Journal of Pharmacology and Experimental Therapeutics: 301 (1)

April 01, 2002; Volume 301,Issue 1

PERSPECTIVES IN PHARMACOLOGY

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Pharmacology and Toxicology of Astrocyte-Neuron Glutamate Transport and Cycling
Ursula Sonnewald, Hong Qu and Michael Aschner

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 1-6; DOI: https://doi.org/10.1124/jpet.301.1.1
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Role of Multidrug Transporters in Pharmacoresistance to Antiepileptic Drugs
Wolfgang Löscher and Heidrun Potschka

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 7-14; DOI: https://doi.org/10.1124/jpet.301.1.7

ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION

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Gender-Specific and Developmental Influences on the Expression of Rat Organic Anion Transporters
Susan C. N. Buist, Nathan J. Cherrington, Supratim Choudhuri, Dylan P. Hartley and Curtis D. Klaassen

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 145-151; DOI: https://doi.org/10.1124/jpet.301.1.145
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Mechanism-Based Inactivation of Cytochrome P450 3A4 by 17α-Ethynylestradiol: Evidence for Heme Destruction and Covalent Binding to Protein
Hsia-lien Lin, Ute M. Kent and Paul F. Hollenberg

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 160-167; DOI: https://doi.org/10.1124/jpet.301.1.160
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Identification of a Novel Route of Extraction of Sirolimus in Human Small Intestine: Roles of Metabolism and Secretion
Mary F. Paine, Louis Y. Leung, H. K. Lim, Kecheng Liao, Aram Oganesian, Mei-Yi Zhang, Kenneth E. Thummel and Paul B. Watkins

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 174-186; DOI: https://doi.org/10.1124/jpet.301.1.174
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Influence of Porcine Actinobacillus pleuropneumoniae Infection and Dexamethasone on the Pharmacokinetic Parameters of Enrofloxacin
Lynn O. Post, Carol V. Cope, Dorothy E. Farrell, John D. Baker and Michael J. Myers

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 217-222; DOI: https://doi.org/10.1124/jpet.301.1.217
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Human Organic Anion Transporters and Human Organic Cation Transporters Mediate Renal Transport of Prostaglandins
Hiroaki Kimura, Michio Takeda, Shinichi Narikawa, Atsushi Enomoto, Kimiyoshi Ichida and Hitoshi Endou

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 293-298; DOI: https://doi.org/10.1124/jpet.301.1.293
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Kinetic Interactions of Dopamine and Dobutamine with Human Catechol-O-methyltransferase and Monoamine Oxidase in Vitro
Maohe Yan, Leslie T. Webster and Jeffrey L. Blumer

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 315-321; DOI: https://doi.org/10.1124/jpet.301.1.315
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In Vitro Analysis of Human Drug Glucuronidation and Prediction of in Vivo Metabolic Clearance
M. G. Soars, B. Burchell and R. J. Riley

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 382-390; DOI: https://doi.org/10.1124/jpet.301.1.382
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Intranasal Delivery of Morphine
L. Illum, P. Watts, A. N. Fisher, M. Hinchcliffe, H. Norbury, I. Jabbal-Gill, R. Nankervis and S. S. Davis

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 391-400; DOI: https://doi.org/10.1124/jpet.301.1.391

BEHAVIORAL PHARMACOLOGY

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Effects of (±)-4-{[2-(1-Methyl-2-pyrrolidinyl)ethyl]thio}phenol Hydrochloride (SIB-1553A), a Selective Ligand for Nicotinic Acetylcholine Receptors, in Tests of Visual Attention and Distractibility in Rats and Monkeys
A. V. Terry, V. B. Risbrough, J. J. Buccafusco and F. Menzaghi

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 284-292; DOI: https://doi.org/10.1124/jpet.301.1.284

