Journal of Pharmacology and Experimental Therapeutics: 323 (1)

October 01, 2007; Volume 323,Issue 1

BEHAVIORAL PHARMACOLOGY

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The Time-Course for Up- and Down-Regulation of the Cortical 5-Hydroxytryptamine (5-HT)_2A Receptor Density Predicts 5-HT_2A Receptor-Mediated Behavior in the Rabbit
Kuldip D. Dave, John A. Harvey and Vincent J. Aloyo

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 327-335; DOI: https://doi.org/10.1124/jpet.107.121707

CARDIOVASCULAR

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Methyl-β-cyclodextrin Prevents Angiotensin II-Induced Tachyphylactic Contractile Responses in Rat Aorta
A. Elizabeth Linder, Keshari M. Thakali, Janice M. Thompson, Stephanie W. Watts, R. Clinton Webb and Romulo Leite

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 78-84; DOI: https://doi.org/10.1124/jpet.107.123463
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N-Hydroxy-pyrroline Modification of Verapamil Exhibits Antioxidant Protection of the Heart against Ischemia/Reperfusion-Induced Cardiac Dysfunction without Compromising Its Calcium Antagonistic Activity
Rajarsi Mandal, Vijay Kumar Kutala, Mahmood Khan, Iyyapu K. Mohan, Saradhadevi Varadharaj, Arun Sridhar, Cynthia A. Carnes, Tamás Kálai, Kálmán Hideg and Periannan Kuppusamy

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 119-127; DOI: https://doi.org/10.1124/jpet.107.127167
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Tissue Kallikrein Is Involved in the Cardioprotective Effect of AT1-Receptor Blockade in Acute Myocardial Ischemia
Erij Messadi-Laribi, Violaine Griol-Charhbili, Anne Pizard, Marie-Pascale Vincent, Didier Heudes, Pierre Meneton, François Alhenc-Gelas and Christine Richer

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 210-216; DOI: https://doi.org/10.1124/jpet.107.124859
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Systemic Activation of the Calcium Sensing Receptor Produces Acute Effects on Vascular Tone and Circulatory Function in Uremic and Normal Rats: Focus on Central versus Peripheral Control of Vascular Tone and Blood Pressure by Cinacalcet
Ryan M. Fryer, Jason A. Segreti, Deborah L. Widomski, Pamela H. Franklin, Patricia N. Banfor, Kristin A. Koch, Masaki Nakane, J. Ruth Wu-Wong, Bryan F. Cox and Glenn A. Reinhart

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 217-226; DOI: https://doi.org/10.1124/jpet.107.123901
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Peripheral Benzodiazepine Receptor-Induced Myocardial Protection is Mediated by Inhibition of Mitochondrial Membrane Permeabilization
Fatou Nsoure Obame, Roland Zini, Rachid Souktani, Alain Berdeaux and Didier Morin

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 336-345; DOI: https://doi.org/10.1124/jpet.107.124255
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Inhibition of Ryanodine Receptors by 4-(2-Aminopropyl)-3,5-dichloro-N,N-dimethylaniline (FLA 365) in Canine Pulmonary Arterial Smooth Muscle Cells
Olga Ostrovskaya, Ravi Goyal, Noah Osman, Claire E. McAllister, Isaac N. Pessah, Joseph R. Hume and Sean M. Wilson

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 381-390; DOI: https://doi.org/10.1124/jpet.107.122119
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Activation of Large-Conductance Calcium-Activated Potassium Channels by Puerarin: The Underlying Mechanism of Puerarin-Mediated Vasodilation
Xiao-Hui Sun, Jiu-Ping Ding, Hui Li, Na Pan, Lu Gan, Xiang-Liang Yang and Hui-Bi Xu

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 391-397; DOI: https://doi.org/10.1124/jpet.107.125567

CELLULAR AND MOLECULAR

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Potent Inhibition of Native TREK-1 K⁺ Channels by Selected Dihydropyridine Ca²⁺ Channel Antagonists
Haiyan Liu, Judith A. Enyeart and John J. Enyeart

