Journal of Pharmacology and Experimental Therapeutics: 306 (3)

September 01, 2003; Volume 306,Issue 3

PERSPECTIVES IN PHARMACOLOGY

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The Cholinergic Hypothesis of Age and Alzheimer's Disease-Related Cognitive Deficits: Recent Challenges and Their Implications for Novel Drug Development
A. V. Terry and J. J. Buccafusco

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 821-827; DOI: https://doi.org/10.1124/jpet.102.041616

ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION

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Contribution of Lymphatically Transported Testosterone Undecanoate to the Systemic Exposure of Testosterone after Oral Administration of Two Andriol Formulations in Conscious Lymph Duct-Cannulated Dogs
David M. Shackleford, W. A. (Fried) Faassen, Natalie Houwing, Holger Lass, Glenn A. Edwards, Christopher J. H. Porter and William N. Charman

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 925-933; DOI: https://doi.org/10.1124/jpet.103.052522
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Characterization of Blood-Brain Barrier Permeability to PYY_3-36 in the Mouse
Naoko Nonaka, Seiji Shioda, Michael L. Niehoff and William A. Banks

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 948-953; DOI: https://doi.org/10.1124/jpet.103.051821
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Avasimibe Induces CYP3A4 and Multiple Drug Resistance Protein 1 Gene Expression through Activation of the Pregnane X Receptor
Jasminder Sahi, Mark A. Milad, Xianxian Zheng, Kelly A. Rose, Hongbing Wang, Linda Stilgenbauer, Darryl Gilbert, Summer Jolley, Ralph H. Stern and Edward L. LeCluyse

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1027-1034; DOI: https://doi.org/10.1124/jpet.103.050526
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Multiple Injections of Pegylated Liposomal Doxorubicin: Pharmacokinetics and Therapeutic Activity
Gregory J. R. Charrois and Theresa M. Allen

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1058-1067; DOI: https://doi.org/10.1124/jpet.103.053413
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Aromatase Is the Major Enzyme Metabolizing Buprenorphine in Human Placenta
Sujal V. Deshmukh, Tatiana N. Nanovskaya and Mahmoud S. Ahmed

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1099-1105; DOI: https://doi.org/10.1124/jpet.103.053199
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Genetic Variability at the Human FMO1 Locus: Significance of a Basal Promoter Yin Yang 1 Element Polymorphism (FMO1^*6)
Ronald N. Hines, Zhaohui Luo, Kathleen A. Hopp, Erwin T. Cabacungan, Sevasti B. Koukouritaki and D. Gail McCarver

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1210-1218; DOI: https://doi.org/10.1124/jpet.103.053686

BEHAVIORAL PHARMACOLOGY

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Topical Capsaicin-Induced Allodynia in Unanesthetized Primates: Pharmacological Modulation
Eduardo R. Butelman, Jonathan W. Ball, Todd J. Harris and Mary Jeanne Kreek

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1106-1114; DOI: https://doi.org/10.1124/jpet.103.052381
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Temporal Effects of Stress by Immobilization and Sensitivity of the Isolated Rat Pacemaker to Isoproterenol: Roles of Corticosterone, Neuronal Uptake, and β-Adrenergic Homogeneity
Marco Aurelio de Paula Brotto

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1152-1158; DOI: https://doi.org/10.1124/jpet.103.052670
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GABAergic Systems Modulate Nicotinic Receptor-Mediated Seizures in Mice
Peter Dobelis, Scott Hutton, Ying Lu and Allan C. Collins

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1159-1166; DOI: https://doi.org/10.1124/jpet.103.053066
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Relative Efficacy of Buprenorphine, Nalbuphine and Morphine in Opioid-Treated Rhesus Monkeys Discriminating Naltrexone
Stacy L. Sell, Lance R. McMahon and Charles P. France

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1167-1173; DOI: https://doi.org/10.1124/jpet.103.051425

