The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
Vol. 315, No. 1
October 2005
Contents
PERSPECTIVES IN PHARMACOLOGY
Acetaminophen and the Cyclooxygenase-3 Puzzle: Sorting out
Facts, Fictions, and Uncertainties
Bela Kis, James A. Snipes, and
David W. Busija
ABSORPTION, DISTRIBUTION, METABOLISM, AND
EXCRETION Uptake of L-Carnitine and Its Short-Chain Ester
Propionyl-L-carnitine in the Isolated Perfused Rat Liver
Angelo Mancinelli, Allan M. Evans,
Roger L. Nation, and Antonio Longo
Multiple Components of 2,4-Dichlorophenoxyacetic Acid Uptake by Simon Lowes, Destiny Sykes,
Christopher M. Breen, Leigh J. Ragone, and
Rat Choroid Plexus
David S. Miller
Distribution of the Novel Antifolate Pemetrexed to the Brain
Haiqing Dai, Ying Chen, and
William F. Elmquist
Scott M. Ocheltree, Hong Shen,
Role and Relevance of Peptide Transporter 2 (PEPT2) in the
Kidney and Choroid Plexus: In Vivo Studies with Glycylsarcosine Yongjun Hu, Richard F. Keep, and
David E. Smith
in Wild-Type and PEPT2 Knockout Mice
Krzysztof
L Reszka, Laura H. Britigan, and
Oxidation of Anthracyclines by Peroxidase Metabolites of Salicylic
Bradley
E.
Britigan
Acid
Harunobu Tahara, Hiroyuki Kusuhara,
A Species Difference in the Transport Activities of H 2 Receptor
Antagonists by Rat and Human Renal Organic Anion and Cation Hitoshi Endou, Hermann Koepsell,
Tomoki Imaoka, Eiichi Fuse, and
Transporters
Yuichi Sugiyama
118
136
222
240
283
337
Influence of Atorvastatin on Apolipoprotein E and AI Kinetics in
Patients with Type 2 Diabetes
K. Bach-Ngohou, K. Ouguerram, R. Frenais,
P. Maugere, B. Ripolies-Piquer, Y. Zair, M.
Exempt", and J. M. Bard
363
Vascular Binding, Blood Flow, Transporter, and Enzyme
Interactions on the Processing of Digoxin in Rat Liver
Lichuan Liu, Ernie Mak, Rommel G. Tirona,
Eugene Tan, Phyllis M. Novikoff, Pijun
Wang, Allan W. Wolkoff, and K. Sandy
Pang
433
Becky Kinkead, Paul R. Dobner,
Vasili Egnatashvjli, Tiesha Murray,
Nancy Deitemeyer, and Charles B. Nemeroff
256
Rajeev I. Desai, Theresa A. Kopajtic,
Dawn French, Amy H. Newman, and
Jonathan L. Katz
397
BEHAVIORAL PHARMACOLOGY
Neurotensin-Deficient Mice Have Deficits in Prepulse
Inhibition: Restoration by Clozapine but Not Haloperidol,
Olanzapine, or Quetiapine
Relationship between in Vivo Occupancy at the Dopamine
Transporter and Behavioral Effects of Cocaine, GBR 12909
[1 - {2- [Bis- (4-fluoropheny l)methoxy ]ethyl} -4-(3phenylpropyl)piperazine], and Benztropine Analogs
Differential Behavioral Tolerance to the o"-Opioid Agonist
SNC80 ([(+)-4-[(«ff)-tt-[(2S,5ff)-2,5-Dimethyl-4-(2-propenyl)-lpiperazinyl]-(3-methoxyphenyl)methyI]-AyV-diethylbenzamide)
in Sprague-Dawley Rats
Emily M. Jutkiewicz, Sarah T. Kaminsky,
Kenner C. Rice, John R. Traynor, and
James H. Woods
414
Effects of the Competitive iV-Methyl-D-aspartate Receptor
Antagonist, LY2359S9 [(—)-6-Phosphonomethyl-decahydroisoquinoline-3-carboxylic Acid], on Responding for
Cocaine under Both Fixed and Progressive Ratio Schedules of
Reinforcement
