Download 309_02_2004

The Journal of
PHARMACOLOGY
And Experimental Therapeutics
A Publication of the American Society for Pharmacology and Experimental Therapeutics
May 2004
Vol. 309, No. 2
Contents
PERSPECTIVES IN PHARMACOLOGY
Academic Pharmacologists: Confronting New Challenges in
Edward D. French
Educational Programs of Graduate and Health Care Professionals
469
720
ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION
Brain Uptake of the Glucagon-Like Peptide-1 Antagonist
730
Exendin(9-39) after Intranasal Administration
William A. Banks, Matthew J. During, and
Age-Related Differences in CYP3A Expression and Activity in the Michael L. Niehoff
Rat Liver, Intestine, and Kidney
Jill S. Warrington, David J. Greenblatt, and
The Effect of Age on P-Glycoprotein Expression and Function in Lisa L. von Moltke
the Fischer-344 Rat
Jill S. Warrington, David J. Greenblatt, and
Lisa L. von Moltke
BEHAVIORAL PHARMACOLOGY
650
The Discriminative Stimulus Effects of -y-Hydroxybutyrate and
Related Compounds in Rats Discriminating Baclofen or Diazepam: L. P. Carter, A. W. Unzeitig, H. Wu,
The Role of GABAB and GABAA Receptors
W. Chen, A. Coop, W. Koek, and
C. P. France
Effects of iV-Substituted Analogs of Benztropine: Diminished
Cocaine-Like Effects in Dopamine Transporter Ligands
Jonathan L. Kalz, Theresa A. Kopajtic.
Gregory E. Agoston, and Amy Hauck
CARDIOVASCULAR
Newman
490
An Antiarrhythmic Effect of a Chymase Inhibitor after
Myocardial Infarction
Denan Jin, Shinji Takai, Masato Sakaguchi, Yukiko
Okamoto, Michiko Muramatsu, and Mizuo
Pharmacological Characterization of N-tert-ftutyl~N'-[2-(<l'Miyazaki
methylphenylamino)-5-nitrobenzenesulfonyl]urea (BM-573), a
Jean-Michel Dogne, Julien Hanson, Xavier de Leval, 498
Novel Thromboxane A2 Receptor Antagonist and
Philippe Kolh, Vincent Tchana-Sato,
Thromboxane Synthase Inhibitor in a Rat Model of Arterial
Laurence de Leva!, Stephanie Rolin,
Thrombosis and Its Effects on Bleeding Time
Alexandre Ghuysen, Patrick Segers,
Bernard Lambermont, Bernard Masereel,
and Bernard Pirotte
Risk of Ventricular Proarrhythmia with Selective Opening of
the Myocardial Sarcolemmal versus Mitochondrial ATP554
Peter S. Fischbach, Andrew White, Terrance D.
Gated Potassium Channel
Barrett, and Benedict R. Lucchesi
Cardioprotection of Interleukin-2 Is Mediated via K-Opioid
560
Chun-Mei Cao, Qiang Xia, Jie Tu,
Receptors
Mai Chen, Song Wu, and Tak-Ming Wong
Atypical p-Adrenoceptor Subtypes Mediate Relaxations of
Rabbit Corpus Cavernosum
Cleber E. Teixeira, Juliana S. Baracat,
587
Angelina Zanesco,Adson Antunes and
Gilberto De Nucci
Kokichi Suzuki, Yuko Muto,
Kenichi Fushihara, Ken-ichi Kanemoto,
Hiroyuki Iida, Eriko Sato, Chika Kikuchi,
Tetsuya Matsushima, Emiko Kato,
Masahiro Nomoto, Shin Yoshioka, and
Hidemi Ishii
Kenji Okajima, Naoaki Harada,
Mitsuhiro Uchiba, and Hirotaka Isobe
607
Specific Endothetin ETA Receptor Antagonism Does Not
Modulate Insulin-Induced Hemodynamic Effects in the
Human Kidney, Eye, or Forearm
Anna Rab, Susanne Dallinger, Kaija Polak,
Johannes Pleiner, Elzbieta Polska, Michael
Wolzt, and Leopold Schmetterer
692
Immune Cell Regulation and Cardiovascular Effects of
Sphingosine 1-Phosphate Receptor Agonists in Rodents Are
