The Journal of

PHARMACOLOGY

And Experimental Therapeutics

A Publication of the American Society for Pharmacology and Experimental Therapeutics

November 2007


Vol. 323, No. 2

Contents

PERSPECTIVES IN PHARMACOLOGY

Serotonin (5-HT) in Veins: Not All in Vain


A. Elizabeth Under, Wei Ni, 415

Jessica L. Diaz, Theodora Szasz, Robert Burnett, and Stephanie W. Watts

BEHAVIORAL PHARMACOLOGY

k Agonist-Induced Reinstatement of Cocaine Seeking in Squirrel Monkeys: A Role for Opioid and Stress-Related Mechanisms

Drug and Reinforcement History as Determinants of the Response-Maintaining Effects of Quinpirole in the Rat

CARDIOVASCULAR

Platelet-Endothelial Cell Adhesion Molecule-1 -Directed Endothelial Targeting of Superoxide Dismutase Alleviates Oxidative Stress Caused by Either Extracellular or Intracellular Superoxide

B-9972 (D-Arg-[Hyp3,Igls,Oic7,Igl8]-bradykinin) Is an Inactivation-Resistant Agonist of the Bradykinin B2 Receptor Derived from the Peptide Antagonist B-9430 (D-Arg- [Hyp3,Igr,D-lgl7,Oics] -bradykinin): Pharmacologic Profile and Effective Induction of Receptor Degradation

The Cytochrome P450 Inhibitor Ketoconazole Potentiates 5-Hydroxytryptamine-Induced Contraction in Rat Aorta

Af-Benzyladriamycin-14-valerate (AD 198): A Non-Cardiotoxic Anthracycline That Is Cardioprotective through PKC-e Activation


Glenn R. Valdez, Donna M. Platt, 525

James K. Rowlett, Daniela Ruedi-Bettschen, and Roger D. Spealman

Gregory T. Collins and James H. Woods 599

Vladimir V. Shuvaev, Samira Tliba, 450

Marian Nakada, Steven M. Albelda, and Vladimir R. Muzykantov

Marie-Therese Bawolak, Lajos Gera, 534

Guillaume Morissette, John M. Stewart, and Francois Marceau

Kevin K. Ogden, John R. Falck, and 606

Stephanie W. Watts

Polly A. Hofmann, Mervyn Israel, 658

Yoshihiro Koseki, Jeffrey Laskin,

Joshua Gray, Aleksandra Janik,

Trevor W. Sweatman, and Leonard Lothstein

CELLULAR AND MOLECULAR

The Endogenous Cannabinoid Anandamide Inhibits Cromakalim-Activated K+ Currents in Follicle-Enclosed Xenopus Oocytes

Conversion of Phosphodiesterase-5 (PDE5) Catalytic Site to Higher Affinity by PDE5 Inhibitors


Murat Oz, Keun-Hang Yang, Meral Dine, 547

and Toni S. Shippenberg

Mitsi A. Blount, Roya Zoraghi, 730

Emmanuel P. Bessay, Alfreda Beasley, Sharron H. Francis, and Jackie D. Corbin

CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY Activation of Nonsteroidal Anti-Inflammatory Drug-Activated Gene-1 via Extracellular Signal-Regulated Kinase 1/2 Mitogcn-Activated Protein Kinase Revealed a Isochaihulactone-Triggered Apoptotic Pathway in Human Lung Cancer A549 Cells


Yi-Lin Chen, Po-Cheng Lin, Shee-Ping Chen, Chai-Ching Lin, Nu-Man Tsai, Yeung-Leung Cheng, Wen-Liang Chang, Shinn-Zong Lin, and Horng-Jyh Harn


746

ENDOCRINE AND DIABETES

HI Identification of Novel Orally Available Small Molecule Insulin Mimetics

A Novel Long-Acting Selective Neuropeptide Y2 Receptor Polyethylene Glycol-Conjugated Peptide Agonist Reduces Food Intake and Body Weight and Improves Glucose Metabolism in Rodents


Bo Lin, Zhitao Li, Kaapjoo Park, Liu Deng, 579

Ashok Pai, Ling Zhong, Michael C. Pirrung, and Nicholas J. G. Webster

Aslrid A. Ortiz, Lucinda F. Milardo, 692

Lynn B. DeCarr, Thomas M. Buckholz, Michelle R. Mays, Thomas H. Claus, James N. Livingston, Cathy D. Mahle, and Kevin J. Lumb

GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL Inhibition of Renal Dipeptidyl Peptidase IV Enhances Peptide YYj_3fi-Induced Potentiation of Angiotensin H-Mediated Renal Vasoconstriction in Spontaneously Hypertensive Rats

