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The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
March 2006
Vol. 316, No. 3
Contents
ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION Harunobu Tahara, Hiroyuki Kusuhara,
Is the Monkey an Appropriate Animal Model to Examine Drug- Michihiro Chida, Eiichi Fuse, and
Yuichi Sugiyama
Drug Interactions Involving Renal Clearance? Effect of
Probenecid on the Renal Elimination of H 3 Receptor Antagonists
Anita A. Mathias, Lillian Maggio-Price,
Changes in Pharmacokinetics of Anti-HIV Protease Inhibitors
Yurong
Lai, Anshul Gupta, and
during Pregnancy: The Role of CYP3A and P-glycoprotein
Jashvant D. Unadkat
Improving the in Vitro Prediction of in Vivo Central Nervous
System Penetration: Integrating Permeability, P-glycoprotein
Efflux, and Free Fractions in Blood and Brain
Tibolone Metabolism in Human Liver Is Catalyzed by 3o/3/3Hydroxysteroid Dehydrogenase Activities of the Four lsoforms
of the Aldo-Keto Reductase (AKR)IC Subfamily
Developmental Expression of Aryl, Estrogen, and
Hydroxysteroid Sulfotransferases in Pre- and Postnatal
Human Liver
BEHAVIORAL PHARMACOLOGY
Comparison of the Antinociceptive Response to Morphine and
Morphine-Like Compounds in Male and Female SpragueDawley Rats
Comparative Cue Generalization Profiles of L-838,417,
SL651498, Zolpidem, CL218,872, Ocinaplon, Bretazenil,
Zopiclone, and Various Benzodiazepines in Chlordiazepoxide
and Zolpidem Drug Discrimination
Do Subtype-Selective y-Aminobutyric AcidA Receptor
Modulators Have a Reduced Propensity to Induce Physical
Dependence in Mice?
CARDIOVASCULAR
Erythropoietin, Modified to Not Stimulate Red Blood Cell
Production, Retains Its Cardioprotective Properties
Scott G. Summerfield, Alexander J. Stevens,
Leanne Cutler, Maria del Carmen Osuna,
Beverley Hammond, Sac-Pham Tang, Ann
Hersey, David J. Spalding, and Phil Jeffrey
Slephan Steckelbroeck. Busola Oyesanmi,
Yi Jin, Seon-Hwa Lee,
Helenius J. Kloosterboer, and
Trevor M. Penning
1187
1202
1282
1300
Zhengbo Duanmu, Amy Weckle,
Sevasti B. Koukouritaki, Ronald N. Hines,
Josie L. Falany, Charles N. Falany, Thomas
A. Kocarek, and Melissa Range-Morris
1310
Elizabeth M. Peckham and John R. Traynor
1195
N. R. Mirza, R. J. Rodgers, and
L. S. Mathiasen
1291
N. R. Mirza and E. 0. Nielsen
1378
Chanil Moon, Melissa Krawczyk,
Doojin Paik, Thomas Coleman, Michael
Brines, Magdalena Juhaszova, Steven J.
Sollott, Edward G. Lakatta, and Mark I.
Talan
999
Estrogen Receptor a Mediates Acute Potassium Channel
Stimulation in Human Coronary Artery Smooth Muscle Cells
Guichun Han, Xiuping Yu, Luo Lu,
Shuyi Li, Handong Ma, Shu Zhu,
Xiuyun Cui, and Richard E. White
1025
Comparative Evaluation of HERG Currents and QT Intervals
following Challenge with Suspected Torsadogenic and
Nontorsadogenic Drugs
Alexander N. Katchman, John Koerner,
Toshimasa Tosaka, Raymond L. Woosley,
and Steven N. Ebert
S. G. Burke, C. L. Wainwright, I. Vojnovic,
T. Warner, D. G. Watson, and B. L. Furman
1098
The Effect of NCX4016 [2-Acetoxy-benzoate 2-(2nitroxymethyl)-phenyl Ester] on the Consequences of Ischemia
and Reperfusion in the Streptozotocin Diabetic Rat
1107
The Urotensin-II Receptor Antagonist Palosuran Improves
Pancreatic and Renal Function in Diabetic Rats
Martine Clozel, Patrick Hess, Changbin Qiu,
Shuang-Shuang Ding, and Markus Rey
1115
Fibrin Affinity of Erythrocyte-Coupled Tissue-Type
Plasminogen Activators Endures Hemodynamic Forces and
Enhances Fibrinolysis in Vivo
Kumkum Ganguly, Mukul S. Goel,
Tatyana Krasik, Khalil Bdeir,
Scott L. Diamond, Douglas B. Cines,
Vladimir R. Muzykantov, and
Juan-Carlos Murciano
1130
Angiotensin I-Converting Enzyme Inhibitors Block Protein
Kinase Ce by Activating Bradykinin B1 Receptors in Human
Endothelial Cells
Sinisa Stanisavljevic, Tatjana Ignjatovic,
Peter A. Deddish, Viktor Brovkovych, Kai
Zhang, Ervin G. Erdos, and Randal A.