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 39-48; DOI: https://doi.org/10.1124/jpet.107.125245
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Lysophosphatidic Acid Decreases Epidermal Growth Factor Receptor Binding in Airway Epithelial Cells
Karen M. Kassel, Nancy A. Schulte, Stacey M. Parker, Aaron D. Lanik and Myron L. Toews

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 109-118; DOI: https://doi.org/10.1124/jpet.107.120584
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Sphingosine 1-Phosphate Has Dual Functions in the Regulation of Endothelial Cell Permeability and Ca²⁺ Metabolism
Kiyoshi Itagaki, Jong K. Yun, Jeremy A. Hengst, Atsuko Yatani, Carl J. Hauser, Zoltan Spolarics and Edwin A. Deitch

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 186-191; DOI: https://doi.org/10.1124/jpet.107.121210

CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY

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Combretastatin A4-Induced Differential Cytotoxicity and Reduced Metastatic Ability by Inhibition of AKT Function in Human Gastric Cancer Cells
Heng-Liang Lin, Shih-Hwa Chiou, Chew-Wun Wu, Wen-Bin Lin, Li-Hsin Chen, Yi-Ping Yang, Ming-Long Tsai, Yih-Huei Uen, Jing-Ping Liou and Chin-Wen Chi

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 365-373; DOI: https://doi.org/10.1124/jpet.107.124966
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A Novel Oral Indoline-Sulfonamide Agent, N-[1-(4-Methoxybenzenesulfonyl)-2,3-dihydro-1H-indol-7-yl]-Isonicotinamide (J30), Exhibits Potent Activity against Human Cancer Cells in Vitro and in Vivo through the Disruption of Microtubule
Jing-Ping Liou, Kuo-Shun Hsu, Ching-Chuan Kuo, Chi-Yen Chang and Jang-Yang Chang

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 398-405; DOI: https://doi.org/10.1124/jpet.107.126680

ENDOCRINE AND DIABETES

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Simvastatin Protects against Multiple Low-Dose Streptozotocin-Induced Type 1 Diabetes in CD-1 Mice and Recurrence of Disease in Nonobese Diabetic Mice
Tobias Rydgren, Outi Vaarala and Stellan Sandler

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 180-185; DOI: https://doi.org/10.1124/jpet.107.122655

GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

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Isothiocyanate Inhibits Restitution and Wound Repair after Injury in the Stomach: Ex Vivo and in Vitro Studies
Regina Ragasa, Eiji Nakamura, Lisa Marrone, Saeko Yanaka, Shusaku Hayashi, Koji Takeuchi and Susan J. Hagen

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 1-9; DOI: https://doi.org/10.1124/jpet.107.121640
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Angiotensin II Type 1 Receptor-Dependent Nuclear Factor-κB Activation-Mediated Proinflammatory Actions in a Rat Model of Obstructive Acute Pancreatitis
Yuk Cheung Chan and Po Sing Leung

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 10-18; DOI: https://doi.org/10.1124/jpet.107.124891
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Intra-Renal Angiotensin II/AT₁ Receptor, Oxidative Stress, Inflammation, and Progressive Injury in Renal Mass Reduction
N. D. Vaziri, Y. Bai, Z. Ni, Y. Quiroz, R. Pandian and B. Rodriguez-Iturbe

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 85-93; DOI: https://doi.org/10.1124/jpet.107.123638
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Effects of Melatonin on Gallbladder Neuromuscular Function in Acute Cholecystitis
Pedro J. Gomez-Pinilla, Pedro J. Camello and María J. Pozo

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 138-146; DOI: https://doi.org/10.1124/jpet.107.123240
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GW427353 (Solabegron), a Novel, Selective β₃-Adrenergic Receptor Agonist, Evokes Bladder Relaxation and Increases Micturition Reflex Threshold in the Dog
Alexandra Hicks, Gerald P. McCafferty, Erin Riedel, Nambi Aiyar, Mark Pullen, Christopher Evans, Trudy D. Luce, Robert W. Coatney, Gian C. Rivera, Timothy D. Westfall and J. Paul Hieble