Richard M. Allen, Regina M. Carelli, Linda
A. Dykstra, Therese L. Suchey, and Carson
V. Everett
449
CARDIOVASCULAR
Mechanisms Underlying the Effects of the Pyrethroid
Tefluthrin on Action Potential Duration in Isolated Rat
Ventricular Myocytes
Early and Sustained Inhibition of Nuclear Factor-KB Prevents
Hypertension in Spontaneously Hypertensive Rats
The Role of Akt and Mitogen-Activated Protein Kinase
Systems in the Protective Effect of Poly(ADP-Ribose)
Polymerase Inhibition in Langendorff Perfused and in
Isoproterenol-Damaged Rat Hearts
\s\ Calcium Channel Blocker Inhibits Western-Type Diet-Evoked
Atherosclerosis Development in ApoE-Deficient Mice
CELLULAR AND MOLECULAR
Transfection of Cytochrome P4504B1 into the Cornea
Increases Angiogenic Activity of the Limbal Vessels
Potentiation of P2X1 ATP-Gated Currents by 5Hydroxytryptamine 2A Receptors Involves DiacylglycerolDependent Kinases and Intracellular Calcium
C. Ian Spencer and James S. K. Sham
16
Bernardo Rodriguez-Iturbe, Atilio Ferrebuz,
Valentina Vanegas, Yasmir Quiroz, Sergio
Mezzano, and Nosratola D. Vaziri
51
Anita PaTfi, Arnbrus Tolh, Gyozo Kulcsar,
Katalin Hanto, Peter Deres, Eva Bartha,
Robert Halmosi, Eszter Szabados, Laszlo
Czopf, Tamas Kalai, Kalman Hideg, Balazs
Siimegi, and Kalman Toth
273
Jan Kyselovic, Peter Marlinka, Zuzana
Batova, Andrea Gazova, and Theophile
Godfraind
320
Alexandre Mezentsev, Vladimir Maslyugin,
Francesea Seta, Silvia Ashkar, Rowena
Kemp, D. Sudarshan Reddy, John R. Falck,
Michael W. Dunn, and Michal LaniadoSchwartzman
Ariel R. Ase, Ramin Raouf, Danny
Belanger, Edith Hamel, and
Philippe Seguela
42
144
Proerectile Effects of the Rho-Kinase Inhibitor (S)-(+)-2Methyl-l-[(4-methyI-5-isoquinolinyI)suIfonyl]homopiperazine
(H-1152) in the Rat Penis
Cleber E. Teixeira, Zhekang Ying, and
R. Clinton Webb
155
Acetoacetate Induces CYP2E1 Protein and Suppresses
CYP2E1 mRNA in Primary Cultured Rat Hepatocytes
Mobamed A. Abdclmegeed,
Nicholas J. Carruthers,
Kimberley J. Woodcroft, Sang K. Kim, and
Raymond F. Novak
203
Chronic Morphine Up-Regulates Gall and Cytoskeletal
Proteins in Chinese Hamster Ovary Cells Expressing the
Cloned jx Opioid Receptor
Heng Xu, Xiaoying Wang, Darin
Zimmerman, Emily S. Boja, Jiabei
Wang, Edward J. Bilsky, and Richard
B. Rothman
248
Persistent Binding and Functional Antagonism by Xanomeline
at the Muscarinic M5 Receptor
Marianne K. O. Grant and
Esam E. El-Fakahany
313
Identification of Molecular Targets of the Oligomeric
Nonprenylated Acylphloroglucinols from Myrtus communis and
Their Implication as Anti-Inflammatory Compounds
Christian FeiBt, Lutz Franke, Giovanni
Appendino, and Oliver Werz
389
Gina E. Avila, Xi Zheng, Xiao Xing Cui,
Amanda D. Ryan, Annette Hansson,
Junghan Suh, Arnold B. Rabson, Richard
L. Chang, Weichung Joe Shih, Yong Lin,
Pamela Crowell, Yao Ping Lu, You Rong
Lou, and Allan H. Conney
170
Jordi Martinez, Antonio Gutierrez, Jesus
Casas, Victoria Llado, Alicia Lopez-BeHan,
Joan Besalduch, Ana Dopazo, and Pablo V.
