Journal of Pharmacology and Experimental Therapeutics: 344 (3)

March 01, 2013; Volume 344,Issue 3

Highlighted Papers

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A µ-Opioid Receptor Ligand with Reduced Gastrointestinal and Respiratory Dysfunction
Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 543; DOI: https://doi.org/10.1124/jpet.112.0313HI
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The PK and PD Relationships of an Engineered Human Follistatin Variant
Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 543; DOI: https://doi.org/10.1124/jpet.112.0313HIa
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ADX71743, a Negative Allosteric Modulator of Metabotropic Glutamate Receptor 7
Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 543; DOI: https://doi.org/10.1124/jpet.112.0313HIb
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Puerarin Ameliorates Experimental Alcoholic Liver Injury
Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 543; DOI: https://doi.org/10.1124/jpet.112.0313HIc

Perspectives in Pharmacology

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Autophagy Inhibition for Chemosensitization and Radiosensitization in Cancer: Do the Preclinical Data Support This Therapeutic Strategy?
Molly L. Bristol, Sean M. Emery, Paola Maycotte, Andrew Thorburn, Shweta Chakradeo and David A. Gewirtz

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 544-552; DOI: https://doi.org/10.1124/jpet.112.199802

Behavioral Pharmacology

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Discriminative Stimulus Effects of the GABA_B Receptor-Positive Modulator rac-BHFF: Comparison with GABA_B Receptor Agonists and Drugs of Abuse
Wouter Koek, Kejun Cheng and Kenner C. Rice

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 553-560; DOI: https://doi.org/10.1124/jpet.112.202226
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Cannabinoid Discrimination and Antagonism by CB₁ Neutral and Inverse Agonist Antagonists
Brian D. Kangas, Marcus S. Delatte, V. Kiran Vemuri, Ganesh A. Thakur, Spyridon P. Nikas, Kumara V. Subramanian, Vidyanand G. Shukla, Alexandros Makriyannis and Jack Bergman

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 561-567; DOI: https://doi.org/10.1124/jpet.112.201962

Cellular and Molecular

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High-Throughput Identification and Characterization of Novel, Species-selective GPR35 Agonists
Zaynab Neetoo-Isseljee, Amanda E. MacKenzie, Craig Southern, Jeff Jerman, Edward G. McIver, Nicholas Harries, Debra L. Taylor and Graeme Milligan

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 568-578; DOI: https://doi.org/10.1124/jpet.112.201798
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Identification of Stanniocalcin 2 as a Novel Aryl Hydrocarbon Receptor Target Gene
Tod A. Harper, Aditya D. Joshi and Cornelis J. Elferink

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 579-588; DOI: https://doi.org/10.1124/jpet.112.201111

Drug Discovery and Translational Medicine

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Structure-Based Optimization of Angiostatic Agent 6DBF7, an Allosteric Antagonist of Galectin-1
Ruud P. M. Dings, Nigam Kumar, Michelle C. Miller, Melissa Loren, Huzaifa Rangwala, Thomas R. Hoye and Kevin H. Mayo

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 589-599; DOI: https://doi.org/10.1124/jpet.112.199646
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5-Benzylglycinyl-Amiloride Kills Proliferating and Nonproliferating Malignant Glioma Cells through Caspase-Independent Necroptosis Mediated by Apoptosis-Inducing Factor
Nagarekha Pasupuleti, Leonardo Leon, Kermit L. Carraway and Fredric Gorin

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 600-615; DOI: https://doi.org/10.1124/jpet.112.200519
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An Engineered Human Follistatin Variant: Insights into the Pharmacokinetic and Pharmocodynamic Relationships of a Novel Molecule with Broad Therapeutic Potential
Amita Datta-Mannan, Benjamin Yaden, Venkatesh Krishnan, Bryan E. Jones and Johnny E. Croy

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 616-623; DOI: https://doi.org/10.1124/jpet.112.201491
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ADX71743, a Potent and Selective Negative Allosteric Modulator of Metabotropic Glutamate Receptor 7: In Vitro and In Vivo Characterization
Mikhail Kalinichev, Mélanie Rouillier, Francoise Girard, Isabelle Royer-Urios, Bruno Bournique, Terry Finn, Delphine Charvin, Brice Campo, Emmanuel Le Poul, Vincent Mutel, Sonia Poli, Stuart A. Neale, Thomas E. Salt and Robert Lütjens

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 624-636; DOI: https://doi.org/10.1124/jpet.112.200915