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 202-209; DOI: https://doi.org/10.1124/jpet.107.125757
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Pharmacological Profile of Novel Acid Pump Antagonist 7-(4-Fluorobenzyloxy)-2,3-dimethyl-1-{[(1S,2S)-2-methyl cyclopropyl]methyl}-1H-pyrrolo[2,3-d]pyridazine (CS-526)
Keiichi Ito, Kazuya Kinoshita, Atsuyuki Tomizawa, Fumi Inaba, Yuka Morikawa-Inomata, Mitsuko Makino, Keiichi Tabata and Nobuhiko Shibakawa

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 308-317; DOI: https://doi.org/10.1124/jpet.107.121350

INFLAMMATION, IMMUNOPHARMACOLOGY, AND ASTHMA

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Antieosinophilic Activity of Simendans
Hannu Kankaanranta, Xianzhi Zhang, Ritva Tumelius, Minna Ruotsalainen, Heimo Haikala, Erkki Nissinen and Eeva Moilanen

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 31-38; DOI: https://doi.org/10.1124/jpet.107.124057
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Gastric Antisecretory Drugs Induce Leukocyte-Endothelial Cell Interactions through Gastrin Release and Activation of CCK-2 Receptors
Ángeles Álvarez, M. Sales Ibiza, Mario M. Andrade, Ana Blas-García and Sara Calatayud

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 406-413; DOI: https://doi.org/10.1124/jpet.107.122754

METABOLISM, TRANSPORT, AND PHARMACOGENOMICS

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A Global Drug Inhibition Pattern for the Human ATP-Binding Cassette Transporter Breast Cancer Resistance Protein (ABCG2)
Pär Matsson, Gunilla Englund, Gustav Ahlin, Christel A. S. Bergström, Ulf Norinder and Per Artursson

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 19-30; DOI: https://doi.org/10.1124/jpet.107.124768
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Expression and Characterization of a Human Carboxylesterase 2 Splice Variant
Marissa A. Schiel, Scheri-lyn Green, Wilhelmina I. Davis, Paresh C. Sanghani, William F. Bosron and Sonal P. Sanghani

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 94-101; DOI: https://doi.org/10.1124/jpet.107.127027
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Long-Term Effect of Leptin on H⁺-Coupled Peptide Cotransporter 1 Activity and Expression in Vivo: Evidence in Leptin-Deficient Mice
Patrick Hindlet, André Bado, Robert Farinotti and Marion Buyse

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 192-201; DOI: https://doi.org/10.1124/jpet.107.125799
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Localization of the Human Breast Cancer Resistance Protein (BCRP/ABCG2) in Lipid Rafts/Caveolae and Modulation of Its Activity by Cholesterol in Vitro
Caroline Henrike Storch, Robert Ehehalt, Walter Emil Haefeli and Johanna Weiss

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 257-264; DOI: https://doi.org/10.1124/jpet.107.122994

NEUROPHARMACOLOGY

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Pharmacological Manipulation of Neuronal Ensemble Activity by Reverse Microdialysis in Freely Moving Rats: A Comparative Study of the Effects of Tetrodotoxin, Lidocaine, and Muscimol
E. van Duuren, G. van der Plasse, R. van der Blom, R. N. J. M. A. Joosten, A. B. Mulder, C. M. A. Pennartz and M. G. P. Feenstra

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 61-69; DOI: https://doi.org/10.1124/jpet.107.124784
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P2 Receptor Antagonist Trinitrophenyl-Adenosine-Triphosphate Protects Hippocampus from Oxygen and Glucose Deprivation Cell Death
Fabio Cavaliere, Susanna Amadio, Klaus Dinkel, Klaus G. Reymann and Cinzia Volonté

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 70-77; DOI: https://doi.org/10.1124/jpet.106.119024
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Ex Vivo Occupancy of γ-Secretase Inhibitors Correlates with Brain β-Amyloid Peptide Reduction in Tg2576 Mice
Margi E. Goldstein, Yang Cao, Tracey Fiedler, Jeremy Toyn, Lawrence Iben, Donna M. Barten, Maria Pierdomenico, Jason Corsa, C. V. C. Prasad, Richard E. Olson, Yu-Wen Li, Robert Zaczek and Charles F. Albright