CARDIOVASCULAR

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Role of Peripheral Benzodiazepine Receptors in Mitochondrial, Cellular, and Cardiac Damage Induced by Oxidative Stress and Ischemia-Reperfusion
Nathalie Leducq, Françoise Bono, Thierry Sulpice, Val érie Vin, Philip Janiak, Gérard Le Fur, Steve E. O'Connor and Jean-Marc Herbert

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 828-837; DOI: https://doi.org/10.1124/jpet.103.052068
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Nicotine Induces a Long QT Phenotype in Kcnq1-Deficient Mouse Hearts
Toshimasa Tosaka, Mathew C. Casimiro, Qi Rong, Srihari Tella, Michelle Oh, Alexander N. Katchman, John C. Pezzullo, Karl Pfeifer and Steven N. Ebert

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 980-987; DOI: https://doi.org/10.1124/jpet.103.053017
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Effects of Reboxetine on Sympathetic Neuroeffector Transmission in Rabbit Carotid Artery
Lasse E. Rasmussen and Ove A. Nedergaard

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 995-1002; DOI: https://doi.org/10.1124/jpet.103.052233
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Pilot Intervention: Aerosolized Adrenomedullin Reduces Pulmonary Hypertension
Michael A. Kandler, Katharina von der Hardt, Suleiman Mahfoud, Martin Chada, Ellen Schoof, Thomas Papadopoulos, Wolfgang Rascher and Jörg Dötsch

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1021-1026; DOI: https://doi.org/10.1124/jpet.103.049817
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Inhibition of Canine (NCX1.1) and Drosophila (CALX1.1) Na⁺-Ca²⁺ Exchangers by 7-Chloro-3,5-dihydro-5-phenyl-1H-4,1-benzothiazepine-2-one (CGP-37157)
Alexander Omelchenko, Ron Bouchard, Hoa Dinh Le, Platon Choptiany, Neeraj Visen, Mark Hnatowich and Larry V. Hryshko

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1050-1057; DOI: https://doi.org/10.1124/jpet.103.053389
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Pharmacological Interruption of Acute Thrombus Formation with Minimal Hemorrhagic Complications by a Small Molecule Tissue Factor/Factor VIIa Inhibitor: Comparison to Factor Xa and Thrombin Inhibition in a Nonhuman Primate Thrombosis Model
Osman D. Suleymanov, James A. Szalony, Anita K. Salyers, Rhonda M. LaChance, John J. Parlow, Michael S. South, Rhonda S. Wood and Nancy S. Nicholson

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1115-1121; DOI: https://doi.org/10.1124/jpet.103.052779
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Pharmacological Characterization of the New Stable Antiarrhythmic Peptide Analog Ac-d-Tyr-d-Pro-d-Hyp-Gly-d-Ala-Gly-NH₂ (ZP123): In Vivo and in Vitro Studies
Anne Louise Kjølbye, Carsten Boye Knudsen, Trine Jepsen, Bjarne Due Larsen and Jørgen Søberg Petersen

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1191-1199; DOI: https://doi.org/10.1124/jpet.103.052258
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Functional and Binding Characterizations of Urotensin II-Related Peptides in Human and Rat Urotensin II-Receptor Assay
Alexandre Brkovic, Almut Hattenberger, Evi Kostenis, Thomas Klabunde, Stefanie Flohr, Michael Kurz, Steve Bourgault and Alain Fournier

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1200-1209; DOI: https://doi.org/10.1124/jpet.103.052415

CELLULAR AND MOLECULAR

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A Selective and Oral Small Molecule Inhibitor of Vascular Epithelial Growth Factor Receptor (VEGFR)-2 and VEGFR-1 Inhibits Neovascularization and Vascular Permeability
Neela Patel, Li Sun, Deborah Moshinsky, Hui Chen, Kathleen M. Leahy, Phuong Le, Katherine G. Moss, Xueyan Wang, Audie Rice, Danny Tam, A. Douglas Laird, Xiaoming Yu, Qingling Zhang, Cho Tang, Gerald McMahon and Anthony Howlett

