316_02_2006

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The Journal of

PHARMACOLOGY

And Experimental Therapeutics

A Publication of the American Society for Pharmacology and Experimental Therapeutics

February 2006 Vol.316, No. 2

Contents

PERSPECTIVES IN PHARMACOLOGY

Striatal a6* Nicotinic Acetylcholine Receptors: Potential

Targets for Parkinson's Disease Therapy

Maryka Quik and J. Michael Mclntosh 481

ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION

Nucleoside Ester Prodrug Substrate Specificity of Liver

Carboxylesterase

Christopher P. Landowski, Philip L. Lorenzi, 572

Xueqin Song, and Gordon L. Amidon

In Vivo Evaluation of P-glycoprotein Function at the Blood-

Brain Barrier in Nonhuman Primates Using [ T1 C]Verapamil

Young-Joo Lee, Jun Maeda, 647

Hiroyuki Kusuhara, Takashi Okauchi,

Motoki Inaji, Yuji Nagai, Shigeru Obayashi,

Ryuji Nakao, Kazuloshi Suzuki, Yuichi

Sugiyama, and Tetsuya Suhara

Yvonne Y. Lau, Hideaki Okochi,

Yong Huang, and Leslie Z. Benet

762 Multiple Transporters Affect the Disposition of Atorvastatin and Its Two Active Hydroxy Metabolites: Application of in

Vitro and ex Situ Systems

Repression of Cytochrome P450 Activity in Human

Hepatocytes in Vitro by a Novel Hepatotrophic Factor,

Augmenter of Liver Regeneration

The Lymph Lipid Precursor Pool Is a Key Determinant of

Intestinal Lymphatic Drug Transport

Wolfgang E. Thasler, Rania Dayoub,

Marcus Muhlbauer, Claus Hellerbrand,

Thomas Singer, Anja Grabe,

Thomas S. Weiss

Karl-Walter Jauch, Hans-Jiirgen Schlitt, and

822

881 Natalie L. Trevaskis,

Christopher J. H. Porter, and

William N. Charman

BEHAVIORAL PHARMACOLOGY

Differential in Vivo Potencies of Naltrexone and 6/3-NaltrexoI in the Monkey

772

Analysis of the Antinociceptive Effect of the Flavonoid

Myricitrin: Evidence for a Role of the L-Arginine-Nitric Oxide and Protein Kinase C Pathways

High-Efficacy 5-Hydroxytryptamine 1A Receptor Activation

Counteracts Opioid Hyperallodynia and Affective

Conditioning

Differential Gender-Related Vulnerability to Depression

Induction and Converging Antidepressant Responses in Rats

M. C. Holden Ko, Mary F. Divin,

Heeseung Lee, James H. Woods, and

John R. Traynor

Flavia Carla Meotti, Ana Paula Luiz,

Moacir Geraldo Pizzolatti,

Candida A. L. Kassuya, Joao B. Calixto, and

Adair R. S. Santos

Francis C. Colpaert, Kristof Deseure,

Luis Stinus, and Hugo Adriaensen

Miao-Kun Sun and Daniel L. Alkon

789

892

926

CARDIOVASCULAR

Neuronal Nitric-Oxide Synthase Inhibition Facilitates

Adrenergic Neurotransmission in Rat Mesenteric Resistance

Arteries

[s] QT Prolongation Modifies Dynamic Restitution and Hysteresis of the Beat-to-Beat QT-TQ Interval Relationship during

Normal Sinus Rhythm under Varying States of Repolarization

MRS2500 L2-Iodo-M > -methyl-(,V)-methanocarba-2'deoxyadenosine-3',5'-bispliosphate], a Potent, Selective, and

