Pharmacology




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The Journal of

PHARMACOLOGY



And Experimental Therapeutics

A Publication of the American Society for Pharmacology and Experimental Therapeutics



December 2006

Vol. 319, No. 3



Contents

PERSPECTIVES IN PHARMACOLOGY

A Death-Promoting Role for Extracellular Signal-Regulated Kinase

BEHAVIORAL PHARMACOLOGY

Characterization of Cannabinoid Agonists and Apparent pA2 Analysis of Cannabinoid Antagonists in Rhesus Monkeys Discriminating A9-Tetrahydrocannabinol

CARDIOVASCULAR

Up-Regulation of Heme Oxygenase Provides Vascular Protection in an Animal Model of Diabetes through Its Antioxidant and Antiapoptotic Effects

Cl-IB-MECA [2-Chloro-A'6-{3-iodobenzyl)adenosine-5'-A'-methylcarboxamide] Reduces Ischemia/Reperfusion Injury in Mice by Activating the A3 Adenosine Receptor

Modulation of Contractile Function through Neuropeptidc Y Receptors during Development of Cardiomyocyte Hypertrophy

Protein Kinase A-Mediated Phosphorylation Contributes to Enhanced Contraction Observed in Mice That Overexpress (3-Adrenergic Receptor Kinase-1

Phosphorylation of Endothelial Nitric-Oxide Synthase Is Diminished in Mesenteric Arteries from Septic Rabbits Depending on the Altered Phosphatidylinositol 3-Kinase/Akt Pathway: Reversal Effect of Fluvastatin Therapy

Reversible Blockade of Electron Transport during Ischemia Protects Mitochondria and Decreases Myoeardial Injury following Reperfusion

Raloxifene Elicits Combined Rapid Vasorelaxation and Long-Term Anti-Inflammatory Actions in Rat Aorta

Shougang Zhuang and Rick G. Schnellmann

Lance R.

Adam L. Kruger,

Michal L. Schwarteman, Heidi Fusco,

John A. McClung, Melvin Weiss,

Sylvia Shenouda, Alvin I. Goodman,

Michael S. Goligorsky, Attallah Kappas, and

Nader G. Abraham

Zhi-Dong Ge, Jason N. Peart, Laura M. Kreckler, Tina C. Wan, Marlene A. Jacobson, Garrett J. Gross, and John A. Auchampach

Adrian R. Allen, Elizabeth J. Kelso, David Bell, YouYou Zhao, Paula Dickson, and Barbara J. McDermott

Erin E. Mueller, Scott A. Grandy, and Susan E. Howlett

Naoyuki Matsuda, Yukio Hayashi, Yoshika Takahashi, and Yuichi Hattori

Qun Chen, Shadi Moghaddas,

Charles L. Hoppel, and Edward J. Lesnefsky

Christian Pinna, Chiara Bolego,

Paola Sanvito, Valeria Pelosi,

Roberta Baetta, Alberto Corsini,

Rosa Maria Gaion, and Andrea Cignarella

991


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1200

1286


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CELLULAR AND MOLECULAR

Coadministration of Sorafenib with Rottlerin Potently Inhibits Cell Proliferation and Migration in Human Malignant Glioma Cells

Esther P. Jane, Daniel R. Premkumar, and Ian F. Pollack

1070

Estradiol Protects against Ethanol-Induced Bone Loss by Inhibiting Up-Regulation of Receptor Activator of Nuclear Factor-KB Ligand in Osteoblasts

Ginsenoside-Rh2-Induced Mitochondrial Depolarization and Apoptosis Are Associated with Reactive Oxygen Species- and Ca2+-Mediated c-Jun NH2-Terminal Kinase 1 Activation in HeLa Cells

Proteasome Inhibitors Potentiate Etoposide-Induced Cell Death in Human Astrocytoma Cells Bearing a Mutated p53 Isoform

Block of Specific Gap Junction Channel Subtypes by 2-Aminoethoxydiphenyl Borate (2-APB)

CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY

Reactive Oxygen Species Mediate Caspase Activation and Apoptosis Induced by Lipoic Acid in Human Lung Epithelial Cancer Cells through BcI-2 Down-Regulation

Pifithrin-a Enhances Chemosensitivity by a p38 Mitogen-Activated Protein Kinase-Dependent Modulation of the Eukaryotic Initiation Factor 4E in Malignant Cholangioeytes

Inhibition of Xenograft Tumor Growth and Down-Regulation of ErbB Receptors by an Antibody Directed against Lewis Y Antigen

Jin-Ran Chen, Rani Lynn Haley, 1182

Mats Hidcstrand, Kartik Shankar, Xiaoli Liu, Charles K. Lumpkin, Pippa M. Simpson, Thomas M. Badger, and Martin J. J. Ronis

Young-Mi Ham, Jin-Hee Lim, 1276

Hye-Kyung Na, Joon-Seok Choi, Byoung-Duck Park, Hyungshin Yim, and Seung-Ki Lee

Stcfania Ceruti, Alessia Mazzola, and 1424

Maria P. Abbracchio

Donglin Bai, Cristiane del Corsso, 1452

Miduturu Srinivas, and David C. Spray

Jirapan Moungjaroen, Ubonthip Nimmannit, 1062

Patrick S. Callery, Liying Wang,

Neelam Azad, Vimolmas Lipipun,

Pithi Chanvorachote, and Yon Rojanasakal

Hania Wehbe, Roger Henson, Molly Lang, 1153

Fanyin Meng, and Tushar Patel

Hesso Farhan, Christian Schuster, 1459

Markus Klinger, Eva Weisz,

Gunter Waxenecker, Manfred Schuster,

Veronika Sexl, Geert C. Mudde,

Michael Freissmuth, and Raif Kircheis




ENDOCRINE AND DIABETES

Differential Responses of Corticotropin-Releasing Hormone Receptor Type J Variants to Protein Kinase C Phosphorylation

Calcium Channel Blocker Azelnidipine Reduces Glucose Intolerance in Diabetic Mice via Different Mechanism Than Angiotensin Receptor Blocker Olmesartan

7-But-2-ynyl-9-(6-methoxy -pyridin-3-yl)-6-piperazin-1 -y 1-7,9-dihydro-purin-8-one Is a Novel Competitive and Selective Inhibitor of Dipeptidyl Peptidase IV with an Antihyperglycemic Activity

Inhalation of Human Insulin Is Associated with Improved Insulin Action Compared with Subcutaneous Injection and Endogenous Secretion in Dogs

Danijela Markovic, Nikoileta Papadopoulou, 1032

Thalia Teli, Harpal Randeva,

Michael A. Levine, Edward W. Hillhouse,

and Dimitris K. Grammatopoulos

Masarsu Iwai, Huan-Sheng Li, Rui Chen, 1081

Tetsuya Shiuchi, Lan Wu, Li-Juan Min. Jian-Mei Li. Masahiro Tsuda. Jun Suzuki, Yumiko Tomono, Hirokazu Tomochika, Masaki Mogi, and Masatsugu Horiuchi

Kazuto Yamazaki, Nobuyuki Yasuda, 1253

Takashi Inoue, Tadashi Nagakura, Kazunobu Kira, Masanobu Shinoda, Takao Saeki, and Isao Tanaka

Dale S. Edgerton, Kathryn M. Stettler, 1258

Doss W. Neal, Melanie Scott, Larry Bowen, Warren Wilson, Charles H. Hobbs, Chet Leach, Thomas R. Strack, and Alan D. Cherrington


GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL Translocation of AT,- and AT2-Receptors by Higher Concentrations of Angiotensin II in the Smooth Muscle Cells of Rat Internal Anal Sphincter