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 102-108; DOI: https://doi.org/10.1124/jpet.107.125492
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Repeated Administration of Vanilloid Receptor TRPV1 Antagonists Attenuates Hyperthermia Elicited by TRPV1 Blockade
Narender R. Gavva, Anthony W. Bannon, David N. Hovland, Sonya G. Lehto, Lana Klionsky, Sekhar Surapaneni, David C. Immke, Charles Henley, Leyla Arik, Annette Bak, James Davis, Nadia Ernst, Gal Hever, Rongzhen Kuang, Licheng Shi, Rami Tamir, Jue Wang, Weiya Wang, Gary Zajic, Dawn Zhu, Mark H. Norman, Jean-Claude Louis, Ella Magal and James J. S. Treanor

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 128-137; DOI: https://doi.org/10.1124/jpet.107.125674
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In Vitro Pharmacological Characterization of Novel Isoxazolopyridone Derivatives as Allosteric Metabotropic Glutamate Receptor 7 Antagonists
Gentaroh Suzuki, Naohiro Tsukamoto, Hiroshi Fushiki, Aki Kawagishi, Masayuki Nakamura, Hideki Kurihara, Morihiro Mitsuya, Mitsuru Ohkubo and Hisashi Ohta

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 147-156; DOI: https://doi.org/10.1124/jpet.107.124701
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Stimulation of the P2Y₁ Receptor Up-Regulates Nucleoside-Triphosphate Diphosphohydrolase-1 in Human Retinal Pigment Epithelial Cells
Wennan Lu, David Reigada, Jean Sévigny and Claire H. Mitchell

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 157-164; DOI: https://doi.org/10.1124/jpet.107.124545
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Antiepileptic Drug-Induced Neuronal Cell Death in the Immature Brain: Effects of Carbamazepine, Topiramate, and Levetiracetam as Monotherapy versus Polytherapy
Jinsook Kim, Alexei Kondratyev and Karen Gale

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 165-173; DOI: https://doi.org/10.1124/jpet.107.126250
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Activation of Urothelial Transient Receptor Potential Vanilloid 4 by 4α-Phorbol 12,13-Didecanoate Contributes to Altered Bladder Reflexes in the Rat
Lori Birder, F. Aura Kullmann, Hyosang Lee, Stacey Barrick, William de Groat, Anthony Kanai and Michael Caterina

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 227-235; DOI: https://doi.org/10.1124/jpet.107.125435
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Neuroactive Steroids and Human Recombinant ρ1 GABA Receptors
Wenjun Li, Xiaochun Jin, Douglas F. Covey and Joe Henry Steinbach

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 236-247; DOI: https://doi.org/10.1124/jpet.107.127365
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Agonist Induced-Phosphorylation of G_α11 Protein Reduces Coupling to 5-HT_2A Receptors
Ju Shi, Katerina J. Damjanoska, Rakesh K. Singh, Gonzalo A. Carrasco, Francisca Garcia, Angela J. Grippo, Michelle Landry, Nicole R. Sullivan, George Battaglia and Nancy A. Muma

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 248-256; DOI: https://doi.org/10.1124/jpet.107.122317
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(–)-(1R,2R)-3-(3-Dimethylamino-1-ethyl-2-methyl-propyl)-phenol Hydrochloride (Tapentadol HCl): a Novel μ-Opioid Receptor Agonist/Norepinephrine Reuptake Inhibitor with Broad-Spectrum Analgesic Properties
Thomas M. Tzschentke, Thomas Christoph, Babette Kögel, Klaus Schiene, Hagen-Heinrich Hennies, Werner Englberger, Michael Haurand, Ulrich Jahnel, Thomas I. F. H. Cremers, Elmar Friderichs and Jean De Vry

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 265-276; DOI: https://doi.org/10.1124/jpet.107.126052
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Evaluation of Levodopa Dose and Magnitude of Dopamine Depletion as Risk Factors for Levodopa-Induced Dyskinesia in a Rat Model of Parkinson's Disease
Daniel B. Putterman, Adam C. Munhall, Laura B. Kozell, John K. Belknap and Steven W. Johnson