CARDIOVASCULAR

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Sustained Activation of p38 Mitogen-Activated Protein Kinase Contributes to the Vascular Response to Injury
Haisong Ju, Sandhya Nerurkar, Charles F. Sauermelch, Alan R. Olzinski, Rosanna Mirabile, Dawn Zimmerman, John C. Lee, Jerry Adams, Joseph Sisko, Marinella Berova and Robert N. Willette

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 15-20; DOI: https://doi.org/10.1124/jpet.301.1.15
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The Angiotensin Type 1 Receptor Antagonist, Eprosartan, Attenuates the Progression of Renal Disease in Spontaneously Hypertensive Stroke-Prone Rats with Accelerated Hypertension
Christian T. Abrahamsen, Frank C. Barone, Wallace G. Campbell, Allen H. Nelson, Lisa C. Contino, Mark A. Pullen, Eugene T. Grygielko, Richard M. Edwards, Nicholas J. Laping and David P. Brooks

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 21-28; DOI: https://doi.org/10.1124/jpet.301.1.21
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Differential Effects of Bucindolol and Carvedilol on Noradenaline-Induced Hypertrophic Response in Ventricular Cardiomyocytes of Adult Rats
Klaus Pönicke, Ingrid Heinroth-Hoffmann and Otto-Erich Brodde

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 71-76; DOI: https://doi.org/10.1124/jpet.301.1.71
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Altered Cardiovascular Responses in Mice Lacking the M₁ Muscarinic Acetylcholine Receptor
Sandrine N. Hardouin, Keith N. Richmond, Andrew Zimmerman, Susan E. Hamilton, Eric O. Feigl and Neil M. Nathanson

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 129-137; DOI: https://doi.org/10.1124/jpet.301.1.129
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Cardiovascular Responses Elicited by the “Binge” Administration of Methamphetamine
Kurt J. Varner, Brian A. Ogden, Joseph Delcarpio and Suzanne Meleg-Smith

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 152-159; DOI: https://doi.org/10.1124/jpet.301.1.152
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In Vivo α₁-Adrenergic Lipolytic Activity in Subcutaneous Adipose Tissue of Obese Subjects
M. Flechtner-Mors, C. P. Jenkinson, A. Alt, G. Adler and H. H. Ditschuneit

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 229-233; DOI: https://doi.org/10.1124/jpet.301.1.229
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Differential Effects of Sarcolemmal and Mitochondrial K_ATP Channels Activated by 17β-Estradiol on Reperfusion Arrhythmias and Infarct Sizes in Canine Hearts
Chang-Her Tsai, Sheng-Fang Su, Tsai-Fwu Chou and Tsung-Ming Lee

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 234-240; DOI: https://doi.org/10.1124/jpet.301.1.234
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Inhibitors of Pentose Phosphate Pathway Cause Vasodilation: Involvement of Voltage-Gated Potassium Channels
Sachin A. Gupte, Kai-Xun Li, Takao Okada, Koichi Sato and Masahiko Oka

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 299-305; DOI: https://doi.org/10.1124/jpet.301.1.299
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Cyclosporine Adversely Affects Baroreflexes via Inhibition of Testosterone Modulation of Cardiac Vagal Control
Mahmoud M. El-Mas, Elham A. Afify, Amal G. Omar and Fouad M. Sharabi

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 346-354; DOI: https://doi.org/10.1124/jpet.301.1.346

CELLULAR AND MOLECULAR

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β₁-Selective Agonist (−)-1-(3,4-Dimethoxyphenetylamino)-3-(3,4-dihydroxy)-2-propanol [(−)-RO363] Differentially Interacts with Key Amino Acids Responsible for β₁-Selective Binding in Resting and Active States
Yoshiyuki Sugimoto, Reiko Fujisawa, Ryuji Tanimura, Anne Laure Lattion, Susanna Cotecchia, Gozoh Tsujimoto, Taku Nagao and Hitoshi Kurose