Stable Antagonist of the Platelet PlYy Receptor with Strong

Antithrombotic Activity in Mice

Effects of Phytoestrogens on Sarcoplasmic/Endoplasmic

Reticulum Calcium ATPase 2a and Ca 2+ Uptake into Cardiac

Sareoplasmic Reticulum

Differential Effects of the Phosphodiesterase Type 5 Inhibitors

Sildenafil, Vardenafil, and Tadalafil in Rat Aorta

Role of Hydrogen Sulfide in the Cardioprotection Caused by

Ischemic Preconditioning in the Rat Heart and Cardiac

Myocytes

Tachycardia Caused by A

2A

Adenosine Receptor Agonists Is

Mediated by Direct Sympathoexcitation in Awake Rats

Sphingosine 1-Phosphate Induces Endothelial Nitric-Oxide

Synthase Activation through Phosphorylation in Human

Corpus Cavernosum

An Increase in Late Sodium Current Potentiates the

Proarrhythmic Activities of Low-Risk QT-Prolonging Drugs in

Female Rabbit Hearts

In Vivo Cardiac Electrophysiologic Effects of a Novel

Diphenylphosphine Oxide I

Kur

Blockcr, (2-Isopropyl-5methylcyclohexyl) Diphenylphosphine Oxide, in Rat and

Nonhuman Primate

Attenuation of Vascular Smooth Muscle Cell Proliferation by l-

Cyclohexyl-3-dodecyl Urea Is Independent of Soluble Epoxidc

Hydrolase Inhibition

Mesenteric Vasoconstriction and Hindquarters Vasodilatation

Accompany the Pressor Actions of Exendin-4 in Conscious

Rats

CELLULAR AND MOLECULAR

Mapping the Binding Site of Six Nonpeptide Antagonists to the

Human V

2

-Renal Vasopressin Receptor

Dominant Role for Calpain in Thromboxane-Induced

Neuromicrovascular Endothelial Cytotoxicity

Antimelanoma Activity of Apoptogenic Carbonyl Scavengers

Oxymetazoline Inhibits Proinflammatory Reactions: Effect on

Arachidonic Acid-Derived Metabolites

Direct Block of Human Ether-a-go-go -Related Gene Potassium

Channels by Caffeine

CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY

DNA Repair Enzyme, O rt -Methylguanine DNA

Methyltransferase, Modulates Cytotoxicity of Camptothccin-

Derived Topoisomerase I Inhibitors

Yukako Hatanaka, Nariimi Hobara,

Jin Honghua, Shinji Akiyama, Hideki Nawa,

Yuta Kobayashi, Fusako Takayama, Yutaka

Gomita, and Hiromu Kawasaki

Anthony A. Fossa, Todd Wisialowski, and

Kimberly Crimin

Beatrice Hechler, Christelle Nonnc.

Eun Joo Roh, Marco Catlaneo, Jean-Pierre

Cazenave, Francois Lanza, Kenneth A.

Jacobson. and Christian Gachet

Marnie L. Olson, Margaret E. Kargacin,

Thomas W. Honeyman,

Christopher A. Ward, and Gary J. Kargacin

Clebcr E. Teixcira, Fernanda B. M. Priviero, and R. Clinton Webb

Jin-Song Bian, Qian Chen Yong,

Ting-Ting Pan, Zhan-Ning Feng,

Muhammed Yusuf Ali, Shufeng Zhou, and

Philip Keith Moore

Arvinder K. Dhalla, Mei-Yee Wong,

Wei-Qun Wang, Italo Biaggioni, and

Luiz Belardinelli

Roberta d'Emmanuele di Villa Bianca,

Raffaella Sorrentino, Rosalinda Sorrentino,

Ciro Imbimbo, Alessandro Pahnieri,

Ferdinando Fusco, Mario Maggi,

Raffaele De Palma, Giuseppe Cirino, and

Vincenzo Mirone

Lin Wu, John C. Shryock, Yejia Song, and

Luiz, Belardinelli

Christopher P. Regan, Audrey A. Wallace,

Hillary K. Cresswell, Charity L. Atkins, and

Joseph J. Lynch, Jr.

Benjamin B. Davis, Christophe Morisseau,

John W. Newman, Theresa L. Pederscn,

Bruce D. Hammock, and Robert H. Weiss

Sheila M. Gardiner, Julie E. March,

Philip A. Kemp, and Terence Bennett

Rosemarie Macian-Dazard,

Nicholas Callahan, Zhen Xu, Nan Wu, Marc

Thibonnier, and Menachcm Shonam

Chrisliane Quiniou, Florian Sennlaub,

Martin H. Beauchamp, Daniella Checchin,

Isabelle Lahaic, Sonia Brault,

Fernand Gobeil, Jr., Mirna Sirinyan,

Amna Kooli, Pierre Hardy,

Alexey Pshezhetsky, and Sylvain Chemtob

Georg T. Wondrak, Myron K. Jacobson, and

Elaine L. Jacobson

Ingrid Beck-Speier, Niru Dayal, Erwin Karg,

Konrad L. Maier, Gabrielc Schumann,

Manuela Semmler, and Stephan M. Koelsch

S. L. Cockeriil and J. S. Mitcheson

Ching-Chuan Kuo, Jin-Fen Liu, and

Jang-Yang Chang

564

618

805

843

860

946

628

654

670

695

703

490

498

556

718

727

815

852

ENDOCRINE AND DIABETES

Blood Glucose-Lowering Nuclear Receptor Agonists Only

Partially Normalize Hepatic Gene Expression in db/db Mice

Michael Loffler, Martin Bilban,

Mark Reimers, Werner Waldhausl, and

Thomas M. Slulnig

GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

Adenosine Al Receptor Antagonist Blunts Urinary Potassium

Excretion, but Not Renal Hemodynamic Effects, Induced by

Carbonic Anhydrase Inhibitor in Rats

Roles of Cyclooxygenase-2 and Prostacyclin/IP Receptors in

Mucosal Defense against Ischemia/Reperfusion Injury in

Mouse Stomach

Critical Role of Plasminogen Activator Inhibitor-1 in

Cholestatic Liver Injury and Fibrosis

Genetic Variants of the Human Dipeptide Transporter PEPT1

Xiaosun Zhou and Curtis K. Kost, Jr.