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 838-845; DOI: https://doi.org/10.1124/jpet.103.052167
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Dopamine Modulation of Membrane Excitability in Striatal Spiny Neurons is Altered in DARPP-32 Knockout Mice
Shao-Pii Onn, Allen A. Fienberg and Anthony A. Grace

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 870-879; DOI: https://doi.org/10.1124/jpet.103.050062
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The Cytoplasmic Domain of Alzheimer's Amyloid-β Protein Precursor Causes Sustained Apoptosis Signal-Regulating Kinase 1/c-Jun NH₂-Terminal Kinase-Mediated Neurotoxic Signal via Dimerization
Yuichi Hashimoto, Takako Niikura, Tomohiro Chiba, Emi Tsukamoto, Hisae Kadowaki, Hideki Nishitoh, Yohichi Yamagishi, Miho Ishizaka, Marina Yamada, Mikiro Nawa, Kenzo Terashita, Sadakazu Aiso, Hidenori Ichijo and Ikuo Nishimoto

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 889-902; DOI: https://doi.org/10.1124/jpet.103.051383
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cDNA Microarray Analysis Reveals a Nuclear Factor-κB-Independent Regulation of Macrophage Function by Adenosine
Zoltán H. Néemeth, S. Joseph Leibovich, Edwin A. Deitch, E. Sylvester Vizi, Csaba Szabó and György Haskó

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1042-1049; DOI: https://doi.org/10.1124/jpet.103.052944
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Cilostazol Prevents Tumor Necrosis Factor-α-Induced Cell Death by Suppression of Phosphatase and Tensin Homolog Deleted from Chromosome 10 Phosphorylation and Activation of Akt/Cyclic AMP Response Element-Binding Protein Phosphorylation
Ki Whan Hong, Ki Young Kim, Hwa Kyoung Shin, Jeong Hyun Lee, Jae Moon Choi, Yong-Geun Kwak, Chi Dae Kim, Won Suk Lee and Byung Yong Rhim

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1182-1190; DOI: https://doi.org/10.1124/jpet.103.052365

GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

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Prevention of Ethanol-Induced Liver Injury in Rats by an Agonist of Peroxisome Proliferator-Activated Receptor-γ, Pioglitazone
Nobuyuki Enomoto, Yoshiyuki Takei, Miyoko Hirose, Akira Konno, Tomoyoshi Shibuya, Shujiro Matsuyama, Satoko Suzuki, Kenichi Ikejima Tsuneo Kitamura and Nobuhiro Sato

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 846-854; DOI: https://doi.org/10.1124/jpet.102.047217
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Reversal of Multiple Drug Resistance in Cholangiocarcinoma by the Glutathione S-Transferase-π-Specific Inhibitor O¹-Hexadecyl-γ-glutamyl-S-benzylcysteinyl-D-phenylglycine Ethylester
Takaharu Nakajima, Tetsuji Takayama, Koji Miyanishi, Atsushi Nobuoka, Tsuyoshi Hayashi, Tomoyuki Abe, Junji Kato, Kiyoyuki Sakon, Yoshimitsu Naniwa, Hirohumi Tanabe and Yoshiro Niitsu

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 861-869; DOI: https://doi.org/10.1124/jpet.103.052696

INFLAMMATION AND IMMUNOPHARMACOLOGY

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A Small Molecule α₄β₁/α₄β₇ Antagonist Differentiates between the Low-Affinity States of α₄β₁ and α₄β₇: Characterization of Divalent Cation Dependence
Linda A. Egger, Jin Cao, Christine McCallum, Usha Kidambi, Gail Van Riper, Ermengilda McCauley, Richard A. Mumford, Thomas J. Lanza, Linus S. Lin, Stephen E. de Laszlo, David N. Young, Ginger Yang, Dennis C. Dean, Conrad E. Raab, Mike A. Wallace, Allen N. Jones, William K. Hagmann, John A. Schmidt, R. Blake Pepinsky, Daniel M. Scott, Wen-Cherng Lee, Mark A. Cornebise and Patricia A. Detmers

