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The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
August 2005
Vol. 314, No. 2
Contents
PERSPECTIVES IN PHARMACOLOGY
The Origins of Diversity and Specificity in G Protein-Coupled
Receptor Signaling
Stuart Maudsley, Bronwen Martin, and
48
5
ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION Louis M. Luttrell
GO Comparative Pharmacophore Modeling of Organic Anion
Transporting Polypeptides: A Meta-Analysis of Rat Oatplal and
Cheng Chang, K. Sandy Pang,
Human OATP1B1
The p53 Inhibitor Pifithrin-a Is a Potent Agonist of the Aryl
Hydrocarbon Receptor
Variability of CYP3A7 Expression in Human Fetal Liver
53
3
Peter W. Swaan, and Sean Ekins
Martin S. Hoagland, Erica M. Hoagland, and
603
Hepatic Cytochrome P450 Gene Regulation during EndotoxinInduced Inflammation in Nuclear Receptor Knockout Mice
Role of N-Terminal Amino Acids in the Absorption-Enhancing
Effects of the C-Terminal Fragment of Clostridium perfringens
Enterotoxin
Rapid Elimination of Cefaclor from the Cerebrospinal Fluid Is
Mediated by a Benzylpenicillin-Sensitive Mechanism Distinct
from Organic Anion Transporter 3
Bile Salt Export Pump (BSEP/ABCB11) Can Transport a
Nonbile Acid Substrate, Pravastatin
Amino Acid Ester Prodrugs of 2-Bromo-5,6-dichloro-l-(/J-Dribofuranosyl)benzimidazole Enhance Metabolic Stability in
Vitro and in Vivo
Renal Clearance of Endogenous Hippurate Correlates with
Expression Levels of Renal Organic Anion Transporters in
Uremic Rats
BEHAVIORAL PHARMACOLOGY
Neurochemical and Behavioral Responses
Male Rats with Neonatal Isolation Experien :
Hollie I. Swanson
J. Steven Leeder, Roger Gaedigk,
Kenda A. Marcucci, Andrea Gaedigk, Carrie A.
Vyhlidal, Bradley P. Schindel, and Robin E.
Pearce
Terrilyn A. Richardson and
Edward T. Morgan
626
Akane Masuyama, Masuo Kondoh,
Hirotoshi Seguchi, Azusa Takahashi,
Motoki Harada, Makiko Fujii,
Hiroyuki Mizuguchi, Yasuhiko Horiguchi,
and Yoshiteru Watanabe
Misaki Kuroda, Hiroyuki Kusuhara,
Hitoshi Endou, and Yuichi Sugiyama
789
703
855
Masaru Hirano, Kazuya Maeda,
Hisamitsu Hayashi, Hiroyuki Kusuhara, and
Yuichi Sugiyama
876
Philip L. Lorenzi, Christopher P. Landowski,
Xueqin Song, Katherine Z. Borysko,
Julie M. Breitenbach, Jae Seung Kim,
John M. Hilfinger, Leroy B. Townsend,
John C. Drach, and Gordon L. Amidon
883
Tsuneo Deguchi, Mizue Takemoto,
Nao Uehara, W. Edward Lindup, Ayaka
Suenaga, and Masaki Otagiri
932
Therese A. Kosten, Xiang Yang Zhang, and
Priscilla Kehoe
661
Characterization of the Discriminative Stimulus Effects of the
Neuroactive Steroid Pregnanolone in DBA/2J and C57BL/6J
Inbred Mice
Characterization in Rats of the Anxiolytic Potential of
ELB139 [l-(4-Chlorophenyl)-4-piperidin-l-yl-l,5-dihydroimidazol-2-on], a New Agonist at the Benzodiazepine Binding
Site of the GABAA Receptor
CARDIOVASCULAR
Arachidonic Acid Epoxygenase Metabolites Stimulate
Endothelial Cell Growth and Angiogenesis via MitogenActivated Protein Kinase and Phosphatidylinositol 3-Kinase/
Akt Signaling Pathways
Protein Kinase C 011 Peptide Inhibitor Exerts
Cardioprotective Effects in Rat Cardiac Ischemia/Reperfusioii
Injury
Disodium Disuccinate Astaxanthin (Cardax) Attenuates
Complement Activation and Reduces Myocardial Injury
following Ischemia/Reperfusion
Evaluation of PAI-039 [{l-Benzyl-5-[4(trifluoromethoxy)phenyl]-ltf-indol-3-yl}(oxo)acetic Acid], a
Novel Plasminogen Activator Inhibitor-1 Inhibitor, in a
Canine Model of Coronary Artery Thrombosis
Differential Distribution of Functional a1-Adrenergic
Receptor Subtypes along the Rat Tail Artery
Erin E. Shannon, Patrizia Porcu,
Robert H. Purdy, and Kathleen A. Grant