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 51-58; DOI: https://doi.org/10.1124/jpet.301.1.51
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Ethanol Stimulates cAMP-Responsive Element (CRE)-Mediated Transcription via CRE-Binding Protein and cAMP-Dependent Protein Kinase
Orna Asher, Thomas D. Cunningham, Lina Yao, Adrienne S. Gordon and Ivan Diamond

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 66-70; DOI: https://doi.org/10.1124/jpet.301.1.66
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Activation of Endogenous Nitric Oxide Synthase Coupled with Methacholine-Induced Exocytosis in Rat Parotid Acinar Cells
Yasuko Ishikawa, Hirokazu Iida, Mariusz T. Skowronski and Hajime Ishida

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 355-363; DOI: https://doi.org/10.1124/jpet.301.1.355

CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY

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Novel Glutathione-Dependent Thiopurine Prodrugs: Evidence for Enhanced Cytotoxicity in Tumor Cells and for Decreased Bone Marrow Toxicity in Mice
Sjofn Gunnarsdottir, Marian Rucki and Adnan A. Elfarra

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 77-86; DOI: https://doi.org/10.1124/jpet.301.1.77
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Dose Optimization of a Doxorubicin Prodrug (HMR 1826) in Isolated Perfused Human Lungs: Low Tumor pH Promotes Prodrug Activation by β-Glucuronidase
Thomas E. Mürdter, Godehard Friedel, Janne T. Backman, Monika McClellan, Monika Schick, Manfred Gerken, Klaus Bosslet, Peter Fritz, Heikki Toomes, Heyo K. Kroemer and Bernhard Sperker

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 223-228; DOI: https://doi.org/10.1124/jpet.301.1.223

ENDOCRINE AND REPRODUCTIVE

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Pharmacological Profile of a New, Potent, and Long-Acting Gonadotropin-Releasing Hormone Antagonist: Degarelix
Pierre Broqua, Pierre J.-M. Riviere, P. Michael Conn, Jean E. Rivier, Michel L. Aubert and Jean-Louis Junien

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 95-102; DOI: https://doi.org/10.1124/jpet.301.1.95
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Role of Protein Kinase C in Control of Ethanol-Modulated β-Endorphin Release from Hypothalamic Neurons in Primary Cultures
Alok De, Nadka Boyadjieva and Dipak K. Sarkar

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 119-128; DOI: https://doi.org/10.1124/jpet.301.1.119

GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

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Elucidation of Vasoactive Intestinal Peptide Pharmacophore for VPAC₁ Receptors in Human, Rat, and Guinea Pig
Hisato Igarashi, Tetsuhide Ito, Wei Hou, Samuel A. Mantey, Tapas K. Pradhan, Charles D. Ulrich, Simon J. Hocart, David H. Coy and Robert T. Jensen

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 37-50; DOI: https://doi.org/10.1124/jpet.301.1.37

INFLAMMATION AND IMMUNOPHARMACOLOGY

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New Cytokine Delivery System Using Gelatin Microspheres Containing Interleukin-10 for Experimental Inflammatory Bowel Disease
Hiroshi Nakase, Kazuichi Okazaki, Yasuhiko Tabata, Makoto Ozeki, Norihiko Watanabe, Masaya Ohana, Suguru Uose, Kazushige Uchida, Toshiki Nishi, Minoru Mastuura, Hiroyuki Tamaki, Toshiyuki Itoh, Chiharu Kawanami and Tsutomu Chiba

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 59-65; DOI: https://doi.org/10.1124/jpet.301.1.59
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Priming of Alveolar Macrophage Respiratory Burst by H₂O₂ Is Prevented by Phosphatidylcholine-Specific Phospholipase C Inhibitor Tricyclodecan-9-yl-xanthate (D609)
Julio Girón-Calle, Kousthub Srivatsa and Henry Jay Forman