Skidgel
1153
Differential Expression of Components of the Cardiomyocyte
AdrenomedulhWIntermedin Receptor System following Blood
Pressure Reduction in Nitric Oxide-Deficient Hypertension
YouYou Zhao, David Bell, Lisa R. Smith,
Li Zhao, Adrian B. Devine,
Eugene M. McHenry, D. Paul Nicholls, and
Barbara J. McDermott
1269
CELLULAR AND MOLECULAR
[U A Trimeric Anti-HER2/«ew ScFv and Tumor Necrosis Factored Fusion Protein Induces HER2/ne« Signaling and Facilitates
Repair of Injured Epithelia
Tzu-Hsuan Huang and Sherie L. Morrison
Glibenclamide-Induced Apoptosis Is Specifically Enhanced by
Expression of the Sulfonylurea Receptor Isoform SUR1 but
Not by Expression of SUR2B or the Mutant SUR1(M1289T)
Annette Hambrock,
Claudia Bernardo de Oliveira Franz,
Sabrina Hiller, and Hartmut Osswald
1031
Linopirdine Modulates Calcium Signaling and StimulusSecretion Coupling in Adrenal Chromaffin Cells by Targeting
M-Type K+ Channels and Nicotinic Acetylcholine Receptors
Elvira V. Dzhura, Wenjuan He, and
Kevin P. M. Currie
1165
ff(+)-Methanandamide and Other Cannabinoids Induce the
Expression of Cyclooxygenase-2 and Matrix
Metalloproteinases in Human Nonpigmented Ciliary Epithelial
Cells
Susanne Rosen, Robert Ramer, Kay Bntne,
and Burkhard Hinz
1219
Identification of the Insulin Signaling Cascade in the
Regulation of Alpha-Class Glutathione S-Transferase
Expression in Primary Cultured Rat Hepatocytes
Sang K. Kim, Mohamed A. Abdelmegeed,
and Raymond F. Novak
1255
Differential Efficacies of Somatostatin Receptor Agonists for
G-Protein Activation and Desensitization of Somatostatin
Receptor Subtype 4-Mediated Responses
Mia Engstrom, Juha-Matti Savola, and
Siegfried Wurster
1262
Growth Hormone Determines Sexual Dimorphism of Hepatic
Cytochrome P450 3A4 Expression in Transgenic Mice
Connie Cheung, Ai-Ming Yu,
Chong-Sheng Chen, Kristopher W. Krausz,
Linda G. Byrd, Lionel Feigenbaum, Robert
J. Edwards, David J. Waxman, and Frank J.
Gonzalez
1328
Yuling Chi, Sonya M. Khersonsky,
Young-Tae Chang, and Victor L. Schuster
1346
Ying Mu, Jinnan Zhang, Shimin Zhang,
Hong-Hao Zhou, David Toma,
Songrong Ren, Leaf Huang, Maria Yaramus,
Andrew Baum, Raman Venkataramanan, and
Wen Xie
T369
HO Identification of a New Class of Prostaglandin Transporter
Inhibitors and Characterization of Their Biological Effects on
Prostaglandin E2 Transport
Traditional Chinese Medicines Wu Wei Zi (Schisandra
chinensis Bail!) and Gan Cao (Glycyrrhiza uralensis Fisch)
Activate Pregnane X Receptor and Increase Warfarin
Clearance in Rats
CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY
Molecular Targeting of BCL2 and BCLXL Proteins by
Synthetic BCL2 Homology 3 Domain Peptide Enhances the
Efficacy of Chemotherapy
Sonia S. Dharap, Pooja Chandna,
Yang Wang, Jayant J. Khandare, Bo Qiu,
Stanley Stein, and Tamara Minko
992
ENDOCRINE AND DIABETES
A Model of Controlled Acute Hyperglycemia in Rats: Effects of
Insulin and Glucagon-Like Peptide-1 Analog