675
Barbara Langen, Ute Egerland,
Katrin Bernoster, Rita Dost,
Klaus Unverierth, and Chris Rundfeldt
717
Yan Wang, Xin Wei, Xiao Xiao, Rutai Hui,
Jeffrey W. Card, Michelle A. Carey, Dao
Wen Wang, and Darryl C. Zeldin
522
Didi Omiyi, Richard J. Brue,
Philip Taormina II, Margaret Harvey, Norreli
Atkinson, and Lindon H. Young
542
D. Adam Lauver, Samuel F. Lockwood, and
Benedict R. Lucchesi
686
James K. Hennan, Hassan Elokdah,
Mauricip Leal, Allena Ji,
Gregory S. Friedrichs, Gwen A. Morgan,
Robert E. Swillo, Thomas M. Antrim,
Amy Hreha, and David L. Crandall
Susana Y. Kamikihara, Andre Mueller,
Vanessa Lima, Aderbai R. T. Silva, Isabela
Bazzo da Costa, Jose Buratirn, Jr., and Andre
S. Pupo
710
753
Resveratrol-Mediated Activation of cAMP Response ElementBinding Protein through Adenosine A 3 Receptor by AktDependent and -Independent Pathways
Samarjit Das, Arpad Tosaki, Debasis Bagchi,
Nilanjana Maulik, and Dipak K. Das
762
Two "Knockout" Mouse Models Demonstrate That Aortic
Vasodilatation Is Mediated via a2A-Adrenoceptors Located on
the Endothelium
Majid Malekzadeh Shat'aroudi,
Melissa McBride, Clare Deighan,
Alexis Wokoma, Joyce Macmillan,
Craig J. Daly, and John C. McGrath
804
Effect of Tempol on Renal Cyclooxygenase Expression and
Activity in Experimental Diabetes in the Rat
Jing Li, Yu-Jung Chen, and John Quilley
818
Jin-Sung Kim, Jin-Yong Park,
Ho-Won Kang, Eun-Jung Lee,
Hyoweon Bang, and Jung-Ha Lee
618
Resistance of Human Astrocytoma Cells to Apoptosis Induced
by Mitochondria-Damaging Agents: Possible Implications for
Anticancer Therapy
Stefania Ceruti, Alessia Mazzola, and
Maria P. Abbracchio
825
The Endocannabinoid Noladin Ether Acts as a Full Agonist at
Human CB2 Cannabinoid Receptors
Jennifer L. Shoemaker, Biny K. Joseph,
Michael B. Ruckle, Philip R. Mayeux, and
Paul L. Prather
868
Phenoxybenzamine and Benextramine, but Not 4Diphenylacetoxy-Ar-[2-chIoroethyl]piperidine Hydrochloride,
Display Irreversible Noncompetitive Antagonism at G ProteinCoupled Receptors
Johannes Bodenstein, Daniel P. Venter, and
Christiaan B. Brink
891
Zhi-Yuan Xu, Martin Loignon, Fei-Yu Han,
Lawrence Panasci, and Raquel Aloyz
495
Lalitha R. Belur, Rohaizah I. James,
Chad May, Miechaleen D. Diers, Debra
Swanson, Roland Gunther, and R. Scott
Mclvor
668
Hiroshi Akahori, Tsuguhito Ota,
Muneyoshi Torita, Hitoshi Ando, Shuichi
Kaneko, and Toshinari Takamura
514
CELLULAR AND MOLECULAR
Zinc Activates TREK-2 Potassium Channel Activity
CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY
Xrcc3 Induces Cisplatin Resistance by Stimulation of Rad51Related Recombinational Repair, S-Phase Checkpoint
Activation, and Reduced Apoptosis
Methotrexate Preconditioning Allows Sufficient Engraftment to
Confer Drug Resistance in Mice Transplanted with Marrow
Expressing Drug-Resistant Dihydrofolate Reductase Activity
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL
Tranilast Prevents the Progression of Experimental Diabetic
Nephropathy through Suppression of Enhanced Extracellular
Matrix Gene Expression
A Farnesoid X Receptor-Small Heterodimer Partner
Regulatory Cascade Modulates Tissue Metalloproteinase
Inhibitor-1 and Matrix Metalloprotease Expression in Hepatic
Stellate Cells and Promotes Resolution of Liver Fibrosis
Stefano Fiorucci, Giovanni Rizzo,
Elisabetta Antonelli, Barbara Renga, Andrea
Mencarelli, LuJsa Riccardi, Stefano Orlandi,
Mark Pruzanski, Antonio Morelli, and Roberto
Pellicciari
584
Functional Selectivity of Nociceptin/Orphanin FQ Peptide
Receptor Partial Agonists on Cardiovascular and Renal
Function
Daniel R. Kapusta, Melissa A. Burmeister,
Girolamo Calo', Remo Guerrini, Helmut B.
