Nociceptive Sensitivity and Opioid Antinociception and
Antihyperalgesia in Freund's Adjuvant-Induced Arthritic
Male and Female Rats
CARDIOVASCULAR
Vascular Dysfunction of Venous Bypass Conduits Is Mediated
by Reactive Oxygen Species in Diabetes: Role of Endothelin-1
154
268
302
Danielle N. McLennan, Christopher J. H.
Porter, Glenn A. Edwards, Steven W.
Martin, Anne C. Heatherington, and Susan
A. Charman
345
Zachary A. Rodd, Richard L. Bell,
Kelly A. Kuc, Ying Zhang,
James M. Murphy, and William J. McBride
134
Charles D. Cook and Michael D. Nickerson
449
Adviye Ergul, Jeanette Schultz Johansen,
Catherine Str0mhaug, Alex K. Harris,
Jimmie Hutchinson, Amany Tawfik, Ali
Rahimi, Edward Rhim, Bryan Wells, R.
William Caldwell. and Mark P. Anstadt
70
Bradykinin Down-Regulates, Whereas Arginine Analogs UpRegulate, Endothelial Nitric-Oxide Synthase Expression in
Coronary Endothelial Cells
N. D. Vaziri, Y. Ding, Z. Ni, and
C. H. Barton
121
Electrophysiological Effects of Prucalopride, a Novel
Enterokinetic Agent, on Isolated Atrial Myocytes from
Patients Treated with /3-Adrenoceptor Antagonists
Davide Pau, Antony J. Workman,
Kathleen A. Kane, and Andrew C. Rankin
146
Marcella Rocchetti, Alessandra Besana,
Gaspare Mostacciuolo, Rosclla Micheletti,
Patrizia Ferrari, Sandor Sarkozi, Csaba
Szegedi, Istvan Jona, and Antonio Zaza
207
Julien Hanson, Stephanie Rolin,
Denis Reynaud, Na Qiao, Leanne P. Kelley,
Helen M. Reid, Francois Valentin,
John Tippins, B. Therese Kinsella,
Bernard Masereel, Cecil Pace-Asciak,
Bernard Pirolte, and Jean-Michel Dogne
293
R. Miquel, R. Gisbert, E. Serna,
F. Perez-Vizcaino, E. Anselmi, M. A. Noguera,
M. D. Ivorra, and M. P. D'Ocon
359
Nicholas A. Flavahan
432
[s] Modulation of Sarcoplasmic Reticulum Function by Na +/K+
Pump Inhibitors with Different Toxicity: Digoxin and
PST2744 [(£,Z)-3-((2-Aminoethoxy)imino)androstane-6,17dione Hydrochloride]
In Vitro and in Vivo Pharmacological Characterization of BM6T3 [Ar-n-Pentyl-A"-[2-(4'-methylphenyIamino)-5nitrobenzenesulfonyl]urea], a Novel Dual Thromboxane
Synthase Inhibitor and Thromboxane Receptor Antagonist
Acute and Chronic Captopril, but Not Prazosin or Nifedipine,
Normalize Alterations in Adrenergic Intracellular Ca 2+
Handling Observed in the Mesenteric Arterial Tree of
Spontaneously Hypertensive Rats
Phenylpropanolamine Constricts Mouse and Human Blood
Vessels by Preferentially Activating a2-Adrenoceptors
CELLULAR AND MOLECULAR
Heterodimerization with J32-Adrenergic Receptors Promotes
Surface Expression and Functional Activity of a „,-Adrenergic
Receptors
A Novel Benzodiazepine Selectively Inhibits Keratinocyte
Proliferation and Reduces Retinoid-Induced Epidermal
Hyperplasia in Organ-Cultured Human Skin
A Highly Conserved Glycine within Linker I and the Extreme
C Terminus of G Protein a Summits Interact Cooperatively
in Switching G Protein-Coupled Receptor-to-Effector
Specificity
Suramin Disrupts Receptor-G Protein Coupling by Blocking
Association of G Protein a and fiy Subunits
Antagonist Efficacy in MORS196L Mutant Is Affected by the
Interaction between Transmembrane Domains of the Opioid
Receptor
BL-1249 [(5,6,7,8-Tetrahydro-naphthalen-l-yl)-[2-(m-tetrazol5-yl)-phenyl]-amine]: A Putative Potassium Channel Opener
with Bladder-Relaxant Properties
Inhibition of Tumor Growth, Angiogenesis, and Tumor Cell
Proliferation by a Small Molecule Inhibitor of c-Jun Nterminal Kinase
Asiatic Acid, a Triterpene, Induces Apoptosis and Cell Cycle
Arrest through Activation of Extracellular Signal-Regulated
Kinase and p38 Mitogen-Activated Protein Kinase Pathways
in Human Breast Cancer Cells
The M3 Muscarinic Receptor Mediates Contraction through
Indirect Mechanisms in Mouse Urinary Bladder
CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY
js] Trimers of iV-Alkylglycines Are Potent Modulators of the
Multidrug Resistance Phenotype
Michelle A. Uberti, Chris Hague,
Heide Oiler, Kenneth P. Minneman, and
Randy A. Hall
16
James Varani, Narasiraharao Bhagavathula,
Kamalakar C. Nerusu, Hilary Sherzer,
Kevin Fay, Anthony E. Boitano,
Gary D. Click, Kent Johnson, Sewon Kang,
and Anthony W. Opipari, Jr.