Mast Cell Stabilizer Ketotifen [4-(l-Methyl-4-piperidylidene)-4ff-benzo[4,5]cyclohepta[l,2-/>]thiophen-10(9tf)-one Fumarate] Prevents Mucosal Mast Cell Hyperplasia and Intestinal Dysmotility in Experimental Trichinella spiralis Inflammation in the Rat

Muscarinic Regulation of Ether-a-go-go -Related Gene K+ Currents in Interstitial Cells of Cajal

A Single Intraperitoneal Dose of Carbon Monoxide-Saturated Ringer's Lactate Solution Ameliorates Postoperative Ileus in Mice

Marcio A. F. de Godov and Satish Rattan 1088

H. Serna, M. Porras, and P. Vergara 1104

Catherine M. McKay and Jan D. Huizinga 1112

Atsunori Nakao, Joachim Schmidt, 1265

Tomoyuki Harada, Allan Tsung,

Burkhard StoffeJs, Ruy J. Cruz, Jr.,

Junichi Kohmoto, Ximei Peng,

Koji Tomiyama, Noriko Murase,

Anthony J. Bauer, and Mitchell P. Fink



INFLAMMATION, IMMUNOPHARMACOLOGY, AND ASTHMA \s} R406, an Orally Available Spleen Tyrosine Kinasc Inhibitor Blocks Fc Receptor Signaling and Reduces Immune Complex-Mediated Inflammation

Prostacyclin Antagonism Reduces Pain and Inflammation in Rodent Models of Hyperalgesia and Chronic Arthritis

A Potent Human Anti-Eotaxinl Antibody, CAT-213: Isolation by Phage Display and in Vitro and in Vivo Efficacy

Sylvia Braselmann, Vanessa Taylor, 998

Haoran Zhao, Su Wang, Catherine Sylvain, Muhammad Baluom, Kunbin Qu, Ellen Herlaar, Angela Lau, Chi Young, Brian R. Wong, Scott Lovell, Thomas Sun, Gary Park, Anfcush Argade, Stipo Jurcevic, Polly Pine, Rajinder Singh, Elliott B. Grossbard, Donald G. Payan, and Esteban S. Masuda

Anne-Marie Pulichino, Steve Rowland, 1043

Tom Wu, Patsy Clark, Daigen Xu,

Marie-Claude Mathieu, Denis Riendeau, and

Laurent P. Audoly

Sarah Main, Rachel Handy, Jane Wiiton, 1395

Stephen Smith, Liz Williams, Leila Du Fou,

John Andrews, Louise A. Conroy.

Richard May, Ian Anderson, and

Tristan J. Vaughan





METABOLISM, TRANSPORT, AND PHARMACOGENOMICS

Pharmacokinetic and Pharmacodynamic Modeling of Recombinant Human Erythropoietin after Intravenous and Subcutaneous Administration in Rats

Antiplatelet Agents Aspirin and Clopidogrel Are Hydrolyzed by Distinct Carboxylesterases, and Clopidogrel Is Transesterificated in the Presence of Ethyl Alcohol

Anti-Influenza Prodrug Oseltamivir Is Activated by Carboxylesterase Human Carboxylesterase 1, and the Activation Is Inhibited by Antiplatelet Agent Clopidogrel Evaluation of the Role of Multidrug Resistance-Associated Proteins (Mrp) 3 and Mrp4 in Hepatic Basolateral Excretion of Sulfate and Glucuronide Metabolites of Acetaminophen, 4-MethyIumbelliferone, and Harmol in Abcc3~/~ and Mkc4~1 Mice

NEUROPHARMACOLOGY

Acetylcholine Release at Neuromuscular Junctions of Adult Tottering Mice Is Controlled by N- (Cav2.2) and R-Type (Cav2.3) but Not L-Type (Cav1.2) Ca2+ Channels Altered Calcium/Calmodulin Kinase II Activity Changes Calcium Homeostasis That Underlies Epileptiform Activity in Hippocampal Neurons in Culture

Rapid Broad-Spectrum Analgesia through Activation of Peroxisome Proliferator-Activated Receptor-a