Tohru Kotani, Atsushi Kobata,

Eiji Nakamura, Kikuko Amagase, and

Koji Takeuchi

Ina Bergheim, Luping Guo,

Molly Anne Davis, Ilinca Duveau, and

Gavin E. Arteel

Paseale Anderle, Carsten Uhd Nielsen, Julia

Pinsonneault, Pernille Lindskov Krog,

Birger Brodin, and Wolfgang Sad6e

Rong-Jyh Lin, Bin-Nan Wu, Yi-Ching Lo,

Li-Mei An, Zen-Kong Dai, Young-Tso Lin,

Chao-Shun Tang, and Ing-Jun Chen

A Xanthine-Based Epithelium-Dependent Airway Relaxant

KMUP-3 {7-[2-[4-(4-Nitrobenzene)piperazinyl]ethyl]-l,3dimethylxanthine) Increases Respiratory Performance and

Protects against Tumor Necrosis Factor-a-Induced Tracheal .

Contraction, Involving Nitric Oxide Release and Expression of cGMP and Protein Kinase G

Sex Differences in the mRNA, Protein, and Functional

Expression of Organic Anion Transporter (Oat) 1, Oat3, and

Organic Cation Transporter (Oct) 2 in Rabbit Renal Proximal

Tubules

The Relaxant Activity of 4,7-Dimethyl-l,2,5-oxadiazolo[3,4-

(flpyridazine 1,5,6-Trioxide in the Mouse Corpus Cavernosum

M

2

and M

3

Muscarinic Receptor Activation of Urinary

Bladder Contractile Signal Transduction. I. Normal Rat

Bladder

M

2

and M

3

Muscarinic Receptor Activation of Urinary

Bladder Contractile Signal Transduction. II. Denervated Rat

Bladder

Selective Inhibition of Phosphodiesterase-4 Ameliorates

Chronic Colitis and Prevents Intestinal Fibrosis

Carlotta E. Groves, Wendy B. Suhre,

Nathan J. Cherrington, and Stephen H.

Wright

Cemil Gormen, H. Sinem Buyiiknacar,

Alexander Ya Kots, Fend Murad, Olcay

Kiroglu, and Eda Karabal Kumcu

Alan S. Braverman, Amit S. Tibb, and

Michael R. Ruggieri, Sr.

Alan S. Braverman, Leo R. Doumanian. and

Michael R. Ruggieri, Sr.