Gottlieb, and Velga A. Kenigs
643
Pharmacodynamic Characterization of ZP120 (AcRYYRWKKKKKKK-NH2), a Novel, Functionally Selective
Nociceptin/Orphanin FQ Peptide Receptor Partial Agonist
with Sodium-Potassium-Sparing Aquaretic Activity
Daniel R. Kapusta, Christian Thorkildsen,
Velga A. Kenigs, Eddi Meier, Mette M.
Vinge, Charlotte Quist, and J0rgen
S0berg Petersen
652
Barakol Extracted from Cassia siamea Stimulates Chloride
Secretion in Rat Colon
Cbatsri Deachapunya,
Sutthasinee Poonyachoti,
Watchareewan Thongsaard, and
Nateetip Krishnamra
Trent M. Woodruff, Sandra Pollitt,
Lavinia M. Proctor, Shelli Z. Stocks. Helga D.
Manthey, Hua M. Williams, Indumathy B.
Mahadevan, Ian A. Shiels, and Stephen M.
Taylor
732
Dynamic Activation of Cystic Fibrosis Transmembrane
Conductance Regulator by Type 3 and Type 4D
Phosphodiesterase Inhibitors
Susana Liu, Alain Veilleux, Lei Zhang,
Andrew Young, Evonne Kwok, France
Laliberte, Christine Chung, Michael R.
Tota, Daniel Dube, Richard W. Friesen,
and Zheng Huang
846
Functional Consequences of Single Nucleotide Polymorphisms
in the Human Organic Anion Transporter hOATl (SLC22A6)
