In This Section

This virtual issue comprises a representative selection of outstanding peer-reviewed original research and topical reviews in the area of pain pharmacology that have recently published in Pharmacology Research & Perspectives (PR&P) as well as the other ASPET journals including Pharmacological Reviews, Drug Metabolism and Disposition, Journal of Pharmacology and Experimental Therapeutics, and Molecular Pharmacology. The innovative research in this virtual issue highlights a diverse array of nociceptive mechanisms, models, and novel interventional strategies that are particularly timely in light of the safety and societal issues associated with opioid dependence and abuse. In addition to new pharmacological insights for well-established analgesic mechanisms (e.g., NSAIDS and opioid receptor subtypes), there are many articles on state-of-the-art experimental methodologies and findings for promising drug targets including cannabinoids, gabapentinoids, voltage-gated and ligand-gated ion channels, and associated down-stream signaling mechanisms that underlie the neuronal and immunological pathophysiology of chronic nociception. The articles contained in this joint virtual issue should be of considerable interest to both experienced and early career pain investigators. We encourage potential authors to review these excellent papers as they consider venues for communicating their pharmacology research on pain mechanisms and treatments.

Andrew J. Lawrence

Michael F. Jarvis
Deputy Editor

Table of Contents

Pharmacological Reviews | Drug Metabolism and Disposition | Journal of Pharmacology and Experimental Therapeutics | Molecular Pharmacology | Pharmacology Research & Perspectives

All of these articles are freely accessible; some are open access.

Pharmacological Reviews

Pharmacological Reviews

Molecular Pharmacology of δ-Opioid Receptors
Louis Gendron, Catherine Cahill, Peter W Schiller, Mark von Zastrow, and Graciela Pineyro
Pharmacological Reviews 2016, 68 (3) 631-700 DOI:

Nociceptin/Orphanin FQ Receptor Structure, Signaling, Ligands, Functions, and Interactions with Opioid Systems
Lawrence Toll, Michael R Bruchas, Girolamo Calo, Brian M Cox, and Nurulain T Zaveri
Pharmacological Reviews 2016, 68 (2) 419-457 DOI:

Open AccessEtiology and Pharmacology of Neuropathic Pain
Sascha R. A. Alles and Peter A Smith
Pharmacological Reviews 2017, 70 (2) 351-347 DOI:

Drug Metabolism and Disposition

Drug Metabolism and Disposition

Stereoselective Pharmacokinetics and Chiral Inversion of Ibuprofen in Adjuvant-induced Arthritic Rats
Hiroyuki Ikuta, Atsushi Kawase, and Masahiro Iwaki
Drug Metabolism and Disposition 2017, 45 (3) 316-324 DOI:

Modeling Sex Differences in Pharmacokinetics, Pharmacodynamics, and Disease Progression Effects of Naproxen in Rats with Collagen-Induced Arthritis
Xiaonan Li, Debra C DuBois, Richard R Almon, and William J Jusko
Drug Metabolism and Disposition 2017, 45 (5) 484-491 DOI:

Modeling Combined Immunosuppressive and Anti-inflammatory Effects of Dexamethasone and Naproxen in Rats Predicts the Steroid-Sparing Potential of Naproxen
Xiaonan Li, Debra C DuBois, Dawei Song, Richard R Almon, William J Jusko, and Xijing Chen
Drug Metabolism and Disposition 2017, 45 (7) 834-845 DOI:

Effect of Probiotics on Pharmacokinetics of Orally Administered Acetaminophen in Mice
Jeon-Kyung Kim, Min Sun Choi, Jin-Ju Jeong, Su-Min Lim, In Sook Kim, Hye Hyun Yoo, and Dong-Hyun Kim
Drug Metabolism and Disposition 2016, 46 (2) 122-130 DOI:


Journal of Pharmacology and Experimental Therapeutics

Behavioral Characterization of κ Opioid Receptor Agonist Spiradoline and Cannabinoid Receptor Agonist CP55940 Mixtures in Rats
Vanessa Minervini, Sujata S Dahal, and Charles France
Journal of Pharmacology and Experimental Therapeutics 2017, 360 (2) 280-287 DOI:

Two Janus Cannabinoids That Are Both CB2 Agonists and CB1 Antagonists
Amey Dhopeshwarkar, Natalia Murataeva, Alex Makriyannis, Alex Straiker, and Ken P. Mackie
Journal of Pharmacology and Experimental Therapeutics 2017, 360 (2) 300-311 DOI:

Thermolytic Degradation of Synthetic Cannabinoids: Chemical Exposures and Pharmacological Consequences
Brian F Thomas, Timothy W Lefever, Ricardo A Cortes, Alexander L Kovach, Anderson O Cox, Purvi R Patel, Gerald T Pollard, Julie A Marusich, Richard A Kevin, Thomas F Gamage, and Jenny L. Wiley
Journal of Pharmacology and Experimental Therapeutics 2017, 361 (1) 162-171 DOI:

Preference for an Opioid/Benzodiazepine Mixture over an Opioid Alone Using a Concurrent Choice Procedure in Rhesus Monkey
Peter F. Weed, Charles P. France, and Lisa R Gerak
Journal of Pharmacology and Experimental Therapeutics 2017, 362 (1) 59-66 DOI:

Apparent Affinity Estimates and Reversal of the Effects of Synthetic Cannabinoids AM-2201, CP-47,497, JWH-122, and JWH-250 by Rimonabant in Rhesus Monkeys
Lenka Hruba and Lance R McMahon
Journal of Pharmacology and Experimental Therapeutics 2017, 362 (2) 278-286 DOI:

Relief of Pain-Depressed Behavior in Rats by Activation of D1-like Dopamine Receptors
Matthew F Lazenka, Kelen C Freitas, Sydney Henck, and S. Stevens Negus
Journal of Pharmacology and Experimental Therapeutics 2017, 362 (1) 14-23 DOI:

The Cannabinoid CB2 agonist GW405833 Suppresses Inflammatory and Neuropathic Pain through a CB1 Mechanism that Is Independent of CB2 Receptors in Mice
Ai-Ling Li, Lawrence M Carey, Ken Mackie, and Andrea G Hohmann
Journal of Pharmacology and Experimental Therapeutics 2017, 362 (2) 296-305 DOI:

NKTR-181: A Novel Mu-Opioid Analgesic with Inherently Low Abuse Potential
Takahiro Miyazaki, Irene Y. Choi, Werner Rubas, Neel K. Anand, Cherie Ali, Juli Evans, Hema Gursahani, Marlene Hennessy, Grace Kim, Daniel McWeeney, Juergen Pfeiffer, Phi Quach, David Gauvin, Timothy A. Riley, Jennifer A. Riggs, Kathleen Gogas, Jonathan Zalevsky, and Stephen K. Doberstein
Journal of Pharmacology and Experimental Therapeutics 2017, 363 (1) 104-113 DOI:

Molecular Pharmacology

Molecular Pharmacology

Voltage-Gated R-Type Calcium Channel Inhibition via Human μ-, δ-, and κ-opioid Receptors Is Voltage-Independently Mediated by Gβγ Protein Subunits
Geza Berecki, Leonid Motin, and David J Adams
Molecular Pharmacology 2016, 89 (1) 187-196 DOI:

Structure-Driven Pharmacology of Transient Receptor Potential Channel Vanilloid 1Structure-Driven Pharmacology of Transient Receptor Potential Channel Vanilloid 1
Ignacio Diaz-Franulic, Javier Caceres-Molina, Romina V Sepulveda, Fernando Gonzalez-Nilo, and Ramon Latorre
Molecular Pharmacology 2016, 90 (3) 300-308 DOI:

Dissecting the Signaling Pathways Involved in the Crosstalk between Metabotropic Glutamate 5 and Cannabinoid Type 1 Receptors
Isabella G Olmo, Talita H Ferreira-Vieira, and Fabiola M Ribeiro
Molecular Pharmacology 2016, 90 (5) 609-619 DOI:

Epigenetic Activation of μ-Opioid Receptor Gene via Increased Expression and Function of Mitogen- and Stress-Activated Protein Kinase 1
Yadav Wagley, Ping-Yee Law, Li-Na Wei, and Horace H. Loh
Molecular Pharmacology 2017, 91 (4) 357-372 DOI:

Sequence-Specific Regulation of Endocytic Lifetimes Modulates Arrestin-Mediated Signaling at the µ Opioid Receptor
Zara Y Weinberg, Amanda S Zajac, Tiffany Phan, Daniel J Shiwarski, and Manojkumar A Puthenveedu
Molecular Pharmacology 2017, 91 (4) 416-427 DOI:

p38β Mitogen-Activated Protein Kinase Signaling Mediates Exenatide-Stimulated Microglial β-Endorphin Expression
Hai-Yun Wu, Xiao-Fang Mao, Hui Fan, and Yong-Xiang Wang
Molecular Pharmacology 2017, 91 (5) 451-463 DOI:

Agonist-Dependent and -Independent κ Opioid Receptor Phosphorylation: Distinct Phosphorylation Patterns and Different Cellular Outcomes
Yi-Ting Chiu, Chongguang Chen, Daohai Yu, Stefan Schulz, and Lee-Yuan Liu-Chen
Molecular Pharmacology 2017, 92 (5) 588-600 DOI:

Desensitization and Tolerance of Mu Opioid Receptors on Pontine Kölliker-Fuse Neurons
Erica S. Levitt and John T. Williams
Molecular Pharmacology 2018, 93 (1) 8-13 DOI:

ABIN-1 Negatively Regulates μ-Opioid Receptor Function
Peilan Zhou, Jiebing Jiang, Hui Yan, Yulei Li, Junru Zhao, Xiao Wang, Ruibin Su, and Zehui Gong
Molecular Pharmacology 2018, 93 (2) 36-48 DOI:

Slowly Signaling G Protein–Biased CB2 Cannabinoid Receptor Agonist LY2828360 Suppresses Neuropathic Pain with Sustained Efficacy and Attenuates Morphine Tolerance and Dependence
Xiaoyan Lin, Amey S. Dhopeshwarkar, Megan Huibregtse, Ken Mackie, and Andrea G. Hohmann
Molecular Pharmacology 2018, 93 (2) 49-62 DOI:

Pharmacological Evidence for a Putative Conserved Allosteric Site on Opioid Receptors
Kathryn E Livingston, M Alexander Stanczyk, Neil Burford, Andrew Alt, Merixtell Canals, and John R. Traynor
Molecular Pharmacology 2018, 93 (2) 157-167 DOI:

Molecular Imaging of GLUT1 and GLUT5 in Breast Cancer: A Multitracer Positron Emission Tomography Imaging Study in Mice
Melinda Wuest, Ingrit Hamann, Vincent Bouvet, Darryl Glubrecht, Alison Marshall, Brendan Trayner, Olivier Soueidan, Daniel Krys, Michael Wagner, Chris Cheeseman, Frederick West, and Frank Wuest
Molecular Pharmacology 2018, 93 (2) 79-89 DOI:

N-Acyl Amino Acids (Elmiric Acids): Endogenous Signaling Molecules with Therapeutic Potential
Sumner Burstein
Molecular Pharmacology 2018, 93 (3) 228-238 DOI:

G Protein Preassembly Rescues Efficacy of W6.48 Toggle Mutations in Neuropeptide Y2 Receptor
Anette Kaiser, Caroline Hempel, Lizzy Wanka, Mario Schubert, Heidi E. Hamm, and Annette G. Beck-Sickinger
Molecular Pharmacology 2018, 93 (4) 387-401 DOI:

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Pharmacology Research & Perspectives

Open AccessMechanisms of the gabapentinoids and α2δ‐1 calcium channel subunit in neuropathic pain
Ryan Patel and Anthony H. Dickenson
Pharmacology Research & Perspectives 2016, 4 (2) DOI:

Open AccessPharmacological characterization of cebranopadol a novel analgesic acting as mixed nociceptin/orphanin FQ and opioid receptor agonist
Anna Rizzi, Maria Camilla Cerlesi, Chiara Ruzza, Davide Malfacini, Federica Ferrari, Sara Bianco, Tommaso Costa, Remo Guerrini, Claudio Trapella, and Girolamo Calo
Pharmacology Research & Perspectives2016 44DOI:

Open AccessSlow drug delivery decreased total body clearance and altered bioavailability of immediate- and controlled- release oxycodone formulations
Yan Li, Duxin Sun, Maria Palmisano, and Simon Zhou
Pharmacology Research & Perspectives 2016, 4 (1) DOI:

Open AccessThe anti-inflammatory compound palmitoylethanolamide inhibits prostaglandin and hydroxyeicosatetraenoic acid production by a macrophage cell line
Linda Gabrielsson, Sandra Gouveia‐Figueira, Jenny Häggström, Mireille Alhouayek, and Christopher J. Fowler
Pharmacology Research & Perspectives 2017, 5 (2) DOI:

Open AccessDiclofenac, a nonsteroidal anti-inflammatory drug, is an antagonist of human TRPM3 isoforms
Hiroka Suzuki, Eiji Sasaki, Ayumi Nakagawa, Yukiko Muraki, Noriyuki Hatano, and Katsuhiko Muraki
Pharmacology Research & Perspectives 2016, 4 (3) DOI:

Open AccessFibromyalgia syndrome: metabolic and autophagic processes in intermittent cold stress mice
Lisa Oezel, Hanna Then, Anna L. Jung, Samir Jabari, Gabriel A. Bonaterra, Thaddeus T. Wissniowski, Susanne F. Önel, Matthias Ocker, Kati Thieme, Ralf Kinscherf, and Pietro Di Fazio
Pharmacology Research & Perspectives 2016, 4 (5) DOI:

Open AccessPharmacological comparison of a nonhuman primate and a rat model of oxaliplatin-induced neuropathic cold hypersensitivity
Yuka Shidahara, Shinya Ogawa, Mari Nakamura, Shingo Nemoto, Yuji Awaga, Miyuki Takashima, Aldric Hama, Akihisa Matsuda, and Hiroyuki Takamatsu
Pharmacology Research & Perspectives 2016, 4 (1) DOI:

Open AccessPDE4 inhibitor rolipram inhibits the expression of microsomal prostaglandin E synthase-1 by a mechanism dependent on MAP kinase phosphatase-1
Lauri Tuure, Mari Hämäläinen, and Eeva Moilanen
Pharmacology Research & Perspectives 2017, 5 (6) DOI:

Open AccessNerve growth factor inhibitor with novel-binding domain demonstrates nanomolar efficacy in both cell-based and cell-free assay systems
Allison E. Kennedy, Corey A. Laamanen, Mitchell S. Ross, Rahul Vohra, Douglas R. Boreham, John A. Scott, and Gregory M. Ross
Pharmacology Research & Perspectives 2017, 5 (5) DOI:

Open AccessEthics of animal research in human disease remediation, its institutional teaching; and alternatives to animal experimentation
Rajkumar Cheluvappa, Paul Scowen, and Rajaraman Eri
Pharmacology Research & Perspectives 2017 5 (4) DOI:

Open AccessAnalgesic and anti-inflammatory properties of novel, selective, and potent EP4 receptor antagonists
Srinivasan Chandrasekhar, Xiao‐Peng Yu, Anita K. Harvey, Jennifer L. Oskins, Chaohua Lin, Xushan Wang, Maria‐Jesus Blanco, Matthew J. Fisher, Steven L. Kuklish, Matthew A. Schiffler, Tatiana Vetman, Alan M. Warshawsky, Jeremy S. York, Alison M. Bendele, and Mark G. Chambers
Pharmacology Research & Perspectives 2017 5 (3) DOI:

Open AccessAdverse reactions to fluoroquinolones in the Nigerian population: an audit of reports submitted to the National Pharmacovigilance Centre from 2004 to 2016
Ibrahim A. Oreagba, Kazeem A. Oshikoya, Comfort Ogar, Abiodun O. Adefurin, Ali Ibrahim, Olufunsho Awodele, and Yetunde Oni
Pharmacology Research & Perspectives 2017, 5 (2) DOI:

Open AccessGastrointestinal safety, chemotherapeutic potential, and classic pharmacological profile of NOSH-naproxen (AVT-219) a dual NO- and H2S-releasing hybrid
Mitali Chattopadhyay, Ravinder Kodela, Pascale L. Duvalsaint, and Khosrow Kashfi
Pharmacology Research & Perspectives 2016, 4 (2) DOI:

Open AccessTaurolidine and congeners activate hTRPA1 but not hTRPV1 channels and stimulate CGRP release from mouse tracheal sensory nerves
Tatjana I. Kichko, Rolf W. Pfirrmann, and Peter W. Reeh
Pharmacology Research & Perspectives 2016 4 (1) DOI:


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