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 87-94; DOI: https://doi.org/10.1124/jpet.301.1.87
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Inhibitors of ATP-Binding Cassette Transporters Suppress Interleukin-12 p40 Production and Major Histocompatibility Complex II Up-Regulation in Macrophages
György Haskó, Edwin A. Deitch, Zoltán H. Németh, David G. Kuhel and Csaba Szabó

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 103-110; DOI: https://doi.org/10.1124/jpet.301.1.103
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Pharmacological Profile of a Novel Phosphodiesterase 4 Inhibitor, 4-(8-Benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridin-6-yl)-benzoic Acid (NVP-ABE171), a 1,7-Naphthyridine Derivative, with Anti-Inflammatory Activities
Alexandre Trifilieff, Daniel Wyss, Christoph Walker, Lazzaro Mazzoni and Rene Hersperger

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 241-248; DOI: https://doi.org/10.1124/jpet.301.1.241
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The Selective Phosphodiesterase 4 Inhibitor RP 73-401 Reduced Matrix Metalloproteinase 9 Activity and Transforming Growth Factor-β Release During Acute Lung Injury in Mice: The Role of the Balance Between Tumor Necrosis Factor-α and Interleukin-10
Marianne Corbel, Noëlla Germain, Jérôme Lanchou, Sophie Molet, Patricia M. R. e Silva, Marco A. Martins, Elisabeth Boichot and Vincent Lagente

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 258-265; DOI: https://doi.org/10.1124/jpet.301.1.258

NEUROPHARMACOLOGY

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Prevention of in Vivo Excitotoxicity by a Family of Trialkylglycines, a Novel Class of Neuroprotectants
Carmina Montoliu, Marc Humet, Juan-José Canales, Jozef Burda, Rosa Planells-Cases, Francisco Sánchez-Baeza, Teresa Carbonell, Enrique Pérez-Payá, Angel Messeguer, Antonio Ferrer-Montiel and Vicente Felipo

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 29-36; DOI: https://doi.org/10.1124/jpet.301.1.29
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3,4-Methylenedioxymethamphetamine Produces Glycogenolysis and Increases the Extracellular Concentration of Glucose in the Rat Brain
Altaf S. Darvesh, Mahalakshmi Shankaran and Gary A. Gudelsky

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 138-144; DOI: https://doi.org/10.1124/jpet.301.1.138
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Tranexamic Acid, a Widely Used Antifibrinolytic Agent, Causes Convulsions by a γ-Aminobutyric Acid_A Receptor Antagonistic Effect
Roman Furtmüller, Michael G. Schlag, Michael Berger, Rudolf Hopf, Sigismund Huck, Werner Sieghart and Heinz Redl

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 168-173; DOI: https://doi.org/10.1124/jpet.301.1.168
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Effects of Acute and Subchronic Administration of Dexefaroxan, an α₂-Adrenoceptor Antagonist, on Memory Performance in Young Adult and Aged Rodents
Philippe Chopin, Francis C. Colpaert and Marc Marien

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 187-196; DOI: https://doi.org/10.1124/jpet.301.1.187
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Differential Effects of Haloperidol and Clozapine on [³H]cAMP Binding, Protein Kinase A (PKA) Activity, and mRNA and Protein Expression of Selective Regulatory and Catalytic Subunit Isoforms of PKA in Rat Brain
Yogesh Dwivedi, Hooriyah S. Rizavi and Ghanshyam N. Pandey

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 197-209; DOI: https://doi.org/10.1124/jpet.301.1.197
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Neuroprotective Effect of (2S,3S,4R)-N"-cyano-N-(6-amino-3, 4-dihydro-3-hydroxy-2-methyl-2-dimethoxymethyl-2H-benzopyran-4-yl)-N′-benzylguanidine (KR-31378), a Benzopyran Analog, against Focal Ischemic Brain Damage in Rats
Ki Whan Hong, Ki Young Kim, Jeong Hyun Lee, Hwa Kyoung Shin, Yong Geun Kwak, Sun-Ok Kim, Hong Lim and Sung-Eun Yoo