Escriba
466
Juhyun Kim, Di Wu, Dong Jin Hwang,
Duane D. Miller, and James T. Dalton
230
CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY
Inhibitory Effects of 12-0-Tetradecanoylphorbol-13-acetate
Alone or in Combination with KW-trans Retinoic Acid on the
Growth of Cultured Human Pancreas Cancer Cells and
Pancreas Tumor Xenografts in Immunodeficient Mice
The Repression of E2F-1 Is Critical for the Activity of
Minerval against Cancer
ENDOCRINE AND DIABETES
The Para Substituent of S-3-(Phenoxy)-2-hydroxy-2-methyl-A'(4-nitro-3-trifluoromethyl-phenyl)-propionamides Is a Major
Structural Determinant of in Vivo Disposition and Activity of
Selective Androgen Receptor Modulators
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL
Modification of Heat Shock Protein 90 by 4-Hydroxynonenal
in a Rat Model of Chronic Alcoholic Liver Disease
Proapoptotic Effect on Normal and Tumor Intestinal Cells of
Cytostatic Drugs with Enterohepatic Organotropism
Cross-Talk between Farnesoid-X-Receptor (FXR) and
Peroxisome Proliferator-Activated Receptor y Contributes to
the Antifibrotic Activity of FXR Ligands in Rodent Models of
Liver Cirrhosis
A Novel A, Adenosine Receptor Antagonist, L-97-1 [3-[2-(4Aminopheny l)-ethy l]-8-benzy I-7-{ 2-ethyl-(2-hydroxy-ethyl)amino]-ethyl}-l-propyl-3,7-dihydro-purine-2,6-dione], Reduces
Allergic Responses to House Dust Mite in an Allergic Rabbit
Model of Asthma
Development of Simplified Vasoactive Intestinal Peptide
Analogs with Receptor Selectivity and Stability for Human
Vasoactive Intestinal Peptide/Pituitary Adenylate CyclaseActivating Polypeptide Receptors
Mechanisms Underlying Capsaicin-Sthnulated HCOJ
Secretion in the Stomach: Comparison with Mucosal
Acidification
Inhibition of Nitric-Oxide Synthase Enhances Antigen-Induced
Contractions and Increases Release of Cysteinyl-Leukotrienes
in Guinea Pig Lung Parenchyma: Nitric Oxide as a Protective
Factor
INFLAMMATION AND IMMUNOPHARMACOLOGY
A-770041, a Novel and Selective Small-Molecule Inhibitor of
Lck, Prevents Heart Allograft Rejection
Nanoparticles Enhance Therapeutic Efficiency by Selectively
Increased Local Drug Dose in Experimental Colitis in Rats
Collagen and Aggrecan Degradation Is Blocked in Interleukinl-Treated Cartilage Explants by an Inhibitor of IKB Kinase
through Suppression of Metalloproteinase Expression
NEUROPHARMACOLOGY
Measurement of the Proportion of D2 Receptors Configured in
State of High Affinity for Agonists in Vivo: A Positron
Emission Tomography Study Using [11C]A'-Propylnorapomorphine and ["C]Raclopride in Baboons
Evidence for the Existence of an Additional Class of
Neuropeptide Y Receptor Sites in Rat Brain
Differential Effects of the 5-Hydroxytryptamine (5-HT)1A
Receptor Inverse Agonists Rec 27/0224 and Rec 27/0074 on
Electrophysiological Responses to 5-HT,A Receptor Activation
in Rat Dorsal Raphe Nucleus and Hippocampus in Vitro
Modulation of W-Methyl-D-aspartate Receptors by Donepezil in
Rat Cortical Neurons
Radioligand Binding Properties and Pharmacological
Characterization of 6-Amino-iV-cyclohexyl-A',3dimethylthiazolo[3,2-«]benzimidazole-2-carboxamide (YM298198), a High-Affinity, Selective, and Noncompetitive
Antagonist of Metabotropic Ghitamate Receptor Type 1
The Histaminergic Signaling System Exerts a Neuroprotective
Role against Neurodegenerative-Induced Processes in the
Hamster
David L. Carbone, Jonathan A. Doom,
Zachary Kiebler, Brian R. Ickes, and
Dennis R. Petersen
Maria J. Monte, Maria R. Ballestero,
Oscar Briz, Maria J. Perez, and
Jose J. G. Marin
Stefano Fiorucci, Giovanni Rizzo,
Elisabetta Antonelli, Barbara Renga,
Andrea Mencarelli, Luisa Riccardi,
Antonio Morelli, Mark Pruzanski, and
Roberto Pellicciari
P. C. M. Obiefuna, V. K. Batra, A. Nadeem,
P. Borron, C. N. Wilson, and S.
Jamal Mustafa
8
24
58
329
Hisato Igarashi, Tetsuhide Ito,
Samuel A. Mantey, Tapas K. Pradhan,
Wei Hou, David H. Coy, and Robert T.
Jensen
370
Eitaro Aihara, Masamune Hayashi,
Yoko Sasaki, Atsushi Kobata, and Koji
Takeuchi
423
Anna-Karin Larsson, Magnus Back,
Josephine Hjoberg, and Sven-Erik Dahlen
458
Robert F. Stachlewitz, Michelle A. Hart,
Brian Bettencourt, Tegest Kebede, Annette
Schwartz, Sheldon E. Ratnofsky, David J.