Mediated via Distinct Receptor Subtypes
M. Forrest, S.-Y. Sun, R. Hajdu,
J. Bergstrom, D. Card, G. Doherty, J. Hale,
C. Keohane, C. Meyers, J. Milligan,
S. Mills, N. Nomura, H. Rosen,
M. Rosenbach, G.-J. Shei, I. I. Singer,
M. Tian, S. West, V. While, J. Xie,
R. L. Proia, and S. Mandala
758
Histamine H, and H2 Receptor Gene and Protein Levels Are
Differentially Expressed in the Hearts of Rodents and
Humans
Naoyuki Matsuda, Subrina Jesmin,
Yoshika Takahashi, Eiicbiro Hatta,
Masanobu Kobayashi, Kazuto Matsuyama,
Nozomi Kawakami, Ichiro Sakuma,
Satoshi Gando, Hiyoyuki Fukui,
Yuichi Hattori, and Roberto Levi
786
5-Hydroxytryptamine,n Receptor-Mediated Contraction of
Rabbit Saphenous Vein and Basilar Artery: Role of Vascular
Endothelium
The Fenfluramine Metabolite (+)-Norfenfluramine Is
Vasoactive
Anindya Bhattacharya, Kathryn W. Schenck,
Yao-Chang Xu, Laura Nisenbaum, Elizabeth
Galbreath, and Marlene L. Cohen
Wei Ni, Melissa W. Li, Keshari Thakali,
Gregory D. Fink, and Stephanie W. Watts
825
Enhancement of Fibrinolysis by EF626S ((S)-7-Amino-2-[[[(«)2-methyl-l-(3-phenylpropanoylamino)propyl]
hydroxyphosphinoyl]methyl]heptanoic Acid), a Specific
Inhibitor of Plasma Carboxypeptidase B
Activation of Capsaicin-Sensitive Sensory Neurons by
Carvedilol, a Nonselective 6-Blocker, in Spontaneous
Hypertensive Rats
CELLULAR AND MOLECULAR
Evidence for Multiple P2Y Receptors in T rabecular
Meshwork Cells
Pharmacological and Signaling Properties of Endogenous
P2Y1 Receptors in Cystic Fibrosis Transmembrane
Conductance Regulator-Expressing Chinese Hamster Ovary
Cells
Oxidation of Protein Tyrosine Phosphatases as a
Pharmaceutical Mechanism of Action: A Study Using 4Hydroxy-3,3-dimethyl-2//-benzoIg]indole-2,5(3i/>Dione
Prostaglandin Ethanolamides (Prostamides): In Vitro
Pharmacology and Metabolism
684
845
Craig E. Crosson, Phillip W. Yates,
Aruna N. Bhat, Yurii V. Mukhin, and
Shahid Husain
Brice Marcet, ValSrie Chappe,
Patrick Delmas, and Bernard Verrier
484
Charlotta Liljebris, Pawel Baranczewski,
Eva Bjorkstrand, Styrbjorn Bystrom,
Bo Lundgren, Agneta Tjernberg, Malin
Warolen, and Stephen R. James
711
I. Matias, J. Chen, L. De Petrocellis,
T. Bisogno, A. Ligresti, F. Fezza,
A.H.-P. Krauss, L. Shi, C. E. Protzman,
C. Li, Y. Liang, A. L. Nieves, K. M. Kedzie,
R. M. Burk, V. Di Marzo, and
D. F. Woodward
745
Daniela A. Eisinger and RUdiger Schulz
776
Charlene R. Johnson, Jiong Chun,
Robert Bittman, and W. David Jarvis
452
Qiwei Zhang, David W. Ohannesian, and
Leonard C. Erickson
506
Amanda P. Struckhoff, Robert Bittman,
Matthew E. Burow, Sanda Clejan,
Steven Elliott, Timothy Hammond, Yan
Tang, and Barbara S. Beckman
523
Edward A. Neuwelt, Michael A. Pagel,
Dale F. Kraemer, Darryl R. Peterson, and
Leslie L. Muldoon
594
533
Extracellular Signal-Regulated Kinase/Mitogen-Activated
Protein Kinases Block Internalization of 5-Opioid Receptors
CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY
Intrinsic Cytotosicity and Chcmomodulatory Actions of Novel
Phenethylisothiocyanate Sphingoid Base Derivatives in HL-60
Human Promyelocytic Leukemia Cells
Hammerhead Ribozyme-Mediated Sensitization of Human
Tumor Cells after Treatment with l,3-Bis(2-chloroethyl)-lnitrosourea