Prostaglandin E2 Receptor EP4 Contributes to Inflammatory Pain Hypersensitivity

Estrogenic Agonist Activity of ICI 182,780 (Kaslodex) in Hippocampal Neurons: Implications for Basic Science Understanding of Estrogen Signaling and Development of Estrogen Modulators with a Dual Therapeutic Profile

Studies to Investigate the in Vivo Therapeutic Window of the

y-Secretase Inhibitor Aj2-[(2S)-2-(3,5-DifluorophenyI)-2-

hydroxyethanoyl]-A'1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5/r-

dibenzo[/»^/]azepin-7-yl]-L-aIaninamide (LY411,575) in the

CRND8 Mouse

Discovery of Novel Hippocampal Neurogenic Agents by Using

an in Vivo Stable Isotope Labeling Technique

Oral Treatment with Rofecoxib Reduces Hippocampal Excitotoxic Ncurodegeneration

In l-Methyl-4-phenyl-l,2,3,6-tetrahydropyridine-Treated Primates, the Selective 5-Hydroxytryptamine la Agonist (R)-(+)-8-OHDPAT Inhibits Levodopa-Induced Dyskinesia but Only with Increased Motor Disability

Sukyung Woo, Wojciech Krzyzanski, and 1297

William J. Jusko

Man Tang, Madhu Mukundan, Jian Yang, 1467

Nathan Charpentier. Edward L. LeCIuyse,

Chris Black, Dongfang Yang, Deshi Shi, and

Bingfang Yan

Deshi Shi, Jian Yang, Dongfang Yang, 1477

Edward L. LeCIuyse, Chris Black, Li You,

Falemeh Akhlaghi, and Bingfang Yan

Maciej J. Zamek-Gliszczynski, Ken-ichi Nezasa, 1485

Xianbin Tian, Arlene S. Bridges, Kun Lee,

Martin G. Belinsky, Gary D. Kruh, and

Kim L. R. Brouwer

Nicole E. Pardo, Ravindra K. Hajela, and 1009

William D. Atchison

Dawn S. Carter, S. Naqeeb Haider, 1021

Robert E. Blair, Laxmikant S. Deshpande,

Sompong Sombati, and Robert J. DeLorenzo

Jesse LoVerme, Roberto Russo, 1051

Giovanna La Rana, Jin Fu, Jesse Farthing,

Giuseppina Mattace-Raso, Rosaria Meli,

Andrea Hohmann, Antonio Calignano, and

Daniele Piomelli

Chung-Ren Lin, Fumimasa Amaya, 1096

Lee Barrett, Haibin Wang, Junji Takada,

Tarek A. Samad, and Clifford J. Woolf

Liqin Zhao, Kathleen O'Neill, and 1124

Roberta Diaz Brinton

Lynn A. Hyde, Nansie A. McHugh, 1133

Joseph Chen, Qi Zhang, Denise Manfra,

Amin A. Nomeir, Hubert Josien,

Thomas Bara, John W. Clader, Lili Zhang,

Eric M. Parker, and Guy A. Higgins

Mahalakshmi Shankaran, Chelsea King, 1172

Jean Lee. Robert Busch, Mary Wolff, and

Marc K. Hellerstein

Sandra J. Heweti. Janna M. Silakova, and 1219

James A. Hewett

Mahmoud M. Iravani, 1225

Kayhan Tayarani-Binazir, Wing B. Chu,

Michael J. Jackson, and Peter Jenner



Effects of Analgesic or Antidepressant Drugs on Pain- or Stress-Evoked Hippocampal and Spinal Neurokinin-1 Receptor and Brain-Derived Neurotrophic Factor Gene Expression in the Rat

The Anxioselective Agent 7-(2-Chloropyridin-4-yl)pyrazoIo-[l,5-a]-pyrimidin-3-yl](pyridin-2-yl)methanone (DOV 51892) Is More Efficacious Than Diazepam at Enhancing GABA-Gated Currents at a^ Subunit-Containing GABAA Receptors