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 903-913; DOI: https://doi.org/10.1124/jpet.102.047704
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Evidence for Cannabinoid Receptor-Dependent and -Independent Mechanisms of Action in Leukocytes
Barbara L. Faubert Kaplan, Cheryl E. Rockwell and Norbert E. Kaminski

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1077-1085; DOI: https://doi.org/10.1124/jpet.103.051961
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Effect of Ibuprofen on Neutrophil Migration in Vivo in Cystic Fibrosis and Healthy Subjects
Michael W. Konstan, Jeanne E. Krenicky, Marcie R. Finney, H. Lester Kirchner, Kathleen A. Hilliard, Jay B. Hilliard, Pamela B. Davis and Charles L. Hoppel

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1086-1091; DOI: https://doi.org/10.1124/jpet.103.052449
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The Orally Available Spleen Tyrosine Kinase Inhibitor 2-[7-(3,4-Dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino]nicotinamide Dihydrochloride (BAY 61-3606) Blocks Antigen-Induced Airway Inflammation in Rodents
Noriyuki Yamamoto, Keisuke Takeshita, Michitaka Shichijo, Toshio Kokubo, Masako Sato, Kosuke Nakashima, Mina Ishimori, Hiroichi Nagai, Ying-Fu Li, Takeshi Yura and Kevin B. Bacon

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1174-1181; DOI: https://doi.org/10.1124/jpet.103.052316

NEUROPHARMACOLOGY

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Sympathetic Innervation in the 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine Primate Model of Parkinson's Disease
David S. Goldstein, Sheng-Ting Li, Courtney Holmes and Krys Bankiewicz

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 855-860; DOI: https://doi.org/10.1124/jpet.103.051714
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Differential Regulation of the Endocannabinoids Anandamide and 2-Arachidonylglycerol within the Limbic Forebrain by Dopamine Receptor Activity
Sachin Patel, David J. Rademacher and Cecilia J. Hillard

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 880-888; DOI: https://doi.org/10.1124/jpet.103.054270
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Differential Actions of Fipronil and Dieldrin Insecticides on GABA-Gated Chloride Channels in Cockroach Neurons
Xilong Zhao, Vincent L. Salgado, Jay Z. Yeh and Toshio Narahashi

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 914-924; DOI: https://doi.org/10.1124/jpet.103.051839
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Steroids Modulate N-Methyl-D-aspartate-Stimulated [³H]Dopamine Release from Rat Striatum via σ Receptors
Samer J. Nuwayhid and Linda L. Werling

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 934-940; DOI: https://doi.org/10.1124/jpet.103.052324
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The Novel Melatonin Agonist Agomelatine (S20098) Is an Antagonist at 5-Hydroxytryptamine_2C Receptors, Blockade of Which Enhances the Activity of Frontocortical Dopaminergic and Adrenergic Pathways
M. J. Millan, A. Gobert, F. Lejeune, A. Dekeyne, A. Newman-Tancredi, V. Pasteau, J.-M. Rivet and D. Cussac

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 954-964; DOI: https://doi.org/10.1124/jpet.103.051797
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μ-Opioid-Induced Desensitization of Opioid Receptor-Like 1 and μ-Opioid Receptors: Differential Intracellular Signaling Determines Receptor Sensitivity
Chitra D. Mandyam, Deepak R. Thakker and Kelly M. Standifer

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 965-972; DOI: https://doi.org/10.1124/jpet.103.051599
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l-Selegiline Potentiates the Cellular Poly(ADP-Ribosyl)ation Response to Ionizing Radiation
Christine Brabeck, Ragen Pfeiffer, Alan Leake, Sascha Beneke, Ralph Meyer and Alexander Bürkle

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 973-979; DOI: https://doi.org/10.1124/jpet.103.051342
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The Endogenous Cannabinoid Anandamide Inhibits α₇ Nicotinic Acetylcholine Receptor-Mediated Responses in Xenopus Oocytes
Murat Oz, Arippa Ravindran, Oscar Diaz-Ruiz, Li Zhang and Marisela Morales