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 277-284; DOI: https://doi.org/10.1124/jpet.107.126219
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[³H]A-778317 [1-((R)-5-tert-Butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a Novel, Stereoselective, High-Affinity Antagonist Is a Useful Radioligand for the Human Transient Receptor Potential Vanilloid-1 (TRPV1) Receptor
Bruce R. Bianchi, Rachid El Kouhen, Torben R. Neelands, Chih-Hung Lee, Arthur Gomtsyan, Shirish N. Raja, Sriajan N. Vaidyanathan, Bruce Surber, Heath A. McDonald, Carol S. Surowy, Connie R. Faltynek, Robert B. Moreland, Michael F. Jarvis and Pamela S. Puttfarcken

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 285-293; DOI: https://doi.org/10.1124/jpet.107.124305
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An Allosteric Modulator of the α7 Nicotinic Acetylcholine Receptor Possessing Cognition-Enhancing Properties in Vivo
Daniel B. Timmermann, Jens Halvard Grønlien, Kathy L. Kohlhaas, Elsebet Ø. Nielsen, Eva Dam, Tino D. Jørgensen, Philip K. Ahring, Dan Peters, Dorte Holst, Jeppe K. Chrsitensen, John Malysz, Clark A. Briggs, Murali Gopalakrishnan and Gunnar M. Olsen

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 294-307; DOI: https://doi.org/10.1124/jpet.107.120436
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Blockade of Cannabinoid Type 1 Receptors Augments the Antiparkinsonian Action of Levodopa without Affecting Dyskinesias in 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine-Treated Rhesus Monkeys
Xuebing Cao, Li Liang, John R. Hadcock, Philip A. Iredale, David A. Griffith, Frank S. Menniti, Stewart Factor, J. Timothy Greenamyre and Stella M. Papa

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 318-326; DOI: https://doi.org/10.1124/jpet.107.125666
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Pharmacokinetics and Pharmacodynamics of Seven Opioids in P-Glycoprotein-Competent Mice: Assessment of Unbound Brain EC_50,u and Correlation of in Vitro, Preclinical, and Clinical Data
J. Cory Kalvass, Emily R. Olson, Michael P. Cassidy, Dana E. Selley and Gary M. Pollack

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 346-355; DOI: https://doi.org/10.1124/jpet.107.119560
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Calcium Release from Presynaptic Internal Stores Is Required for Ethanol to Increase Spontaneous γ-Aminobutyric Acid Release onto Cerebellum Purkinje Neurons
M. Katherine Kelm, Hugh E. Criswell and George R. Breese

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 356-364; DOI: https://doi.org/10.1124/jpet.107.126144
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[N-Allyl-Dmt¹]-Endomorphins Are μ-Opioid Receptor Antagonists Lacking Inverse Agonist Properties
Ewa D. Marczak, Yunden Jinsmaa, Tingyou Li, Sharon D. Bryant, Yuko Tsuda, Yoshio Okada and Lawrence H. Lazarus

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 374-380; DOI: https://doi.org/10.1124/jpet.107.125807

TOXICOLOGY

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Effects of Endogenous Ascorbate on Oxidation, Oxygenation, and Toxicokinetics of Cell-Free Modified Hemoglobin after Exchange Transfusion in Rat and Guinea Pig
Paul W. Buehler, Felice D'Agnillo, Victoria Hoffman and Abdu I. Alayash

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 49-60; DOI: https://doi.org/10.1124/jpet.107.126409
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Gambierol Acts as a Functional Antagonist of Neurotoxin Site 5 on Voltage-Gated Sodium Channels in Cerebellar Granule Neurons
K. T. LePage, J. D. Rainier, H. W. B. Johnson, D. G. Baden and T. F. Murray

Journal of Pharmacology and Experimental Therapeutics October 2007, 323 (1) 174-179; DOI: https://doi.org/10.1124/jpet.107.124271

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Table of Contents

BEHAVIORAL PHARMACOLOGY

CARDIOVASCULAR

CELLULAR AND MOLECULAR

CHEMOTHERAPY, ANTIBIOTICS, AND GENE THERAPY

ENDOCRINE AND DIABETES

GASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

INFLAMMATION, IMMUNOPHARMACOLOGY, AND ASTHMA

METABOLISM, TRANSPORT, AND PHARMACOGENOMICS

NEUROPHARMACOLOGY

TOXICOLOGY

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