GABAB(1) Receptor Suliunit Isoforms Exert a Differential Influence on Baseline but Not GABAB Receptor Agonist-Induced Changes in Mice

Low-Dose Methylphenidate Actions on Tonic and Phasic Locus Coeruleus Discharge

Sigma-1 Receptor Activation Prevents Intracellular Calcium Dysregulation in Cortical Neurons during in Vitro Ischemia

Differential Effects of Systemic Ethanol Administration on Protein Kinase Ce, y, and /3 Isoform Expression, Membrane Translocation, and Target Phosphorylation: Reversal by Chronic Ethanol Exposure

A-740003 |7V-(l-{{(Cyanoimino){5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a Novel and Selective P2X7 Receptor Antagonist, Dose-Dependently Reduces Neuropathic Pain in the Rat

The Use of the Isolated Mouse Whole Bladder for Investigating Bladder Overactivity

TOXICOLOGY


Differentiation-Specific Factors Modulate Epidermal CYP1-4 Gene Expression in Human Skin in Response to Retinoic Acid and Classic Aryl Hydrocarbon Receptor Ligands Modest Inflammation Enhances Diclofenac Hepatotoxicity in Rats: Role of Neutrophils and Bacterial Translocation



Cardioprotective Effects of a Novel Iron Chelator, Pyridoxal 2-Chlorobenzoyl Hydrazone, in the Rabbit Model of Daunorubicin-Induced Cardiotoxicity

Hepatocellular Toxicity and Pharmacological Effect of Amiodarone and Amiodarone Derivatives

Cycloheximide Protects HepG2 Cells from Serum Withdrawal-Induced Apoptosis by Decreasing p53 and Phosphorylated p53 Levels

ERRATUM

Correction to "A Novel Phospholipid Derivative of Indomethacin, DP-155 [Mixture of 1-Steroyl and 1-Palmkoyl-2- {4- [1 -

Vanja Duric and Kenneth E. McCarson

Piotr Popik, Emmanuel Kostakis, Martyna Krawczyk, Gabriel Nowak, Bernadeta Szewczyk, Philip Krieter, Zhengming Chen, Shelley J. Russck, Terrell T. Gibbs, David H. Farb, Phil Skolnick, Arnold S. Lippa, and Anthony S. Basile Laura H. Jacobson, Bernhard Bettler, Klemens Kaupmann, and John F. Cryan

David M. Devilbiss and Craig W. Berridge

Christopher Katnik, Waldo R. Guerrero, Keith R. Pennypacker, Yelenis Herrera, and Javier Cuevas S. Kumar, B. M. Lane, and A. L. Morrow

Prisca Honore, Diana Donnelly-Roberts, Marian T. Namovic, Gin Hsieh, Chang Z. Zhu, Joe P. Mikusa, Gricelda Hernandez, Chengmin Zhong, Donna M. Gauvin, Peasant Chandran, Richard Harris, Arturo Perez Medrano, William Carroll, Kennan Marsh, James P. Sullivan, Connie R, Faltynek, and Michael F. Jarvis Adebola C. Fabiyi and Alison F. Brading

Liping Du, Mark M. Neis, Patricia A. Ladd, and Diane S. Keeney

Xiaomin Deng, Robert F. Stachlewitz,

Michael J. Liguori, Eric A. G. Blomme,

Jeffrey F. Waring, James P. Luyendyk,

Jane F. Maddox, Patricia E. Ganey,

and Robert A. Roth

Martin Sterba,

Olga Popelova, Tomas Simunek,

Yvona Mazurova", Anna Potacova,

Michaela Adamcova, Helena Kaiserova,

Pfemysl Ponka, and Vladimir Gersl

Katri Maria Waldhauser, Michael Torok,

Huy-Riem Ha, Urs Thomet, Daniel Konrad,

Karin Brecht, Ferenc Follath, and

Stephan Krahenbiihl

Jingxiang Bai and Arthur I. Cederbaum


1235

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1327 1355

1366 1376

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