56
Evi Kostenis, Lene Martini, James Ellis,
Maria Waldhoer, Ame Heydorn,
Mette M. Rosenkilde, Pia K. Norregaard,
Rasmus Jorgensen, Jennifer L. Whistler, and
Graeme MilHgan
78
Wen-Cheng Chung and John C. Kermode
191
Patricia A. Claude-Geppert, Jiahui Liu,
Jonathan Solberg,
Laurie J. Erickson-Herbrandson,
Horace H. Loh, and Ping-Yee Law
216
Svetlana Tertyshnikova, Ronald J. Knox,
Mary Jane Plym, George Thalody,
Corinne Griffin, Torben Neelands,
David G. Harden, Laura Signor,
David Weaver, Robert A. Myers, and
Nicholas J. Lodge
Bruce W. Ennis, Kimberly E. Fultz,
Kent A. Smith, John K. Westwick, Dan Zhu,
Michael Boluro-Ajayi, Graham K. Bilter, and
Bernd Stein
Ya-Ling Hsu, Po-Lin Kuo, Liang-Tzung Lin,
and Chun-Chi ng Lin
250
325
333
Frederick J. Ehlert, Michael T. Griffin,
Diane M. Abe, Tran H. Vo,
Makoto M. Taketo, Toshiya Manabe, and
Minoru Matsui
368
Maria J. Abad-Merin, Nuria Cortes,
Isabel Masip, Enrique Perez-Paya, Jose
A. Ferragut, Angel Messeguer, and
Antonio Ferrer-Montiel
112
Free Exchange across Cells, and Echistatin-Sensitive
Membrane Target for the Metastasis Inhibitor NAMI-A
(Imidazolium trans -Imidazole Dimethyl Sulfoxide
Tetrachlororuthenate) on KB Tumor Cells
F. Frausin, V. Scarcia, M. Cocchietto,
A. Furlani, B. Serli, E. Alessio, and G. Sava
227
Michael F. Ethier, Erika Cappelluti, and
J. Mark Madison
127
Proximal Tubular Toxicity of Ochratoxin A Is Amplified by
Simultaneous Inhibition of the Extracellular Signal-Regulated
Kinases 1/2
C. Sauvant, H. Holzinger, and M. Gekle
234
Does Cyclic AMP Mediate Rat Urinary Bladder Relaxation by
Isoproterenol?