Differential Down-Regulation of Aquaporin-2 in Rat Kidney Zones by Peripheral Nociceptin/Orphanin FQ Receptor Agonism and Vasopressin Type-2 Receptor Antagonism

Influence of Estrogen and Xenoestrogens on Basolateral Uptake of Tetraethylammonium by Opossum Kidney Cells in Culture

3- [5-(3,4-Dichloro-phenyl)-1 -(4-methoxy-phenyl)- \H -py razol-3-yl]-2-m-tolyl-propionate (JNJ-17156516), a Novel, Potent, and Selective Cholecystokinin 1 Receptor Antagonist: In Vitro and in Vivo Pharmacological Comparison with Dexloxiglumide


Edwin K. Jackson, Mingdi Zhang, Weili Liu, 431

and Zaichuan Mi

Niels Hadrup, J0rgen S. Petersen, 516

S0ren Windfeld, Lotte Risom, Claus B. Andersen, S0ren Nielsen, Slen Christensen, and Thomas E. N. Jonassen

Ryan M. Pelis, Randall C. Hartman, 555

Stephen H. Wright, Theresa M. Wunz, and Carlotta E. Groves

Magda F. Morton, Terrance D. Barrett, 562

Wen Yan, Jamie M. Freedman, Guy Lagauci,

Clodagh E. Prendergast, Veronica Moreno,

Jayashree Pyati, Katherine Figueroa, Lina Li,

Xiaodong Wu, Michele Rizzolio,

James G. Breitenbucher, Kelly McChire, and

Nigel P. Shankley

INFLAMMATION, IMMUNOPHARMACOLOGY, AND ASTHMA Brain Penetration of the Oral Immunomodulatory Drug FTY720 and Its Phosphorylation in the Central Nervous System during Experimental Autoimmune Encephalomyelitis: Consequences for Mode of Action in Multiple Sclerosis

Pharmacology and Antitussive Efficacy of 4-(3-Trifluoromethyl-pyridin-2-yl)-piperazine-l-carboxylic Acid (5-Trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a Transient Receptor Potential Vanilloid 1 Antagonist in Guinea Pigs

Modulation of Airway Responses to Influenza A/PR/8/34 by A9-Tetrahydrocannabinol in C57BL/6 Mice


Carolyn A. Foster, Laurence M. Howard, 469

Alain Schweitzer, Elke Persohn, Peter C. Hiestand, Balazs Balatoni, Roland Reuschel, Christian Beerli, Manuela Schwartz, and Andreas Billich

Anindya Bhattacharya, Brian P. Scott, 665

Nadia Nasser, Hong Ao, Michael P. Maher, Adrienne E. Dubin, Devin M. Swanson, Nigel P. Shankley, Alan D. Wickenden, and Sandra R. Chaplan

John P. Buchweitz, Peer W. F. Karmaus, 675

Jack R. Harkema, Kurt J. Williams, and Norbert E. Kaminski

METABOLISM, TRANSPORT, AND PHARMACOGENOMICS

Human Renal Cortical and Medullary UDP-Glucuronosyltransferases (UGTs): Immunohistochemical Localization of UGT2B7 and UGT1A Enzymes and Kinetic Characterization of S-Naproxen Glucuronidation


Paraskevi Gaganis, John O. Miners, James S. Brennan, Anthony Thomas, and Kathleen M. Knights


422

CYP2A13: Variable Expression and Role in Human Lung Microsomal Metabolic Activation of the Tobacco-Specific Carcinogen 4-(Methylnitrosamino)-l-(3-pyridyl)-l-butanone

Positive and Negative Regulation of Human Hepatic Hydroxysteroid Sulfotransferase (SULT2A1) Gene Transcription by Rifampicin: Roles of Hepatocyte Nuclear Factor 4a; and Pregnane X Receptor


Xiiiling Zhang, Jaime D'Agostino,

Hong Wu, Qing-Yu Zhang,

Linda von Weymarn, Sharon E. Murphy, and

Xinxin Ding

Hai-Lin Fang, Stephen C. Strom, Ewa Ellis, Zhengbo Duanmu, Jiaqi Fu, Zofia Duniec-Dmuchowski, Charles N. Falany, Josie L. Falany, Thomas A. Kocarek, and Melissa Runge-Morris


570

586

NEUROPHARMACOLOGY

Activity-Dependent Neuroprotective Protein Snippet NAP Reduces Tau Hyperphosphorylation and Enhances Learning in a Novel Transgenic Mouse Model

Prolonged Attenuation of Amygdala-Kindled Seizure Measures in Rats by Convection-Enhanced Delivery of the N-Type Calcium Channel Antagonists o>-Conotoxin GVIA and w-Conotoxin MVIIA