Kelly Bleasby, Laura A. Hall,
Jennifer L. Perry,Harvey W. Mohrenweiser, and
John B. Pritchard
923
Maria G. Belvisi, Daniela S. Bundschuh,
Michael Stoeck, Sharon Wicks,
Stephen Underwood, Clifford H. Battram,
El-Bdaoui Haddad, Stephen E. Webber, and
Martyn L. Foster
568
Fiorentina Roviezzo, Stelios Tsigkos,
Anastasia Kotanidou, Mariarosaria Bucci,
Vincenzo Brancaleone, Giuseppe Cirino, and
Andreas Papapetropoulos
Natsuko Kusunoki, Takumi Ito,
Nobuyuki Sakurai, Tom Suguro,
Hiroshi Handa, and Shinichi Kawai
738
Increased Potency of a Novel .Complement Factor 5a Receptor
Antagonist in a Rat Model of Inflammatory Bowel Disease
INFLAMMATION AND IMMUNOPHARMACOLOGY
Preclinical Profile of Ciclesonide, a Novel Corticosteroid for
the Treatment of Asthma
Angiopoietin-2 Causes Inflammation in Vivo by Promoting
Vascular Leakage
A Novel Celecoxib Derivative Potently Induces Apoptosis of
Human Synovial Fibroblasts
NEUROPHARMACOLOGY
j31 Adrenergic Receptor-Mediated Enhancement of
Hippocampal CA3 Network Activity
Functional Characterization of the /3-Adrenergic Receptor
Subtypes Expressed by CA1 Pyramidal Cells in the Rat
Hippocampus
Recognition of Benztropine by the Dopamine Transporter
(DAT) Differs from That of the Classical Dopamine Uptake
Inhibitors Cocaine, Methylphenidate, and Mazindol as a
Function of a DAT Transmembrane 1 Aspartic Acid Residue
JH Opioid Receptor
Coupling to GVo Proteins Increases during
Postnatal Development in Rat Brain
Systemic Morphine Inhibits Dorsal Horn Projection Neurons
through Spinal Cholinergic System Independent of Descending
Pathways
Brain Uptake Kinetics of Nicotine and Cotinine after Chronic
Nicotine Exposure
Chris W. D. Jurgens, Katie E. Rau,
Chris A. Knudson, Jacob D. King,
Patrick A. Carr, James E. Porter, and
Van A. Doze
Kristin L. Hillman, Van A. Doze, and
James E. Porter
811
796
552
561
Okechukwu T. Ukairo, Corry D. Bondi,
Amy Hauck Newman, Santosh S. Kulkarni,
Alan P. Kozikowski, Stephen Pan, and
Christopher K. Surratt
Jeffery N. Talbot, H. Kevin Happc. and
L. Charles Murrin
575
Yan-Ping Chen, Shao-Rui Chen, and
Hui-Lin Pan
611
P. R. Lockman, G. McAfee,
W. J. Geldenhuys, C. J. Van der Schyf, T. J.
Abbruscato, and D. D. Allen
636
596
Quantitative in Vivo Microdialysis Study on the Influence of
Multidrug Transporters on the Blood-Brain Barrier Passage
of Oxcarbazepine: Concomitant Use of Hippocampal
Monoamines as Pharmacodynamic Markers for the
Anticonvulsant Activity
Ralph Clinckers, Use Smolders,
Alfred Meurs, Guy Ebinger, and
Yvette Michotte
725
VPAC2 Receptors Mediate Vasoactive Intestinal PeptideInduced Neuroprotection against Neonatal Excitotoxic Brain
Lesions in Mice
Claire-Marie Rangon, Stephanie Goursaud,
Fadia Medja, Vincent Lelievre, Lourdes
Moiznien, Isabelle Husson, Philippe Brabet,
Sylvie Jegou, Thierry Janet, and Pierre Gressens
745
Yun Liu, Guang-Di Chen, Megan R. Lerner,
Danie! J. Bracken, and Rae R. Matsumoto
770
Carol Hamelink, Aidan Hampson,
David A. Wink, Lee E. Eiden, and
Robert L. Eskay
V. Gonzalez-Nunez, G. Arsequell,
E. Szemenyei, G. Toth, G. Valencia, and R. E.
Rodriguez
780
Barbara Nightingale, Christina M. Dersch,
Terrence L. Boos, Elisabeth Greiner, William J.
Calhoun, Arthur E. Jacobson, Kenner C. Rice,
and Richard B. Rothman
906
Kota Ishida, Mikio Murata,
Nobuyuki Katagiri, Masago Ishikawa, Kenji Abe,
Masatoshi Kato, Iku Utsunomiya, and Kyoji
Taguchi
916
Andrew J. Phimister, Kurt J. Williams,
Laura S. Van Winkle, and
Charles G. Plopper
J. van Grevenynghe, M. Bernard,
S. Langouet, C. Le Berre, T. Fest, and
O. Fardel
506
Cocaine Up-Regulates Fra-2 and tr-1 Receptor Gene and
Protein Expression in Brain Regions Involved in Addiction
and Reward
Comparison of Cannabidiol, Antioxidants, and Diuretics in
Reversing Binge Ethanol-Induced Neurotoxicity
Binding Profile of the Endogenous Novel Heptapeptide MetEnkephalin-Gly-Tyr in Zebrafish and Rat Brain
Studies of the Biogenic Amine Transporters. XI. Identification
of a H2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3phenylpropyDpiperazine (GBR12909) Analog That
Allosterically Modulates the Serotonin Transporter
Effects of J3-Phenylethylamine on Dopaminergic Neurons of
the Ventral Tegmental Area in the Rat: A Combined
Electrophysiological and Microdialysis Study
TOXICOLOGY
Consequences of Abrupt Glutathione Depletion in Murine
Clara Cells: Ultrastructural and Biochemical Investigations
into the Role of Glutathione Loss in Naphthalene Cytotoxicity
Human CD34-Positive Hematopoietic Stem Cells Constitute
Targets for Carcinogenic Polycyclic Aromatic Hydrocarbons
Primaquine-Induced Hemolytic Anemia: Role of Membrane
Lipid Peroxidation and Cytoskeletal Protein Alterations in the
Hemotoxicity of 5-Hydroxyprimaquine
Zachary S. Bowman, Jason D. Morrow,
David J. Jollow, and David C. McMillan
862
693
838
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