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL
Opposite Effects of Pre- and Postischemic Treatments with
Nitric Oxide Donor on Ischemia/Reperfusion-Induced Renal
Injury
Effects of Calcium Channel Blockade on Angiotensin IIInduced Peritubular Ischemia in Rats
Metformin Prevents Endotoxin-Induced Liver Injury after
Partial Hepatectomy
Joy K. Saha, Jinqi Xia, Steven K. Engle,
Yun-Fei Chen, Wolfgang Glaesner, and
Joseph A. Jakubowski
1159
Atsushi Nakajima, Kyoko Ueda, Masanori
Takaoka, Yoshiko Yoshimi, and YaSUO
Matsumura
1038
Naoki Kondo, Hideyasu Kiyomoto,
Tokunori Yamamoto, Akira Miyatake,
Guang-Ping Sun, Matlubur Rahman,
Hirofumi Hitomi, Kumiko Moriwaki,
Taiga Hara, Shoji Kimura, Youichi Abe,
Masakazu Kohno, and Akira Nishiyama
Ina Bergheim, James P. Luyendyk,
Chad Steele, Gilandra K. Russell,
Luping Guo, Robert A. Roth, and
Gavin E. Arteel
1047
1053
Pharmacologic Characterization of Intrinsic Mechanisms
Controlling Tone and Relaxation of Porcine Lower
Esophageal Sphincter
Ricard Farre, Mariona Aulf, Begona Lecea,
Emma Martinez, and Pere Clave
1238
Superoxide Dismutase Mimetic Preserves the Glomerular
Capillary Permeability Barrier to Protein
Pu Duann, Prasun K. Datta, Cynthia Pan,
Jeffrey B. Blumberg, Mukut Sharma, and
Eli as A. Lianos
1249
Tiziana Genovese, Emanuela Mazzon,
Concetta Crisafulli, Rosanna Di Paola,
Carmelo Muia, Placido Bramanti, and
Salvatore Cuzzocrea
Elizabeth B. Kelso, John C. Lockhart, Todd
Hembrough, Lynette Dunning, Robin Plevin,
Morley D. Hollenberg, Christian P.
Sommerhoff, John S. McLean, and William
R. Ferrell
1006
INFLAMMATION AND IMMUNOPHARMACOLOGY
Immunoniodulatory Effects of Etanercept in an Experimental
Model of Spinal Cord Injury
Therapeutic Promise of Proteinase-Activated Receptor-2
Antagonism in Joint Inflammation
The Phase 2 Enzyme Inducers Ethacrynic Acid, DLSulforaphane, and Oltipraz Inhibit LipopolysaccharideInduced High-Mobility Group Box 1 Secretion by RAW 264.7
Cells
S-Adenosyl-i.-homocysteine Hydrolase Inactivation Curtails
Ovalbumin-Induced Immune Responses
Second-Generation Inhibitors Demonstrate the Involvement of
p38 Mitogen-Activated Protein Kinase in Post-Transcriptional
Modulation of Inflammatory Mediator Production in Human
and Rodent Airways
NEUROPHARMACOLOGY
Elevation of Endocannabinoid Levels in the Ventrolateral
Periaqueductal Grey through Inhibition of Fatty Acid Amide
Hydrolase Affects Descending Nociceptive Pathways via Both
Cannabinoid Receptor Type 1 and Transient Receptor
Potential Vanilloid Type-1 Receptors
1017
Meaghan E. Killeen, Joshua A. Englert,
Donna Beer Stolz, Mingchen Song, Yusheng
Han, Russell L. Delude, John A. Kellum,
and Mitchell P. Fink
1070
Yun-Feng Fu, Jun-Xia Wang, Yang Zhao,
Yang Yang, Wei Tang, Jia Ni, Yi-Na Zhu,
Ru Zhou, Pei-Lan He, Chuan Li, Xiao-Yu
Li, Yi-Fu Yang, Brian R. Lawson, and JianPing Zuo
1229
Mark A. Birrell, Sissie Wong, Kerryn
McCluskie, Matthew C. Catley, Elizabeth L.
Hardaker, Saleem Haj-Yahia, and Maria G.