Endocrine and Diabetes

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Pharmacological Inhibition of Mitochondrial Carbonic Anhydrases Protects Mouse Cerebral Pericytes from High Glucose-Induced Oxidative Stress and Apoptosis
Gul N. Shah, Tulin O. Price, William A. Banks, Yoichi Morofuji, Andrej Kovac, Nuran Ercal, Christine M. Sorenson, Eui S. Shin and Nader Sheibani

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 637-645; DOI: https://doi.org/10.1124/jpet.112.201400

Gastrointestinal, Hepatic, Pulmonary, and Renal

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Puerarin Ameliorates Experimental Alcoholic Liver Injury by Inhibition of Endotoxin Gut Leakage, Kupffer Cell Activation, and Endotoxin Receptors Expression
Jing-Hua Peng, Tuan Cui, Fu Huang, Liang Chen, Yu Zhao, Lin Xu, Li-Li Xu, Qin Feng and Yi-Yang Hu

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 646-654; DOI: https://doi.org/10.1124/jpet.112.201137

Metabolism, Transport, and Pharmacogenomics

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Mechanisms Limiting Distribution of the Threonine-Protein Kinase B-RaF^V600E Inhibitor Dabrafenib to the Brain: Implications for the Treatment of Melanoma Brain Metastases
Rajendar K. Mittapalli, Shruthi Vaidhyanathan, Arkadiusz Z. Dudek and William F. Elmquist

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 655-664; DOI: https://doi.org/10.1124/jpet.112.201475
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Carboxylesterase 1 as a Determinant of Clopidogrel Metabolism and Activation
Hao-Jie Zhu, Xinwen Wang, Brian E. Gawronski, Bryan J. Brinda, Dominick J. Angiolillo and John S. Markowitz

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 665-672; DOI: https://doi.org/10.1124/jpet.112.201640
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Cynomolgus Monkey as a Potential Model to Assess Drug Interactions Involving Hepatic Organic Anion Transporting Polypeptides: In Vitro, In Vivo, and In Vitro-to-In Vivo Extrapolation
Hong Shen, Zheng Yang, Gabe Mintier, Yong-Hae Han, Cliff Chen, Praveen Balimane, Mohammed Jemal, Weiping Zhao, Renjie Zhang, Sanjith Kallipatti, Sabariya Selvam, Sunil Sukrutharaj, Prasad Krishnamurthy, Punit Marathe and A. David Rodrigues

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 673-685; DOI: https://doi.org/10.1124/jpet.112.200691

Neuropharmacology

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Pharmacodynamics of Selective Inhibition of γ-Secretase by Avagacestat
Charles F. Albright, Randy C. Dockens, Jere E. Meredith, Richard E. Olson, Randy Slemmon, Kimberley A. Lentz, Jun-Sheng Wang, R. Rex Denton, Gary Pilcher, Paul W. Rhyne, Joseph J. Raybon, Donna M. Barten, Catherine Burton, Jeremy H. Toyn, Sethu Sankaranarayanan, Craig Polson, Valerie Guss, Randy White, Frank Simutis, Thomas Sanderson, Kevin W. Gillman, John E. Starrett, Joanne Bronson, Oleksandr Sverdlov, Shu-Pang Huang, Lorna Castaneda, Howard Feldman, Vlad Coric, Robert Zaczek, John E. Macor, John Houston, Robert M. Berman and Gary Tong

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 686-695; DOI: https://doi.org/10.1124/jpet.112.199356
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The Antinociceptive Effect of Milnacipran in the Monosodium Iodoacetate Model of Osteoarthritis Pain and Its Relation to Changes in Descending Inhibition
Liam J. Burnham and Anthony H. Dickenson

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 696-707; DOI: https://doi.org/10.1124/jpet.112.199489
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A G Protein-Biased Ligand at the μ-Opioid Receptor Is Potently Analgesic with Reduced Gastrointestinal and Respiratory Dysfunction Compared with Morphine
Scott M. DeWire, Dennis S. Yamashita, David H. Rominger, Guodong Liu, Conrad L. Cowan, Thomas M. Graczyk, Xiao-Tao Chen, Philip M. Pitis, Dimitar Gotchev, Catherine Yuan, Michael Koblish, Michael W. Lark and Jonathan D. Violin

Journal of Pharmacology and Experimental Therapeutics March 2013, 344 (3) 708-717; DOI: https://doi.org/10.1124/jpet.112.201616

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Table of Contents

Highlighted Papers

Perspectives in Pharmacology

Behavioral Pharmacology

Cellular and Molecular

Drug Discovery and Translational Medicine

Endocrine and Diabetes

Gastrointestinal, Hepatic, Pulmonary, and Renal

Metabolism, Transport, and Pharmacogenomics

Neuropharmacology

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