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1003-1010; DOI: https://doi.org/10.1124/jpet.103.049981
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N-n-Alkylpyridinium Analogs, a Novel Class of Nicotinic Receptor Antagonists: Selective Inhibition of Nicotine-Evoked [³H]Dopamine Overflow from Superfused Rat Striatal Slices
Vladimir P. Grinevich, Peter A. Crooks, Sangeetha P. Sumithran, Aaron J. Haubner, Joshua T. Ayers and Linda P. Dwoskin

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1011-1020; DOI: https://doi.org/10.1124/jpet.103.051789
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Effect of Transport Inhibitors and Additional Anti-HIV Drugs on the Movement of Lamivudine (3TC) across the Guinea Pig Brain Barriers
J. E. Gibbs, T. Rashid and S. A. Thomas

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1035-1041; DOI: https://doi.org/10.1124/jpet.103.053827
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Group II Metabotropic and α-Amino-3-hydroxy-5-methyl-4-isoxazole Propionate (AMPA)/Kainate Glutamate Receptors Regulate the Deficit in Brain Reward Function Associated with Nicotine Withdrawal in Rats
Paul J. Kenny, Fabrizio Gasparini and Athina Markou

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1068-1076; DOI: https://doi.org/10.1124/jpet.103.052027
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Treatment of Adverse Effects of Excessive Phencyclidine Exposure in Rats with a Minimal Dose of Monoclonal Antibody
Elizabeth M. Laurenzana, Melinda G. Gunnell, W. Brooks Gentry and S. Michael Owens

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1092-1098; DOI: https://doi.org/10.1124/jpet.103.053140
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Role of Na⁺,K⁺-ATPase in Morphine-Induced Antinociception
Willias Masocha, Gyongyi Horvath, Ahmad Agil, María Ocaña, Esperanza Del Pozo, Margit Szikszay and José M. Baeyens

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1122-1128; DOI: https://doi.org/10.1124/jpet.103.052977
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ATP Augments Peptide Release from Rat Sensory Neurons in Culture through Activation of P2Y Receptors
H. Huang, X. Wu, G. D. Nicol, S. Meller and M. R. Vasko

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1137-1144; DOI: https://doi.org/10.1124/jpet.103.052951
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Long-Term Effects of Olanzapine, Risperidone, and Quetiapine on Ionotropic Glutamate Receptor Types: Implications for Antipsychotic Drug Treatment
Frank I. Tarazi, Ross J. Baldessarini, Nora S. Kula and Kehong Zhang

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1145-1151; DOI: https://doi.org/10.1124/jpet.103.052597

TOXICOLOGY

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Rat Hepatic CYP2E1 Is Induced by Very Low Nicotine Doses: An Investigation of Induction, Time Course, Dose Response, and Mechanism
Alina L. Micu, Sharon Miksys, Edward M. Sellers, Dennis R. Koop and Rachel F. Tyndale

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 941-947; DOI: https://doi.org/10.1124/jpet.103.052183
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Role of Cysteine S-Conjugate β-Lyase in the Metabolism of Cisplatin
Lei Zhang and Marie H. Hanigan

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 988-994; DOI: https://doi.org/10.1124/jpet.103.052225
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Comparative Effects of Methylmercury and Hg²⁺ on Human Neuronal N- and R-Type High-Voltage Activated Calcium Channels Transiently Expressed in Human Embryonic Kidney 293 Cells
Ravindra K. Hajela, Shuang-Qing Peng and William D. Atchison

Journal of Pharmacology and Experimental Therapeutics September 2003, 306 (3) 1129-1136; DOI: https://doi.org/10.1124/jpet.103.049429

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Table of Contents

PERSPECTIVES IN PHARMACOLOGY

ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION

BEHAVIORAL PHARMACOLOGY

CARDIOVASCULAR

CELLULAR AND MOLECULAR

GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

INFLAMMATION AND IMMUNOPHARMACOLOGY

NEUROPHARMACOLOGY

TOXICOLOGY

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