Belvisi
1318
Sabatino Maione, Tiziana Bisogno, Vito de
Novellis, Enza Palazzo, Luigia Cristino,
Marta Valenti, Stefania Petrosino, Vittorio
Guglielmotti, Francesco Rossi, and
Vincenzo Di Marzo
Cumulative Activation of Akt and Consequent Inhibition of
Glycogen Synthase Kinase-3 by Brain-Derived Neurotrophic
Factor and Insulin-Like Growth Factor-1 in Cultured
Hippocampal Neurons
Nadine N. Johnson-Farley,
Tatyana Travkina, and Daniel S. Cowen
1062
Ex Vivo Imaging of Fatty Acid Amide Hydrolase Activity and
Its Inhibition in the Mouse Brain
Sherrye T. Glaser, S. John Gatley, and
Andrew N. Gifford
1088
TrkAd5: A Novel Therapeutic Agent for Treatment of
Inflammatory Pain and Asthma
Judy J. Watson, Mark S. Fahey, Edwin
van den Worm, Ferdi Engels, Frans P.
Nijkamp, Paul Stroemer, Steve
McMahon, Shelley J. Allen, and David
Dawbarn
1122
Advantages for Transdermal over Oral Oxybutynin to Treat
Overactive Bladder: Muscarinic Receptor Binding, Plasma
Drug Concentration, and Salivary Secretion
Tomomi Oki, Ayako Toma-Okura, and
Shizuo Yamada
1137
Brain Cholesterol Synthesis in Mice Is Affected by High Dose
of Simvastatin but Not of Pravastatin
Karin M. Thelen, Katbarina M. Rentsch,
Ursula Gutteck, Maura Heverin, Maria OHn,
Ulla Andersson, Arnold von Eckardstein,
Ingemar Bjb'rkhem, and Dieter Liitjohann
G. R. Dawson, K. A. Maubach,
N. Collinson, M. Cobain, B. J. Everitt,
A. M. MacLeod, H. I. Choudhury,
L. M. McDonald, G. Pillai, W. Rycroft,
A. J. Smith, F. Sternfeld, F. D. Tattersall,
K. A. Wafford, D. S. Reynolds,
G. R. Seabrook, and J. R. Atack
Signe I Storuslovu and Bjarke Ebert
1 146
An Inverse Agonist Selective for «5 Subunit- Containing
GABAA Receptors Enhances Cognition
Pharmacological Characterization of Agonists at S-Containing
GABAA Receptors: Functional Selectivity for Extrasynaptic
Receptors Is Dependent on the Absence of y2
The 8 Subunit of y-Aminobutyric Acid Type A Receptors
Does Not Confer Sensitivity to Low Concentrations of Ethanol
TOXICOLOGY
H Microarray Analysis of Lipopolysaccharide Potentiation of
Trovafloxacin-Induced Liver Injury in Rats Suggests a Role for
Proinflammatory Chemokines and Neutrophils
Cecilia M. Borghese, Signe i Storustovu,
Bjarke Ebert, Murray B. Herd, Delia BelelH,
Jeremy J. Lambert, George Marshall, Keith
A. Wafford, and R. Adron Harris
1335
1351
1360
Jeffrey F. Waring, Michael J. Liguori,
James P. Luyendyk, Jane F. Maddox,
Patricia E. Ganey, Robert F. Stachlewitz,
Colin North, Eric A. G. Blomme, and
Robert A. Roth
1080
Modulation of Expression of Rat Mitochondrial 2Oxoglutarate Carrier in NRK-52E Cells Alters Mitochondrial
Transport and Accumulation of Glutathione and Susceptibility
to Chemically Induced Apoptosis
Feng Xu, David A. Putt, Larry H. Matherly,
and Lawrence H. Lash
1175
Relationship between Temperature, Dopaminergic
Neurotoxicity, and Plasma Drug Concentrations in
Methamphetamine-Treated Squirrel Monkeys
Jie Yuan, George Hatzidimitriou,
Pranav Suthar, Melanie Mueller,
Una McCann, and George Ricaurte
1210
Kari T. Kivisto
1386
Yvonne Y. Lau, Hideaki Okochi,
Yong Huang, and Leslie Z. Benet
1387
LETTERS TO THE EDITOR
Comments on "Multiple Transporters Affect the Disposition of
Atorvastatin and Its Two Active Hydroxy Metabolites:
Application of in Vitro and ex Situ Systems"
Response to Comments on "Multiple Transporters Affect the
Disposition of Atorvastatin and Its Two Active Hydroxy
Metabolites: Application of in Vitro and ex Situ Systems"