Elfaridah P. Frazier, Marie-Jeanne Mathy,
Stephan L. M. Peters, and Martin C. Michel
260
Involvement of Mast Cells in Adenosine-Mediated
Bronchoconstriction and Inflammation in an Allergic Mouse
Model
Peter J. Oldenburg and S. Jamai Mustafa
319
Shuang Mei, Wei Yao, Yuanjue Zhu, and
Jinyuan Zhao
379
Timo Ricg, Hannah Steigele,
Jurgen Schnermann, Kerstin Richter,
Hartmut Osswald, and Volker Vallon
403
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL
Mechanisms of Interleukin-4 Effects on Calcium Signaling in
Airway Smooth Muscle Cells
\s\ Protection of Pirfenidone against an Early Phase of Oleic
Acid-Induced Acute Lung Injury in Rats
Requirement of Intact Adenosine A, Receptors for the
Diuretic and Natriuretic Action of the Methylxanthines
Theophylline and Caffeine
INFLAMMATION AND IMMUNOPHARMACOLOGY
Therapeutic Dosing with Anti-Interleukin-13 Monoclonal
Antibody Inhibits Asthma Progression in Mice
Combination Therapy with an Angiotensin-Converting
Enzyme Inhibitor and an Angiotensin II Receptor Blocker
Synergistically Suppresses Chronic Pancreatitis in Rats
Effects of Prostaglandin D2, 15-Deoxy-A12'J4-prostaglandin J2,
and Selective DP^ and DP2 Receptor Agonists on Pulmonary
Infiltration of Eosinophils in Brown Norway Rats
Significance of CycIooxygenase-2 Induced via p38 MitogenActivated Protein Kinase in Mechanical Stimulus-Induced
Peritoneal Adhesion in Mice
Gaoyun Yang, Li Li, Amy Volk,
8
Eva Emmell, Ted Petley, Jill Giles-Komar,
Patricia Rafferty, Mani Lakshminarayanan,
Don E. Griswold, Peter J. Bugelski, and
Anuk M. Das
Tamaki Yamada, Atsushi Kuno,
Kumiko Ogawa, Mingxi Tang,
Kazuhiko Masuda, Soichi Nakamura,
Tomoaki Ando, Telsu Okamoto,
Hirotaka Ohara, Tomoyuki Nomura,
Takashi Joh, Tomoyuki Shirai, and
Makoto ftoh
Wagdi Almishri, Chantal Cossette,
Joshua Rokach, James G. Martin, Qulayba
Hamid, and William S. Powell
36
64
Jun Katada, Hitomi Saito, and Akira Ohashi
286
Carla F. Franco-Penteado,
Ivani A. De Souza, Enilton A. Camargo,
Simone A. Teixeira, Marcelo N. Muscara,
Gilberio De Nucci, and Edson Antunes
440
Mechanisms Involved in the Enhancement of Allergic Airways
Neutrophil Influx by Permanent C-Fiber Degeneration in Rats
NEUROPHARMACOLOGY
High-Affinity Epibatidine Binding of Functional, Human alNicotinic Acetylcholine Receptors Stably and Heterologously
Expressed de Novo in Human SH-EP1 Cells
Jian-Hong Peng. John D. Fryer,
Raymond S. Hurst, Katherine M. Schroeder,
Andrew A. George, Steven Morrissy,
Vincent E. Groppi, Sherry S. Leonard, and
Ronald J. Lukas
24
Involvement of Protein Kinase A in Cannabinoid ReceptorMediated Protection from Oxidative Neuronal Injury
Sun Hee Kim, Seok Joon Won,
Xiao Ou Mao, Kunlin Jin, and
David A. Greenberg
88
Pharmacological Properties of ABT-239
[4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyI}-benzofuran-5-yl)benzonitrile]:
I. Potent and Selective Histamine H3 Receptor Antagonist with DrugLike Properties
Timothy A. Esbenshade, Gerard B. Fox,
Kathleen M. Krueger, Thomas R. Miller,
Chae Hee Kang, Lynne I. Denny,
David G. Witte, Betty B. Yao, Liping Pan,
Jill Wetter, Kennan Marsh,
Youssef L. Bennani, Marlon D. Cowart,
James P. Sullivan, and Arthur A. Hancock
165
Pharmacological Properties of ABT-239
[4-(2-{24(2ff)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitriIe]:
n. Neurophysiological Characterization and Broad Preclinical Efficacy
in Cognition and Schizophrenia of a Potent and Selective Histamine H3
Receptor Antagonist
A Novel Selective Positive AUosteric Modulator of
Metabotropic Glutamate Receptor Subtype 5 Has in Vivo
Activity and Antipsychotic-Like Effects in Rat Behavioral
Models
Somatostatin-Induced Activation and Up-Regulation of NMethyl-D-aspartate Receptor Function: Mediation through
Calmodulin-Dependent Protein Kinase II, Phospholipase C,
Protein Kinase C, and Tyrosine Kinase in Hippocampal
Noradrenergic Nerve Endings
Positive a-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
(AMPA) Receptor Modulators Have Different Impact on
Synaptic Transmission in the Thalamus and Hippocampus
Antinociceptive Properties of Mixture of a-Amyrin and 6Amyrin Triterpenes: Evidence for Participation of Protein
Kinase C and Protein Kinase A Pathways
Characterization of the Fatty Acid Amide Hydrolase Inhibitor
Cyclohexyl Carbamic Acid 3 -Carbamoyl-biphenyl-3-yl Ester
(URB597): Effects on Anandamide and Oleoylethanolamide
Deactivation
The Dorsal Raphe Nucleus as a Site of Action of the
Antinociceptive and Behavioral Effects of the <x4 Nicotinic
Receptor Agonist Epibatidine
Metabotropic Glutamate Receptor mGlu5 Is a Mediator of
Appetite and Energy Balance in Rats and Mice
Inverse Agonism and Neutral Antagonism at Wild-Type and
Constitutively Active Mutant Delta Opioid Receptors
Induction Patterns of Transcription Factors of the Nur Family
(Nurrl, Nur77, and Nor-1) by Typical and Atypical
Antipsychotics in the Mouse Brain: Implication for Their
Mechanism of Action
Gerard B. Fox, Timothy A. Esbenshade, Jia
Bao Pan, Richard J. Radek, Kathleen M.