Caldcrwood, Wendy O. Waegell, and Gavin
C. Hirst
Alf Lamprecht, Hirornitsu Yamamoto,
Hirofumi Takeuchi, and
Yoshiaki Kawashima
Mark A. Pattoli, John F. MacMaster,
Kurt R. Gregor, and James R. Burke
36
196
382
Rajesh Narendran, Dah-Ren Hwang,
Mark Slifstein, Yuying Hwang,
Yiyun Huang, Jesper Ekelund,
Olivier Guillin, Erica Scher, Diana Martinet,
and Marc Laruelle
80
Yvan Dumont, Emmanuel Moyse,
Alain Foumier, and Remi Quirion
99
Renato Corradetti, Boris Mlinar,
Chiara Falsini, Anna Maria Pugliese,
Antonio Cilia, Carla Destefani, and
Rodolfo Testa
109
Shigeki Moriguchi, Xilong Zhao,
William Marszalec, Jay Z. Yeh, and
Toshio Narahashi
125
Atsuyuki Kohara, Takashi Toya,
Seiji Tamura, Tomonari Watabiki, Yukinori
Nagakura, Yoshitsugu Shitaka, Satoshi
Hayashibe, Shigeki Kawabata, and Masamichi
Okada
Marcello Canonaco, Maria Madeo,
Raffaella A16, Giuseppina Giusi,
Teresa Granata, Antonio Carelli,
Alessia Canonaco, and Rosa Maria Facciolo
163
188
G-Protein Activation by Neurokinin-1 Receptors Is
Dynamically Regulated during Persistent Nociception
Michelle K. Winter and
Kenneth E. McCarson
214
Contrasting Contribution of 5-Hydroxytryptamine 1A
Receptor Activation to Neurochemical Profile of Novel
Antipsychotics: Frontocortical Dopamine and Hippocampal
Serotonin Release in Rat Brain
Progress toward Acetate Supplementation Therapy for
Canavan Disease: Glyceryl Triacetate Administration
Increases Acetate, but Not A'-Acetylaspartate, Levels in Brain
Marie-Bernadette Assie, Veronique Ravailhe,
Valerie Faucillon, and
Adrian Newman-Tancredi
265
Raji Mathew, Peethambaran Arun,
Chikkathur N. Madhavarao, John R. Moffett, and
M. A. Aryan Namboodiri
297
Petrine Wellendorph, Signe H0g,
Jeremy R. Greenwood, Anne de Lichtenberg,
Birgitte Nielsen, Bente Fr0lund, Lotte Brehm,
Rasmus P. Clausen, and Hans Brauner-Osborne
346
Shi-Bing Yang, Felix Major, Lutz F. Tietze,
and Marjan Rupnik
352
Kristen K. Ford, Michete Matchett,
James E. Krause, and Weifeng Yu
405
Novel Cyclic y-Hydroxybutyrate (GHB) Analogs with High
Affinity and Stereoselectivity of Binding to GHB Sites in Rat
Brain
Block of Delayed-Rectifier Potassium Channels by Reduced
Haloperidol and Related Compounds in Mouse Cortical
Neurons
The P2X3 Antagonist P\ P5-Di[inosine-5] Pentaphosphate
Binds to the Desensitized State of the Receptor in Rat Dorsal
Root Ganglion Neurons
TOXICOLOGY
Dieldrin Induces Ubiquitin-Proteasome Dysfunction in aSynuclein Overexpressing Dopaminergic Neuronal Cells and
Enhances Susceptibility to Apoptotic Cell Death
Amphetamine Treatment Similar to That Used in the
Treatment of Adult Attention-Deficit/Hyperactivity Disorder
Damages Dopaminergic Nerve Endings in the Striatum of
Adult Nonhuman Primates
Involvement of Na+-Ca2+ Exchanger in Intracellular Ca2+
Increase and Neuronal Injury Induced by Polychlorinated
Biphenyls in Human Neuroblastoma SH-SY5Y Cells
Faneng Sun, Vellareddy Anantharam,
Calivarathan Latchou mycandane,
Arthi Kanthasamy, and Anumantha
G. Kanthasamy
69
George A. Ricaurte, Annis O. Mechan,
Jie Yuan, George Hatzidimitriou, Tao Xie,
Andrew H. Mayne, and Una D. McCann
91
Simona Magi, Pasqualina Castaldo,
Giuseppina Carrieri, Antonella Scorziello,
Gianfranco Di Renzo, and Salvatore
Amoroso
291
Irina G. Kessova and Arthur 1. Cederbaum
304
Stefania Ceruti, Alessia Mazzola, and
Maria P. Abbracchio
475
Digavalli V. Sivarao, Kimberly Newberry,
Shaun Langdon, Alicia V. Lee, Piyasena
Hewawasam, Mary Jane Plym, Laura
Signor, Robert Myers, and Nicholas J.
Lodge
476
The Effect of CYP2E1-Dependent Oxidant Stress on Activity
of Proteasomes in HepG2 Cells
ERRATA
Correction to "Resistance of Human Astrocytoma Cells to
Apoptosis Induced by Mitochondria-Damaging Agents:
Possible Implications for Anticancer Therapy"
Correction to "Effect of 4-(5-Chloro-2-hydroxyphenyl)-3-(2hydroxyethyl)-6-(trifluoromethyl)-quinolin-2(lf/)-one (BMS223131), a Novel Opener of Large Conductance Ca 2+Activated K + (Maxi-K) Channels on Normal and StressAggravated Colonic Motility and Visceral Nociception"