Journal of Pharmacology and Experimental Therapeutics: 304 (3)

March 01, 2003; Volume 304,Issue 3

PERSPECTIVES IN PHARMACOLOGY

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Drugs Targeting Alzheimer's Disease: Some Things Old and Some Things New
Mary L. Michaelis

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 897-904; DOI: https://doi.org/10.1124/jpet.102.035840
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Mechanisms of Renal Cell Repair and Regeneration after Acute Renal Failure
Paul A. Nony and Rick G. Schnellmann

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 905-912; DOI: https://doi.org/10.1124/jpet.102.035022

ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION

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Mechanisms of Down-Regulation of CYP2E1 Expression by Inflammatory Cytokines in Rat Hepatoma Cells
Jukka Hakkola, Yin Hu and Magnus Ingelman-Sundberg

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1048-1054; DOI: https://doi.org/10.1124/jpet.102.041582
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Distribution of STI-571 to the Brain Is Limited by P-Glycoprotein-Mediated Efflux
HaiQing Dai, Peter Marbach, Michel Lemaire, Michael Hayes and William F. Elmquist

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1085-1092; DOI: https://doi.org/10.1124/jpet.102.045260
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Pharmacokinetics and Interactions of a Novel Antagonist of Chemokine Receptor 5 (CCR5) with Ritonavir in Rats and Monkeys: Role of CYP3A and P-Glycoprotein
Sanjeev Kumar, Gloria Y. Kwei, Grace K. Poon, Susan A. Iliff, Yanfeng Wang, Qing Chen, Ronald B. Franklin, Varsha Didolkar, Regina W. Wang, Masayo Yamazaki, Shuet-Hing Lee Chiu, Jiunn H. Lin, Paul G. Pearson and Thomas A. Baillie

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1161-1171; DOI: https://doi.org/10.1124/jpet.102.045096
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Metabolism of Flavonoids via Enteric Recycling: Role of Intestinal Disposition
Jun Chen, Huimin Lin and Ming Hu

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1228-1235; DOI: https://doi.org/10.1124/jpet.102.046409
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Effects of the Flavonoids Biochanin A, Morin, Phloretin, and Silymarin on P-Glycoprotein-Mediated Transport
Shuzhong Zhang and Marilyn E. Morris

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1258-1267; DOI: https://doi.org/10.1124/jpet.102.044412
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Active Transport of High-Affinity Choline and Nicotine Analogs into the Central Nervous System by the Blood-Brain Barrier Choline Transporter
David D. Allen, Paul R. Lockman, Karen E. Roder, Linda P. Dwoskin and Peter A. Crooks

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1268-1274; DOI: https://doi.org/10.1124/jpet.102.045856
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Pharmacology, Pharmacokinetics, and Metabolism of Acetothiolutamide, a Novel Nonsteroidal Agonist for the Androgen Receptor
Donghua Yin, Huiping Xu, Yali He, Leonid I. Kirkovsky, Duane D. Miller and James T. Dalton

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1323-1333; DOI: https://doi.org/10.1124/jpet.102.040832

BEHAVIORAL PHARMACOLOGY

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Discrimination of a Single Dose of Morphine Followed by Naltrexone: Substitution of Other Agonists for Morphine and Other Antagonists for Naltrexone in a Rat Model of Acute Dependence
Stephen G. Holtzman

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1033-1041; DOI: https://doi.org/10.1124/jpet.102.044875
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Behavioral Pharmacology of AR-A000002, a Novel, Selective 5-Hydroxytryptamine_1B Antagonist
T. J. Hudzik, M. Yanek, T. Porrey, J. Evenden, C. Paronis, M. Mastrangelo, C. Ryan, S. Ross and C. Stenfors

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1072-1084; DOI: https://doi.org/10.1124/jpet.102.045468

CARDIOVASCULAR

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Soy-Derived Isoflavones Exert Opposing Actions on Guinea Pig Ventricular Myocytes
Reginald Liew, J. Koudy Williams, Peter Collins and Kenneth T. MacLeod