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 210-216; DOI: https://doi.org/10.1124/jpet.301.1.210
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Attenuation of Scopolamine-Induced and Age-Associated Memory Impairments by the Sigma and 5-Hydroxytryptamine_1A Receptor Agonist OPC-14523 (1-{3-[4-(3-chlorophenyl)-1-piperazinyl]propyl}-5-methoxy-3,4-dihydro-2[1H]-quinolinone monomethanesulfonate)
Katsura Tottori, Masami Nakai, Yasufumi Uwahodo, Takashi Miwa, Sakiko Yamada, Yasuo Oshiro, Tetsuro Kikuchi and C. Anthony Altar

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 249-257; DOI: https://doi.org/10.1124/jpet.301.1.249
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Intravenous Buprenorphine Self-Administration by Detoxified Heroin Abusers
Sandra D. Comer, Eric D. Collins and Marian W. Fischman

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 266-276; DOI: https://doi.org/10.1124/jpet.301.1.266
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In Utero Ethanol Suppresses Cerebellar Activator Protein-1 and Nuclear Factor-κB Transcriptional Activation in a Rat Fetal Alcohol Syndrome Model
George K. Acquaah-Mensah, James P. Kehrer and Steven W. Leslie

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 277-283; DOI: https://doi.org/10.1124/jpet.301.1.277
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ς₂-Receptor Regulation of Dopamine Transporter via Activation of Protein Kinase C
Alicia E. Derbez, Rupal M. Mody and Linda L. Werling

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 306-314; DOI: https://doi.org/10.1124/jpet.301.1.306
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4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine Hydrochloride (SSR125543A): A Potent and Selective Corticotrophin-Releasing Factor₁ Receptor Antagonist. I. Biochemical and Pharmacological Characterization
Danielle Gully, Michel Geslin, Laurence Serva, Evelyne Fontaine, Pierre Roger, Christine Lair, Valerie Darre, Claudine Marcy, Pierre-Eric Rouby, Jacques Simiand, Josette Guitard, Georgette Gout, Regis Steinberg, Daniel Rodier, Guy Griebel, Philippe Soubrie, Marc Pascal, Rebecca Pruss, Bernard Scatton, Jean-Pierre Maffrand and Gerard Le Fur

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 322-332; DOI: https://doi.org/10.1124/jpet.301.1.322
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4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1, 3-thiazol-2-amine Hydrochloride (SSR125543A), a Potent and Selective Corticotrophin-Releasing Factor₁ Receptor Antagonist. II. Characterization in Rodent Models of Stress-Related Disorders
Guy Griebel, Jacques Simiand, Régis Steinberg, Mireille Jung, Danielle Gully, Pierre Roger, Michel Geslin, Bernard Scatton, Jean-Pierre Maffrand and Philippe Soubrié

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 333-345; DOI: https://doi.org/10.1124/jpet.301.1.333
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Characterization of μ, κ, and δ Opioid Binding in Amphibian Whole Brain Tissue Homogenates
Leslie C. Newman, Steven S. Sands, David R. Wallace and Craig W. Stevens

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 364-370; DOI: https://doi.org/10.1124/jpet.301.1.364
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Alterations in Responses of Ventral Pallidal Neurons to Excitatory Amino Acids after Long-Term Dopamine Depletion
Michael S. Turner, Laurence Mignon and T. Celeste Napier

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 371-381; DOI: https://doi.org/10.1124/jpet.301.1.371

TOXICOLOGY

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Adenovirus-Mediated Overexpression of Catalase in the Cytosolic or Mitochondrial Compartment Protects against Toxicity Caused by Glutathione Depletion in HepG2 Cells Expressing CYP2E1
Montserrat Marı́, Jingxiang Bai and Arthur I. Cederbaum

Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 111-118; DOI: https://doi.org/10.1124/jpet.301.1.111

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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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