Novel Ceramide Analogs as Potential Chemotherapeutic
Agents in Breast Cancer
Bone Marrow Chemoprotection without Compromise of
Chemotherapy Efficacy in a Rat Brain Tumor Model
ENDOCRINE AND REPRODUCTIVE
Robert N. Pechnick and Russell E. Poland
515
David E. Potter, Karen R. M. Russell, and
Marlina Manhiani
548
Shuhei Tomimoto, Hitoshi Hashimoto,
Norihito Shintani, Kyohei Yamamoto, Yuki
Kawabata, Ken-Ichi Hamagami, Kazuya
Yamagata, Jun-Ichiro Miyagawa, and
Akemichi Baba
796
Niel C. Hoglen, Long-Shiuh Chen,
Craig D. Fisher, Brad P. Hirakawa, Todd
Groessl, and Patricia C. Contreras
634
Tumor Necrosis Factor-a-Induced Cytokine-Induced
Neutrophil Chemoattractant-1 (CINC-1) Production by Rat
Gastric Epithelial Cells: Role of Reactive Oxygen Species and
Nuclear Factories
Osamu Handa, Yiiji Naito, Tomohisa Takagi,
Makoto Shimozawa, Satoshi Kokura,
Norimasa Yoshida, Hirofumi Matsui,
Gediminas Cepinskas, Peter R. Kvietys, and
Toshikazu Yoshikawa
670
Role of Adenosine A2A Receptor in the Regulation of Gastric
Somatostatin Release
Linda Yip and Yin Nam Kwok
804
Genya Gekker, Shuxian Hu,
Mark P. Wentland, Jean M. Bidlack, James
R. Lokensgard, and Phillip K. Peterson
600
John L. Wallace,
Marcelo N. Muscarl, Gilberto de Nucci,
Stella Zamuner, Giuseppe Cirino, Piero del
Soldato, and Ennio Ongini
626
Jean Gougat, Bernard Ferrari, Lionel Sarran,
Claudine Planchenault, Martine Poncelet,
Jeanne Maruani, Richard Alonso,
Annie Cudennec, Tiziano Croci,
Fabio Guagnini, Katalin Urban-Szabo,
Jean-Pierre MartinoIIe,
Philippe Soubrie, Olivier Finance, and
Gerard Le Fur
661
Cuifen Hou, Thomas Kirchner,
Monica Singer, Michele Matheis, Dennis
Argentieri, and Druie Cavender
697
Chang Seok Park, Hyun Lim, Kee Jung Han,
Sun Heum Baek, Hyung Ok Sohn, Dong
Wook Lee, Yang-Gyun Kim, Hye-Young
Yun, Kwang Jin Baek, and Nyoun Soo
Kwon
705
Koremu K. Meja, Matthew C. Catley,
Lisa M. Cambridge, Peter J. Barnes, Hazel
Lum, Robert Newton, and Mark A.
Giembycz
833
Kar-Chan Choong and Roh-Yu Shen
444
Francesco Crespi and Zvani L. Rossetti
462
Thomas F. Finnegan, De-Pei Li,
Shao-Rui Chen, and Hui-Lin Pan
476
Comparison of the Effects of Dextromethorphan,
Dextrorphan, and Levorphanol on the Hypothalamo-PituitaryAdrenal Axis
Bremazocine Increases C-Type Natriuretic Peptide Levels in
Aqueous Humor and Enhances Outflow Facility
Overexpression of Pituitary Adenylate Cyclase-Activating
Polypeptide in Islets Inhibits Hyperinsulinemia and Islet
Hyperplasia in Agouti Yellow Mice
GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL
Characterization of IDN-6556 (3-{2-[2-tert-Butylphenylaminooxalyl)-amino]-propionylamino}-4-oxo-5-(2,3,5,6tetrafluoro-phenoxy)-pentanoic Acid): a Liver-Targeted
Caspase Inhibitor
-^
INFLAMMATION AND IMMUNOPHARMACOLOGY
K-Opioid Receptor Ligands Inhibit Cocaine-Induced HIV-1
Expression in Microglial Cells
Gastric Tolerability and Prolonged Prostaglandin Inhibition in
the Brain with a Nitric Oxide-Releasing Flurbiprofen
Derivative, NCX-2216 [3-[4-(2-Fluoro-a-methyl-[l,lbiphenyI]-4-acetyloxy)-3-methoxyphenyl]-2-propenoic acid 4nitrooxy butyl ester]
SSR240612IX2tf)-2-[((3/0-3-(l,3-BenzodioxoI-5-yl)-3-{[(6methoxy-2-naphthyl)sulfonyl]amino}propanoyl)amino]-3-(4{|2tf,6S)-2,6-dimethylpiperidinyl]methyI}phenyl)-iV-isopropyliV-methylpropanamide Hydrochloride], a New Nonpeptide