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 985-993; DOI: https://doi.org/10.1124/jpet.102.042986
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Prevention of Heart Failure in Rats by Trimetazidine Treatment: A Consequence of Accelerated Phospholipid Turnover?
Imène Tabbi-Anneni, Cécile Helies-Toussaint, Didier Morin, Anne Bescond-Jacquet, Arnaud Lucien and Alain Grynberg

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1003-1009; DOI: https://doi.org/10.1124/jpet.102.042143
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Modification of Noradrenaline Release in Pithed Spontaneously Hypertensive Rats by I₁-Binding Sites in Addition to α₂-Adrenoceptors
Walter Raasch, Britta Jungbluth, Ulrich Schäfer, Walter Häuser and Peter Dominiak

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1063-1071; DOI: https://doi.org/10.1124/jpet.102.044966
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Enhancement Effect under High-Glucose Conditions on U46619-Induced Spontaneous Phasic Contraction in Mouse Portal Vein
Koji Nobe, Yasushi Sakai, Hiromi Nobe, Junko Takashima, Richard J. Paul and Kazutaka Momose

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1129-1142; DOI: https://doi.org/10.1124/jpet.102.040964
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Minalrestat, an Aldose Reductase Inhibitor, Corrects the Impaired Microvascular Reactivity in Diabetes
Eliana H. Akamine, Thomas C. Hohman, Dorothy Nigro, Maria Helena C. Carvalho, Rita de Cássia Tostes and Zuleica B. Fortes

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1236-1242; DOI: https://doi.org/10.1124/jpet.102.044693
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The Nitric Oxide- and Prostaglandin-Independent Component of the Renal Vasodilator Effect of Thimerosal Is Mediated by Epoxyeicosatrienoic Acids
Y.-J. Chen, H. Jiang and J. Quilley

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1292-1298; DOI: https://doi.org/10.1124/jpet.102.042671

CELLULAR AND MOLECULAR

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Selective Cyclooxygenase-2 Inhibition Does Not Alter Keratinocyte Wound Responses in the Mouse Epidermis after Abrasion
Medora M. Hardy, Eric A. G. Blomme, Andrew Lisowski, Kevin S. Chinn, Amy Jones, Janet M. Harmon, Alan Opsahl, Richard L. Ornberg and Catherine S. Tripp

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 959-967; DOI: https://doi.org/10.1124/jpet.102.044545
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Bradykinin B₂ Receptor Activates Extracellular Signal-Regulated Protein Kinase in mIMCD-3 Cells via Epidermal Growth Factor Receptor Transactivation
Yurii V. Mukhin, Evgeny A. Garnovsky, Michael E. Ullian and Maria N. Garnovskaya

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 968-977; DOI: https://doi.org/10.1124/jpet.102.043943
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Distinct Effects of Ketone Bodies on Down-Regulation of Cell Surface Insulin Receptor and Insulin Receptor Substrate-1 Phosphorylation in Adrenal Chromaffin Cells
Hiroki Yokoo, Tomokazu Saitoh, Seiji Shiraishi, Toshihiko Yanagita, Takashi Sugano, Shin-Ichi Minami, Hideyuki Kobayashi and Akihiko Wada

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 994-1002; DOI: https://doi.org/10.1124/jpet.102.044115
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Nateglinide, a d-Phenylalanine Derivative Lacking Either a Sulfonylurea or Benzamido Moiety, Specifically Inhibits Pancreatic β-Cell-Type K_ATP Channels
Motohiko Chachin, Mitsuhiko Yamada, Akikazu Fujita, Tetsuro Matsuoka, Kenji Matsushita and Yoshihisa Kurachi

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1025-1032; DOI: https://doi.org/10.1124/jpet.102.044917
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Isostrychnopentamine, an Indolomonoterpenic Alkaloid fromStrychnos usambarensis, Induces Cell Cycle Arrest and Apoptosis in Human Colon Cancer Cells
Michel Frédérich, Mohamed Bentires-Alj, Monique Tits, Luc Angenot, Roland Greimers, Jacques Gielen, Vincent Bours and Marie-Paule Merville