Krueger, Betty B. Yao, Kaitlin E. Browman,
Michael J. Buckley, Michael E. Ballard,
Victoria A. Komater, Holly Miner, Min
Zhang, Ramin Faghih, Lynne E. Rueter, R.
Scott Bitner, Karla U. Drescher, Jill Wetter,
Kennan Marsh, Marline Lemaire, Roger D.
Porsolt, Youssef L. Bennani, James P.
Sullivan, Marlon D. Cowart, Michael W.
Decker, and Arthur A. Hancock
Gene G. Kinney, Julie A. O'Brien,
Wei Lemaire, Maryann Burno,
Denise J. Bickel, Michelle K. Clements,
Tsing-Bau Chen, David D. Wisnoski,
Craig W. Lindsley, Philip R. Tiller,
Sheri Smith, Marlene A. Jacobson,
Cyrille Sur, Mark E. Duggan,
Douglas J. Pettibone, P. Jeffrey Conn, and
David L. Williams, Jr.
Anna Pittaluga, Marco Feligioni, Fabio
Longordo, Marica Arvigo, and Maurizio
Raiteri
Yan-Fang Xia, Markus Kessler, and
Amy C. Arai
Michel F. Otuki, Juliano Ferreira, Fabiana V.
Lima, Cristiane Meyre-Silva, Angela
Malheiros, Luciane A. Muller, Graziela S.
Cani, Adair R. S. Santos, Rosendo A. Yunes,
and Joao B. Calixto
Darren Fegley, Silvana Gaetani,
Andrea Duranti, Andrea Tontini, Marco Mor,
Giorgio Tarzia, and Daniele Piomelli
Giovanni Cucchiaro, Nayla Chaijale, and
Kathryn G. Commons
Margaret J. Bradbury, Una Campbell,
Darlene Giracello, Deborah Chapman, Chris
King, Lida Tehrani, Nicholas D. P. Cosford,
Jeff Anderson, Mark A. Varney, and Alison
M. Strack
P. Tryoen-Toth, F. M. Decaillot, D. Filliol, K.
Befort, L. H. Lazarus, P. W. Schiller, H.
Schmidhammer, and B. L. Kieffer
1,1-Dichloroethylene-Induced Mitochondrial Damage Precedes
Apoptotic Cell Death of Bronchiolar Epithelial Cells in
Murine Lung
199
242
277
310
352
389
395
410
Jerome Maheux, Isabelle Efhier, Claude
Rouillard, and Daniel Levesque
460
Narender R. Gavva, Rami Tamir, Yusheng
Qu, Lana Klionsky, T. J. Zhang, David
AMG 9810 [(£)-3-(4-f-Butylphenyl)-iV-(2,3Immke, Judy Wang, Dawn Zhu, Todd W.
dihydrobenzo[6][l,4]dioxin-6-yl)acrylamide], a Novel Vanilloid
Vanderah, Frank Porreca, Elizabeth M.
Receptor 1 (TRPV1) Antagonist with Antihyperalgesic Properties Doherty, Mark H. Norman, Kenneth D. Wild,
Anthony W. Bannon, Jean-Claude Louis, and
James J. S. Treanor
OXICOLOGY
Protein Kinase CS Is a Key Downstream Mediator of
Manganese-Induced Apoptosis in Dopaminergic Neuronal
Cells
176
474
Calivarathan Latchoumycandane,
Vellareddy Anantharam, Masashi Kitazawa,
Yongjie Yang, Arthi Kanthasamy, and
Anumantha G. Kanthasamy
46
Erik J. Martin and Poh-Gek Forkert
95
Role for Membrane Fluidity in Ethanol-Induced Oxidative
Stress of Primary Rat Hepatocytes
Serotonergic Neurotoxic Metabolites of Ecstasy Identified in
Rat Brain
Odile Sergent, Manuella Pereira, Corinne
Belhomme, Martine Chevanne, Laurence
Hue, and Dominique Lagadic-Gossmann
Douglas C. Jones, Christine Duvauchelle,
Aiko Ikegami, Christopher M. Olsen,
Serrine S. Lau, Rafael de la Torre, and
Terrence J. Monks
104
422