Journal of Pharmacology and Experimental Therapeutics: 365 (3)

June 01, 2018; Volume 365,Issue 3

Cardiovascular

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Inhibition of the α-Subunit of Phosphoinositide 3-Kinase in Heart Increases Late Sodium Current and Is Arrhythmogenic
Tao Yang, David F. Meoli, Javid Moslehi and Dan M. Roden

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 460-466; DOI: https://doi.org/10.1124/jpet.117.246157
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Transient Receptor Potential Melastatin-8 Activation Induces Relaxation of Pulmonary Artery by Inhibition of Store-Operated Calcium Entry in Normoxic and Chronic Hypoxic Pulmonary Hypertensive Rats
Yun-Ping Mu, Da-Cen Lin, Si-Yi Zheng, Hai-Xia Jiao, James S. K. Sham and Mo-Jun Lin

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 544-555; DOI: https://doi.org/10.1124/jpet.117.247320
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New Targets for Old Drugs: Cardiac Glycosides Inhibit Atrial-Specific K_2P3.1 (TASK-1) Channels
Constanze Schmidt, Felix Wiedmann, Anne-Rike Gaubatz, Antonius Ratte, Hugo A. Katus and Dierk Thomas

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 614-623; DOI: https://doi.org/10.1124/jpet.118.247692
Open Access
Pharmacological Characterization of IW-1973, a Novel Soluble Guanylate Cyclase Stimulator with Extensive Tissue Distribution, Antihypertensive, Anti-Inflammatory, and Antifibrotic Effects in Preclinical Models of Disease
Jenny V. Tobin, Daniel P. Zimmer, Courtney Shea, Peter Germano, Sylvie G. Bernier, Guang Liu, Kim Long, Joy Miyashiro, Sheila Ranganath, Sarah Jacobson, Kim Tang, G-Yoon Jamie Im, James Sheppeck, Joel D. Moore, Kristine Sykes, James Wakefield, Renee Sarno, Ali R. Banijamali, Albert T. Profy, G. Todd Milne, Mark G. Currie and Jaime L. Masferrer

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 664-675; DOI: https://doi.org/10.1124/jpet.117.247429

Cellular and Molecular

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Sepiapterin Enhances Tumor Radio- and Chemosensitivities by Promoting Vascular Normalization
Christopher S. Rabender, Ninu Bruno, Asim Alam, Gobalakrishnan Sundaresan, Jamal Zweit and Ross B. Mikkelsen

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 536-543; DOI: https://doi.org/10.1124/jpet.117.245258
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TCL1A, a Novel Transcription Factor and a Coregulator of Nuclear Factor κB p65: Single Nucleotide Polymorphism and Estrogen Dependence
Ming-Fen Ho, Edroaldo Lummertz da Rocha, Cheng Zhang, James N. Ingle, Paul E. Goss, Lois E. Shepherd, Michiaki Kubo, Liewei Wang, Hu Li and Richard M. Weinshilboum

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 700-710; DOI: https://doi.org/10.1124/jpet.118.247718

Chemotherapy, Antibiotics, and Gene Therapy

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Hydroxychloroquine: A Physiologically-Based Pharmacokinetic Model in the Context of Cancer-Related Autophagy Modulation
Keagan P. Collins, Kristen M. Jackson and Daniel L. Gustafson

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 447-459; DOI: https://doi.org/10.1124/jpet.117.245639

Drug Discovery and Translational Medicine

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Indomethacin Enhances Brown Fat Activity
Lei Hao, Jamie Kearns, Sheyenne Scott, Dayong Wu, Sean D. Kodani, Christophe Morisseau, Bruce D. Hammock, Xiaocun Sun, Ling Zhao and Shu Wang

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 467-475; DOI: https://doi.org/10.1124/jpet.117.246256
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Bioengineered Noncoding RNAs Selectively Change Cellular miRNome Profiles for Cancer Therapy
Pui Yan Ho, Zhijian Duan, Neelu Batra, Joseph L. Jilek, Mei-Juan Tu, Jing-Xin Qiu, Zihua Hu, Theodore Wun, Primo N. Lara, Ralph W. DeVere White, Hong-Wu Chen and Ai-Ming Yu

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 494-506; DOI: https://doi.org/10.1124/jpet.118.247775
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AZD7624, an Inhaled p38 Inhibitor, Demonstrates Local Lung Inhibition of LPS-Induced TNFα with Minimal Systemic Exposure
Rikard Pehrson, Tove Hegelund-Myrbäck, Danen Cunoosamy, Sara Asimus, Paul Jansson, Naimish Patel, Annika Borde and Sofia Lundin