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1103-1110; DOI: https://doi.org/10.1124/jpet.102.044867
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Selective Tryptic Cleavage at the Tethered Ligand Site of the Amino Terminal Domain of Proteinase-Activated Receptor-2 in Intact Cells
Bahjat Al-Ani and Morley D. Hollenberg

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1120-1128; DOI: https://doi.org/10.1124/jpet.102.043844
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Dual Action of n-Butanol on Neuronal Nicotinic α4β2 Acetylcholine Receptors
Yi Zuo, Jay Z. Yeh and Toshio Narahashi

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1143-1152; DOI: https://doi.org/10.1124/jpet.102.044537
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Opposite Effects of Rofecoxib on Nuclear Factor-κB and Activating Protein-1 Activation
Ellen Niederberger, Irmgard Tegeder, Christine Schäfer, Maic Seegel, Sabine Grösch and Gerd Geisslinger

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1153-1160; DOI: https://doi.org/10.1124/jpet.102.044016
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Regulation of Semicarbazide-Sensitive Amine Oxidase Expression by Tumor Necrosis Factor-α in Adipocytes: Functional Consequences on Glucose Transport
Nathalie Mercier, Marthe Moldes, Khadija El Hadri and Bruno Fève

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1197-1208; DOI: https://doi.org/10.1124/jpet.102.044420
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Molecular Determinants of Melanocortin 4 Receptor Ligand Binding and MC4/MC3 Receptor Selectivity
Sarah A. Nickolls, Mary I. Cismowski, Xiaochuan Wang, Meira Wolff, Paul J. Conlon and Richard A. Maki

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1217-1227; DOI: https://doi.org/10.1124/jpet.102.044974
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Effects of Large Clostridial Cytotoxins on Activation of RBL 2H3-hm1 Mast Cells Indicate Common and Different Roles of Rac in FcεRI and M1-Receptor Signaling
Nabil Djouder, Eduardo Aneiros, Adolfo Cavalié and Klaus Aktories

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1243-1250; DOI: https://doi.org/10.1124/jpet.102.045351
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Up-Regulation of Regulator of G Protein Signaling 4 Expression in a Model of Neuropathic Pain and Insensitivity to Morphine
Martine Garnier, Paola F. Zaratin, Giovanna Ficalora, Maurizio Valente, Laura Fontanella, Man-Hee Rhee, Kendall J. Blumer and Mark A. Scheideler

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1299-1306; DOI: https://doi.org/10.1124/jpet.102.043471

CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY

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A Long-Acting Suicide Gene Toxin, 6-Methylpurine, Inhibits Slow Growing Tumors after a Single Administration
Vijayakrishna K. Gadi, Sherrie D. Alexander, William R. Waud, Paula W. Allan, William B. Parker and Eric J. Sorscher

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1280-1284; DOI: https://doi.org/10.1124/jpet.102.044743
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Phosphorylation of 4′-thio-β-d-Arabinofuranosylcytosine and Its Analogs by Human Deoxycytidine Kinase
Hitoshi Someya, Sue C. Shaddix, Kamal N. Tiwari, John A. Secrist and William B. Parker

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1314-1322; DOI: https://doi.org/10.1124/jpet.102.045435

ENDOCRINE AND REPRODUCTIVE

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Pharmacodynamics of Selective Androgen Receptor Modulators
Donghua Yin, Wenqing Gao, Jeffrey D. Kearbey, Huiping Xu, Kiwon Chung, Yali He, Craig A. Marhefka, Karen A. Veverka, Duane D. Miller and James T. Dalton

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1334-1340; DOI: https://doi.org/10.1124/jpet.102.040840

GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

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Facilitation by Endogenous Prostaglandins of Capsaicin-Induced Gastric Protection in Rodents through EP2 and IP Receptors
Koji Takeuchi, Shinichi Kato, Masanori Takeeda, Yoshihiro Ogawa, Masato Nakashima and Masahiro Matsumoto