Antagonist of the Bradykinin B t Receptor: Biochemical and
Pharmacological Characterization
In Vivo Activity of a Phospholipase C Inhibitor, l-(6-((17/3-3Mcthoxyestra-1,3,5( 10)-trien- 17-yl)amino)hexyl)- l#-py rrole2,5-dione (U73122), in Acute and Chronic Inflammatory
Reactions
Inhibition of Nitric Oxide Generation by 23,24Dihydrocucurbitacin D in Mouse Peritoneal Macrophages
Adenovirus-Mediated Delivery and Expression of a cAMPDependent Protein Kinase Inhibitor Gene to BEAS-2B
Epithelial Cells Abolishes the Anti-Inflammatory Effects of
Rolipram, Salbutamol, and Prostaglandin E 2: A Comparison
with H-89
NEUROPHARMACOLOGY
Methylphenidate Restores Ventral Tegmental Area Dopamine
Neuron Activity in Prenatal Ethanol-Exposed Rats by
Augmenting Dopamine Neurotransmission
Pulse of Nitric Oxide Release in Response to Activation of NMethyl-D-aspartate Receptors in the Rat Striatum: Rapid
Desensitization, Inhibition by Receptor Antagonists, and
Potentiation by Glycine
Activation of /*-Opioid Receptors Inhibits Synaptic Inputs to
Spinally Projecting Rostral Ventromedial Medulla Neurons
A Novel Selective Allosteric Modulator Potentiates the
Activity of Native Metabotropic Glutamate Receptor Subtype
5 in Rat Forebrain
Julie A. O'Brien, Wei Lemaire,
Marion Wittmann, Marlene A. Jacobson,
Sookhee N. Ha, David D. Wisnoski,
Craig W. Lindsley, Herve J. Schaffhauser,
Blake Rowe, Cyrille Sur, Mark E. Duggan,
Douglas J. Pettibone, P. Jeffrey Conn, and
David L. Williams, Jr.
568
Alterations in Vesicular Dopamine Uptake Contribute to
Tolerance to the Neurotoxic Effects of Methamphetamine
Kamisha L. Johnson-Davis,
Jannine G. Truong, Annette E. Fleckenstein,
and Diana G. Wilkins
578
Protein Kinase C e and y: Involvement in Formalin-Induced
Nociception in Neonatal Rats
Sarah M. Sweitzer, Shirley M. E. Wong,
Michael C. Peters,
Daria Mochly-Rosen, David C. Yeomans,
and Joan J. Kendig
616
Phytoestrogen Cimicifugoside-Mediated Inhibition of
Catecholamine Secretion by Blocking Nicotinic Acetylcholine
Receptor in Bovine Adrenal Chroniaffin Cells
Kyung-Chul Woo, Yong-Soo Park,
Dong-Jae Jun, Jeong-Ok Lim, Woon-Yi
Baek, Byung-Sun Suh, and Kyong-Tai
Kim
641
Enantioselectivity of o:-Benzy la-methyl-y-butyrolactoneMediated Modulation of Anticonvulsant Activity and GABAA
Receptor Function
Eric B. Gonzales, Cathy L. Bell-Horner,
Maria Antonette M. de la Cruz,
James A. Ferrendelli, Douglas F. Covey, and
Glenn H. Dillon
677
Dopaminergic Agonists and Muscarinic Antagonists Improve
Lateralization in Hemiparkinsonian Rats in a Novel
Exploratory Y-Maze
Makoto Nakagawa, Makoto Ohgoh,
Yukio Nishizawa, and Hiroo Ogura
737
Fast Onset Medications through Thermally Generated
Aerosols
Joshua D. Rabinowitz, Martin Wensley,
Peter Lloyd, Daniel Myers, William Shen,
Amy Lu, Craig Hodges, Ron Hale, Daniel
Mufson, and Alejandro Zaffaroni
769
Differential Conditioned Place Preference Responses to
Endomorphin-1 and Endomorphin-2 Microinjected into the
Posterior Nucleus Accumbens Shell and Ventral Tegmental
Area in the Rat
Maia Terashvili, Hsiang-en Wu,
Randy J. Leitermann, Kuei-chun Hung,
Andrew D. Clithero, Emma T. Schwasinger,
and Leon F. Tseng
816