S. Videla, J. Vilaseca, C. Medina,

M. Mourelle, F. Guarner, A. Salas, and

J.-R. Malagelada

INFLAMMATION AND IMMUNOPHARMACOLOGY

Inhibition of Leukocyte Elastase, Polymorphonuclear

Chemoinvasion, and Inflammation-Triggered Pulmonary

Fibrosis by a 4-Alkyliden-/j{-Iactam with a Galloyl Moiety

Periplocoside E, an Effective Compound from Periploca

sepium Bge, Inhibited T Cell Activation in Vitro and in Vivo

A Novel Cannabinoid Peripheral Cannabinoid Receptor-

Selective Inverse Agonist Blocks Leukocyte Recruitment in

Vivo

Isabella Dell'Aica, Luigi Sartor, Paola

Galletti, Daria Giacomini, Arianna

Quintavalla, Fiorella Calabrese, Cinzia

Giacometti. Enrico Brunetta, Francesco

Piazza, Carlo Agostini, and Spiridione

Garbisa

Yi-Na Zhu, Wei-Min Zhao, Yi-Fu Yang,

Qun-Fang Liu, Yu Zhou, Jia Tian, Jia Ni,

Yun-Feng Fu, Xiang-Gcn Zhong. Wei Tang,

Ru Zhou, Pti-Lan He, Xiao-Yu Li, and

Jian-Ping Zuo

Charles A. Lunn, Jay S. Fine,

Alberto Rojas-Triana, James V. Jackson,

Xuedong Fan, Ted T. Kung,

Waldemar Gonsiorek, Martin A. Schwarz,

Brian Lavey, Joseph A. Kozlowski,

Satwant K. Narula, Daniel J. Lundell,

R. William Hipkin, and Loretta A. Bober

Nahid A. Shahabi, Kathy McAllen, and

Bnrt M. Sharp

5 Opioid Receptors Stimulate Akt-Dependent Phosphorylation of c-jun in T Cells

NEUROPHARMACOLOGY

5-Hydroxytryptamine 1A Receptor Blockade Facilitates

Aversive Learning in Mice: Interactions with Cholinergic and

Glutamatergic Mechanisms

Nather Madjid, Elin Elvander Tottie, Maria

LuLlgen, Bjorn Meister, Johan Sandin,

Alexander Kuzmin, Oliver Stiedl, and Sven

Ove Ogren

797

539

662

780

933

581

530

547

592

636

709

743

753

869

875

940

Different Effects of Opioid and Cannabinoid Receptor

Agonists on C-Fiber-Induced Extracellular Signal-Regulated

Kinase Activation in Dorsal Horn Neurons in Normal and

Spinal Nerve-Ligated Rats

Effects of Exogenous and Endogenous Cannabinoids on

GABAergic Neurotransmission between the Caudate-Putamen and the Globus Pallidus in the Mouse

Comparison of Galantamine and Donepezil for Effects on

Nerve Growth Factor, Cholinergic Markers, and Memory

Performance in Aged Rats

Presynaptic a x

Adrenergic Receptors Differentially Regulate

Synaptic Glutamate and GABA Release to Hypothalamic

Presympathetic Neurons

D2-Like Receptors Mediate the Expulsion Phase of

Ejaculation Elicited by 8-Hydroxy-2-(di-JVpropylamino)tetralin in Rats

Apolipoprotein E-Derived Peptides Block «7 Neuronal

Nicotinic Acetylcholine Receptors Expressed in Xenopus

Oocytes

Characterization of Opioid-Binding Sites in Zebrafish Brain

Improved Bioavailability of the mGlu2/3 Receptor Agonist

LY354740 Using a Prodrug Strategy: In Vivo Pharmacology of

LY544344

Iptakalim as a Human Nicotinic Acetylcholine Receptor

Antagonist

Novel Compounds That Interact with Both Leukotriene B

4

Receptors and Vanilloid TRPV1 Receptors

Yasuhiko Kawasaki, Tatsuro Kohno, and

Ru-Rong Ji

Birgit Engler, Ilka Freiman,

Michal Urbanski, and Bela Szabo

C. M. Hernandez, D. A. Gearhart, V. Parikh,

E. J. Hohnadel, L. W. Davis,

M. L. Middlemore, S. P. Warsi, J. L. Waller, and A. V. Terry, Jr.

Qian Chen, De-Pei Li, and Hui-Lin Pan

Pierre Clement, Jacques Bernabe,

Hosein Kami Kia, Laurent Alexandre, and

Francois Giuliano

Elaine A. Gay, Rebecca C. Klein, and

Jerrel L. Yakel

Veronica Gonzalez-Nunez,

Alejandro Barrallo, John R. Traynor, and

Raquel E. Rodriguez

Linda M. Rorick-Kehn, Everett J. Perkins,

Karen M. Knitowski, John C. Hart,

Bryan G. Johnson, Darryle D. Schoepp, and

David L. McKinzie

Jim Hu, Kari Lindenberger, Gang Hu,

Hai Wang, Ronald J. Lukas, and Jie Wu

Douglas McHugh, R. Shannon McMaster,

Roger G. Pertwee, Sucharita Roy, Anu

Mahadevan, Raj K. Razdan, and Ruth

A. Ross

TOXICOLOGY

Protective Effect of Type 2 Diabetes on Acetaminophen-

Induced Hepatotoxicity in Male Swiss-Webster Mice

Pulmonary Bronchiolar Cytotoxicity and Formation of

Dichloroacetyl Lysine Protein Adducts in Mice Treated with

Trichloroethylene

LETTERS TO THE EDITOR

Comments on "Shift from Biliary to Urinary Elimination of

Acetaminophen-Glucuronide in Acetaminophen-Pretreated

Rats"

Sharmilee P. Sawant, Ankur V. Dnyanmote,

Mayurranjan S. Mitra, Jaya Chilakapati,

Alan Warbritton, John R. Latendresse, and

Harihara M. Mehendale

Poh-Gek Forkert, Brandie Millen,

Lawrence H. Lash, David A. Putt, and

Burhan I. Ghanayem

K. Allegaert and D. Tibboel

601

608

679

914

955

507

520

966

733

830

835

900

905

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