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1055-1062; DOI: https://doi.org/10.1124/jpet.102.044156
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A Role for TRPV1 in Bradykinin-Induced Excitation of Vagal Airway Afferent Nerve Terminals
Michael J. Carr, Marian Kollarik, Sonya N. Meeker and Bradley J. Undem

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1275-1279; DOI: https://doi.org/10.1124/jpet.102.043422

INFLAMMATION AND IMMUNOPHARMACOLOGY

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Small Molecule Antagonists of Complement Receptor Type 3 Block Adhesion and Adhesion-Dependent Oxidative Burst in Human Polymorphonuclear Leukocytes
Vinay S. Bansal, Sanskruti Vaidya, Elizabeth P. Somers, Mansi Kanuga, Diane Shevell, Renee Weikel and Patricia A. Detmers

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1016-1024; DOI: https://doi.org/10.1124/jpet.102.045286
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Inhibition of Endotoxin Response by E5564, a Novel Toll-Like Receptor 4-Directed Endotoxin Antagonist
Maureen Mullarkey, Jeffrey R. Rose, John Bristol, Tsutomu Kawata, Akufumi Kimura, Seiichi Kobayashi, Melinda Przetak, Jesse Chow, Fabian Gusovsky, William J. Christ and Daniel P. Rossignol

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1093-1102; DOI: https://doi.org/10.1124/jpet.102.044487
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Modulatory Effect of Bolinaquinone, a Marine Sesquiterpenoid, on Acute and Chronic Inflammatory Processes
Rut Lucas, Clelia Giannini, Maria Valeria D'auria and Miguel Payá

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1172-1180; DOI: https://doi.org/10.1124/jpet.102.045278
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Pharmacological Assessment of the Nitric-Oxide Synthase Isoform Involved in Eosinophilic Inflammation in a Rat Model of Sephadex-Induced Airway Inflammation
Mark A. Birrell, Kerryn McCluskie, El-Bdaoui Haddad, Cliff H. Battram, Stephen E. Webber, Martyn L. Foster, Magdi H. Yacoub and Maria G. Belvisi

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1285-1291; DOI: https://doi.org/10.1124/jpet.102.044339

NEUROPHARMACOLOGY

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5-Hydroxytryptamine 1A Receptor Activation Protects againstN-Methyl-d-aspartate-Induced Apoptotic Cell Death in Striatal and Mesencephalic Cultures
Lalitha Madhavan, William J. Freed, Vellareddy Anantharam and Anumantha G. Kanthasamy

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 913-923; DOI: https://doi.org/10.1124/jpet.102.044370
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Serine 329 of the μ-Opioid Receptor Interacts Differently with Agonists
Joost Pil and Jan Tytgat

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 924-930; DOI: https://doi.org/10.1124/jpet.102.040113
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Short-Term Exposure to Melatonin Differentially Affects the Functional Sensitivity and Trafficking of the hMT₁ and hMT₂ Melatonin Receptors
M. J. Gerdin, M. I. Masana, D. Ren, R. J. Miller and M. L. Dubocovich

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 931-939; DOI: https://doi.org/10.1124/jpet.102.044990
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Novel Expression of Vanilloid Receptor 1 on Capsaicin-Insensitive Fibers Accounts for the Analgesic Effect of Capsaicin Cream in Neuropathic Pain
Md Harunor Rashid, Makoto Inoue, Saori Kondo, Toshiko Kawashima, Shiho Bakoshi and Hiroshi Ueda

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 940-948; DOI: https://doi.org/10.1124/jpet.102.046250
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Fluoxetine Increases GABA_A Receptor Activity through a Novel Modulatory Site
Richard T. Robinson, Brandon C. Drafts and Janet L. Fisher

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 978-984; DOI: https://doi.org/10.1124/jpet.102.044834
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Antinociceptive Synergy between Δ⁹-Tetrahydrocannabinol and Opioids after Oral Administration
Diana L. Cichewicz and Erin A. McCarthy