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 567-572; DOI: https://doi.org/10.1124/jpet.117.246132
Open Access
Binding Characteristics and Analgesic Effects of Mirogabalin, a Novel Ligand for the α₂δ Subunit of Voltage-Gated Calcium Channels
Yuki Domon, Naohisa Arakawa, Tatsuya Inoue, Fumihiko Matsuda, Makoto Takahashi, Naotoshi Yamamura, Kiyonori Kai and Yutaka Kitano

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 573-582; DOI: https://doi.org/10.1124/jpet.117.247551
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In Vitro Pharmacological Characterization and In Vivo Validation of LSN3172176 a Novel M1 Selective Muscarinic Receptor Agonist Tracer Molecule for Positron Emission Tomography
Adrian J. Mogg, Thomas Eessalu, Megan Johnson, Rebecca Wright, Helen E. Sanger, Hongling Xiao, Michael G. Crabtree, Alex Smith, Ellen M. Colvin, Douglas Schober, Donald Gehlert, Cynthia Jesudason, Paul J. Goldsmith, Michael P. Johnson, Christian C. Felder, Vanessa N. Barth and Lisa M. Broad

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 602-613; DOI: https://doi.org/10.1124/jpet.117.246454
Open Access
Selective Prostacyclin Receptor Agonist Selexipag, in Contrast to Prostacyclin Analogs, Does Not Evoke Paradoxical Vasoconstriction of the Rat Femoral Artery
Keith Morrison, Franck Haag, Roland Ernst, Marc Iglarz and Martine Clozel

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 727-733; DOI: https://doi.org/10.1124/jpet.117.246058
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Network-Based Analysis of Bortezomib Pharmacodynamic Heterogeneity in Multiple Myeloma Cells
Vidya Ramakrishnan and Donald E. Mager

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 734-751; DOI: https://doi.org/10.1124/jpet.118.247924

Endocrine and Diabetes

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Protectin DX Ameliorates Hepatic Steatosis by Suppression of Endoplasmic Reticulum Stress via AMPK-Induced ORP150 Expression
Tae Woo Jung, Eun Jung Kyung, Hyoung-Chun Kim, Yong Kyu Shin, Sung Hoon Lee, Eon Sub Park, Ahmet Hacımüftüoğlu, A. M. Abd El-Aty and Ji Hoon Jeong

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 485-493; DOI: https://doi.org/10.1124/jpet.117.246686
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AICAR Prevents Acute Olanzapine-Induced Disturbances in Glucose Homeostasis
Natasha D. Bush, Logan K. Townsend and David C. Wright

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 526-535; DOI: https://doi.org/10.1124/jpet.118.248393

Gastrointestinal, Hepatic, Pulmonary, and Renal

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Ultrasound Combined with Microbubbles Enhances the Effects of Methylprednisolone in Lipopolysaccharide-Induced Human Mesangial Cells
Peng-Fei Sun, Tian Tian, Li-Na Chen, Rong-Guo Fu, Shan-Shan Xu, Hong Ai, Bing Wang, Jian Zhang, Ruo-Yan Si, Zhonglin Chai, Mark E. Cooper and Shu-Ting Ren

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 476-484; DOI: https://doi.org/10.1124/jpet.117.246223
Open Access
Potent Sodium/Glucose Cotransporter SGLT1/2 Dual Inhibition Improves Glycemic Control Without Marked Gastrointestinal Adaptation or Colonic Microbiota Changes in Rodents
Fuyong Du, Simon A. Hinke, Cassandre Cavanaugh, David Polidori, Nathanial Wallace, Thomas Kirchner, Matthew Jennis, Wensheng Lang, Gee-Hong Kuo, Micheal D. Gaul, James Lenhard, Keith Demarest, Nadim J. Ajami, Yin Liang and Pamela J. Hornby

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 676-687; DOI: https://doi.org/10.1124/jpet.118.248575

Inflammation, Immunopharmacology, and Asthma

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Anti-inflammatory Properties of Cannabidiol, a Nonpsychotropic Cannabinoid, in Experimental Allergic Contact Dermatitis
Stefania Petrosino, Roberta Verde, Massimo Vaia, Marco Allarà, Teresa Iuvone and Vincenzo Di Marzo