3,4-Methylenedioxymethamphetamine- and 8-Hydroxy-2-di-«-propylamino-tetralin-Induced Hypothermia: Role and Location of 5-Hydroxytryptamine 1A Receptors

Cyclooxygenase Inhibition Limits Blood-Brain Barrier V Disruption following Intracerebral Injection of Tumor Necrosis Factor-a in the Rat

Expression of Cannabinoid CB, Receptors in Models of Diabetic Neuropathy

A Select Set of Opioid Ligands Induce Up-Regulation by Promoting the Maturation and Stability of the Rat K-Opioid Receptor in Human Embryonic Kidney 293 Cells

The Immunomodulator FTY720 Has a Direct Cytoprotective Effect in Oligodendrocyte Progenitors

Regulator of G-Protein Signaling 4 Interacts with Metabotropic Glutamate Receptor Subtype 5 in Rat Striatum: Relevance to Amphetamine Behavioral Sensitization

Ethanol Sensitivity of GABAergic Currents in Cerebellar Granule Neurons Is Not Increased by a Single Amino Acid Change (R100Q) in the a6 GABAA Receptor Subunit

jx-Opioid Receptor Up-Regulation and Functional Supersensitivity Are Independent of Antagonist Efficacy

Pharmacological Characterization of a Novel, Potent Adenosine At and A3A Receptor Dual Antagonist, 5-[5-Amino-3-(4-fluorophenyl)py razin-2-y 1] -1 -isopropylpy ridme-2(lH)-one (ASP5854), in Models of Parkinson's Disease and Cognition

Desvenlafaxine Succinate Identifies Novel Antagonist Binding Determinants in the Human Norepinephrine Transporter

Methylphenidate Administration Alters Vesicular Monoamine Transporter-2 Function in Cytoplasmic and Membrane-Associated Vesicles


Inna Vulih-Shultzman, Albert Pinhasov, 438

Shmuel Mandel, Nikolaos Grigoriadis, Olga Touloumi, Zipora Pittel, and Illana Gozes

Maciej Gasior, Natalie A. White, and 458

Michael A. Rogawski

Daniel E. Rusyniak, Maria V. Zaretskaia, 477

Dmitry V. Zaretsky, and Joseph A. DiMicco

Eduardo Candelario-Jalil, Saeid Taheri, 488

Yi Yang, Rohit Sood, Mark Grossetete, Eduardo Y. Estrada, Bernd L. Fiebich, and Gary A. Rosenberg

Fan Zhang, Shuangsong Hong, Vicki Stone, 508

and Paula J. W. Smith

Kenneth M. Wannemacher, Prem N. Yadav, 614

and Richard D. Howells

Rochelle P. Coelho, Shawn G. Payne, 626

Robert Bittman, Sarah Spiegel, and Carmen Sato-Bigbee

Marek Schwendt and Jacqueline F. McGinty 650

Paolo Botta, Manuel Mameli, 684

Kirsten L. Floyd, Richard A. Radcliffe, and C. Fernando Valenzuela

Sunil Sirohi, Priyank Kumar, and 701

Byron C. Yoburn

Takuma Mihara, Kayoko Mihara, 708

Junko Yarimizu, Yasuyuki Mitani,

Ritsuko Matsuda, Hiroko Yamamoto,

Satoshi Aoki, Atsushi Akahane,

Akinori Iwashita, and

Nobuya Matsuoka

John N. Mason, Darlene C. Deecher, 720

Rhonda L. Richmond, Gary Stack, Paige E. Mahaney, Eugene Trybulski, Richard C. Winneker, and Randy D. Btakely

Trent J. Volz, Sarah J. Farnsworth, 738

Jill L. King, Evan L. Riddle, Glen R. Hanson, and Annette E. Fleckenstein

TOXICOLOGY

Mitochondrial Complex I Inhibitor Rotenone-Elicited Dopamine Redistribution from Vesicles to Cytosol in Human Dopaminergic SH-SY5Y Cells


Masahiko Watabe and Toshio Nakaki


499

Mitochondrially Targeted Effects of Berberine [Natural Yellow 18, 5,6-dihydro-9,10-dimethoxybenzo(£)-l,3-benzodioxolo(5,6-a)quinolizinium] on K1735-M2 Mouse Melanoma Cells: Comparison with Direct Effects on Isolated Mitochondria! Fractions


Goncalo C. Pereira, Ana F. Branco, Julio A. C. Matos, Sandro L. Pereira, Donna Parke, Edward L. Perkins, Teresa L. Serafim, Vilma A. Sardao, Maria S. Santos, Antonio J. M. Moreno, Jon Holy, and Paulo J. Oliveira


636

ERRATUM

Correction to "Lysophosphatidic Acid Decreases Epidermal Growth Factor Receptor Binding in Airway Epithelial Cells"


757