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1010-1015; DOI: https://doi.org/10.1124/jpet.102.045575
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3-[2-[4-(3-Chloro-2-methylphenyl)-1-piperazinyl]ethyl]-5,6-dimethoxy-1-(4-imidazolylmethyl)-1H-indazole Dihydrochloride 3.5 Hydrate (DY-9760e), a Novel Calmodulin Antagonist, Reduces Brain Edema through the Inhibition of Enhanced Blood-Brain Barrier Permeability after Transient Focal Ischemia
Toshiyuki Sato, Yoshiyuki Morishima and Yasufumi Shirasaki

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1042-1047; DOI: https://doi.org/10.1124/jpet.102.045039
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Methylphenidate Alters Vesicular Monoamine Transport and Prevents Methamphetamine-Induced Dopaminergic Deficits
Verónica Sandoval, Evan L. Riddle, Glen R. Hanson and Annette E. Fleckenstein

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1181-1187; DOI: https://doi.org/10.1124/jpet.102.045005
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Selective Depression by General Anesthetics of Glutamate Versus GABA Release from Isolated Cortical Nerve Terminals
Robert I. Westphalen and Hugh C. Hemmings

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1188-1196; DOI: https://doi.org/10.1124/jpet.102.044685
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Neuroendocrine Evidence That (S)-2-(Chloro-5-fluoro-indol- l-yl)-1-methylethylamine Fumarate (Ro 60-0175) Is Not a Selective 5-Hydroxytryptamine_2C Receptor Agonist
K. J. Damjanoska, N. A. Muma, Y. Zhang, D. N. D'Souza, F. Garcia, G. A. Carrasco, G. H. Kindel, K. A. Haskins, M. Shankaran, B. R. Petersen and L. D. Van De Kar

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1209-1216; DOI: https://doi.org/10.1124/jpet.102.043489
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Dose-Dependent EEG Effects of Zolpidem Provide Evidence for GABA_A Receptor Subtype Selectivity in Vivo
S. A. G. Visser, F. L. C. Wolters, P. H. van der Graaf, L. A. Peletier and M. Danhof

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1251-1257; DOI: https://doi.org/10.1124/jpet.102.044859

TOXICOLOGY

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Evidence for Interactions between Intracellular Calcium Stores during Methylmercury-Induced Intracellular Calcium Dysregulation in Rat Cerebellar Granule Neurons
Tobi L. Limke, James K. L. Otero-Montañez and William D. Atchison

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 949-958; DOI: https://doi.org/10.1124/jpet.102.042457
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Delayed Neurologic and Behavioral Effects of Subtoxic Doses of Cholinesterase Inhibitors
Oscar U. Scremin, Tsung-Ming Shih, Ly Huynh, Margareth Roch, Ruth Booth and Donald J. Jenden

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1111-1119; DOI: https://doi.org/10.1124/jpet.102.044818
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Adenosine A₁ Receptor AgonistN ⁶-Cyclopentyladenosine Affects the Inactivation of Acetylcholinesterase in Blood and Brain by Sarin
Tjerk J. H. Bueters, Marloes J. A. Joosen, Herman P. M. van Helden, Ad P. IJzerman and Meindert Danhof

Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1307-1313; DOI: https://doi.org/10.1124/jpet.102.044644

Erratum

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Correction to “Influence of Ovarian Sex Steroids on Spinal Methionine-Enkephalin Release: Comparison with Dynorphin Reveals Asymmetrical Regulation”
Journal of Pharmacology and Experimental Therapeutics March 2003, 304 (3) 1341;

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Table of Contents

PERSPECTIVES IN PHARMACOLOGY

ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION

BEHAVIORAL PHARMACOLOGY

CARDIOVASCULAR

CELLULAR AND MOLECULAR

CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY

ENDOCRINE AND REPRODUCTIVE

GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

INFLAMMATION AND IMMUNOPHARMACOLOGY

NEUROPHARMACOLOGY

TOXICOLOGY

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