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 652-663; DOI: https://doi.org/10.1124/jpet.117.244368

Metabolism, Transport, and Pharmacogenomics

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In Vitro Assessment of Pharmacokinetic Drug-Drug Interactions of Direct Oral Anticoagulants: Type 5-Phosphodiesterase Inhibitors Are Inhibitors of Rivaroxaban and Apixaban Efflux by P-Glycoprotein
Victor Margelidon-Cozzolino, Sophie Hodin, Elodie Jacqueroux, Olivier Delézay, Laurent Bertoletti and Xavier Delavenne

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 519-525; DOI: https://doi.org/10.1124/jpet.117.245993
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In Vitro–In Vivo Extrapolation of OATP1B-Mediated Drug–Drug Interactions in Cynomolgus Monkey
Ayşe Ufuk, Rachel E. Kosa, Hongying Gao, Yi-An Bi, Sweta Modi, Dana Gates, A. David Rodrigues, Larry M. Tremaine, Manthena V. S. Varma, J. Brian Houston and Aleksandra Galetin

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 688-699; DOI: https://doi.org/10.1124/jpet.118.247767

Neuropharmacology

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Extending a Systems Model of the APP Pathway: Separation of β- and γ-Secretase Sequential Cleavage Steps of APP
Eline M. T. van Maanen, Tamara J. van Steeg, Maurice J. Ahsman, Maria S. Michener, Mary J. Savage, Matthew E. Kennedy, Huub Jan Kleijn, Julie Stone and Meindert Danhof

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 507-518; DOI: https://doi.org/10.1124/jpet.117.244699
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Preclinical to Human Translational Pharmacology of the Novel M₁ Positive Allosteric Modulator MK-7622
Jason M. Uslaner, Scott D. Kuduk, Marion Wittmann, Henry S. Lange, Steve V. Fox, Chris Min, Natasa Pajkovic, Dawn Harris, Caroline Cilissen, Chantal Mahon, Kate Mostoller, Steve Warrington and Douglas C. Beshore

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 556-566; DOI: https://doi.org/10.1124/jpet.117.245894
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3β-Methyl-Neurosteroid Analogs Are Preferential Positive Allosteric Modulators and Direct Activators of Extrasynaptic δ-Subunit γ-Aminobutyric Acid Type A Receptors in the Hippocampus Dentate Gyrus Subfield
Shu-Hui Chuang and Doodipala Samba Reddy

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 583-601; DOI: https://doi.org/10.1124/jpet.117.246660
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Pharmacological Characterization of H05, a Novel Serotonin and Noradrenaline Reuptake Inhibitor with Moderate 5-HT_2A Antagonist Activity for the Treatment of Depression
Xiangqing Xu, Yaqin Wei, Qiang Guo, Song Zhao, Zhiqiang Liu, Ting Xiao, Yani Liu, Yinli Qiu, Yuanyuan Hou, Guisen Zhang and KeWei Wang

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 624-635; DOI: https://doi.org/10.1124/jpet.118.248351
Open Access
The Nurr1 Ligand,1,1-bis(3′-Indolyl)-1-(p-Chlorophenyl)Methane, Modulates Glial Reactivity and Is Neuroprotective in MPTP-Induced Parkinsonism
Sean L. Hammond, Katriana A. Popichak, Xi Li, Lindsay G. Hunt, Evan H. Richman, Pranav U. Damale, Edwin K. P. Chong, Donald S. Backos, Stephen Safe and Ronald B. Tjalkens

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 636-651; DOI: https://doi.org/10.1124/jpet.117.246389

Toxicology

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Drug-Induced Alterations of Mitochondrial DNA Homeostasis in Steatotic and Nonsteatotic HepaRG Cells
Dounia Le Guillou, Simon Bucher, Karima Begriche, Delphine Hoët, Anne Lombès, Gilles Labbe and Bernard Fromenty

Journal of Pharmacology and Experimental Therapeutics June 2018, 365 (3) 711-726; DOI: https://doi.org/10.1124/jpet.117.246751

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Table of Contents

Cardiovascular

Cellular and Molecular

Chemotherapy, Antibiotics, and Gene Therapy

Drug Discovery and Translational Medicine

Endocrine and Diabetes

Gastrointestinal, Hepatic, Pulmonary, and Renal

Inflammation, Immunopharmacology, and Asthma

Metabolism, Transport, and Pharmacogenomics

Neuropharmacology

Toxicology

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