Editor's Choice

2017

August (5:4)

In vitro pharmacological characterization of a novel unbiased NOP receptor-selective nonpeptide agonist AT-403
Federica Ferrari, Davide Malfacini, Blair V. Journigan, Mark F. Bird, Claudio Trapella,Remo Guerrini, David G. Lambert, Girolamo Calo,& Nurulain T. Zaveri
This study identifies a small molecule AT-403 as a selective agonist at the Nociceptin receptor (NOP). Since AT-403 acts as an unbiased full agonist it should be a useful tool to probe the (patho)physiological role of NOP receptors.

KCTD12 modulation of GABA (B) receptor function
Melody Li, Carol J. Milligan, Haiyan Wang, Andrew Walker, Leonid Churilov,Andrew J. Lawrence, Christopher A. Reid, Seth C. Hopkins & Steven Petrou

KCTD12 is an auxiliary subunit of GABA-B receptors that may represent a site for functional modulation. This study provides novel in vivo evidence that the interaction between KCTD12 and GABA-B the receptor is of physiological significance, and may be a mechanism to more selectively modulate GABA-B receptor function for therapeutic purposes.

June (5:3)

Analgesic 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 & Mark G. Chambers

Chronic treatment of (R)-α-lipoic acid reduces blood glucose and lipid levels in high-fat diet and low-dose streptozotocin-induced metabolic syndrome and type 2 diabetes in Sprague-Dawley rats
Hardik Ghelani, Valentina Razmovski-Naumovski, & Srinivas Nammi

April (5:2)

GABAB receptor allosteric modulators exhibit pathway-dependent and species-selective activity
Emmanuel Sturchler, Xia Li, Maria de Lourdes Ladino, Kasia Kaczanowska, Michael Cameron, Patrick R. Griffin, M. G. Finn, Athina Markou & Patricia McDonald

Therapeutically targeting guanylate cyclase-C: computational modeling of plecanatide, a uroguanylin analog
Andrea Brancale, Kunwar Shailubhai, Salvatore Ferla, Antonio Ricci, Marcella Bassetto & Gary S Jacob

February (5:1)

Acute cocaine exposure elicits rises in calcium in arousal-related laterodorsal tegmental neurons
Mads Ødum Lambert, Theis Højland Ipsen & Kristi Anne Kohlmeier

Genome-wide DNA methylation profiling of CpG islands in a morpholino anthracycline derivative-resistant leukemia cell line: p38[alpha] as a novel candidate for resistance
Takeshi Asano, Hidehiko Narazaki, Atsushi Fujita

2016

December (4:6)

< a href="http://onlinelibrary.wiley.com/doi/10.1002/prp2.275/full">Preclinical findings predicting efficacy and side-effect profile of LY2940094, an antagonist of nociceptin receptors
Jeffrey M. Witkin, Linda M. Rorick‐Kehn, Mark J. Benvenga, Benjamin L. Adams, Scott D. Gleason, Karen M. Knitowski, Xia Li, Steven Chaney, Julie F. Falcone, Janice W. Smith, et al

Application of a systems pharmacology model for translational prediction of hERG-mediated QTc prolongation
Verena Gotta, Zhiyi Yu, Frank Cools, Karel van Ammel, David J. Gallacher, Sandra A. G. Visser, Frederick Sannajust, Pierre Morissette, Meindert Danhof, Piet H. van der Graaf

October (4:5)

RGS14 regulates the lifetime of G[alpha]-GTP signaling but does not prolong Gβ[gamma] signaling following receptor activation in live cells
Nicole E. Brown, Nevin A. Lambert, John R. Hepler

Use of a new proximity assay (NanoBRET) to investigate the ligand-binding characteristics of three fluorescent ligands to the human β1-adrenoceptor expressed in HEK-293 cells
Mark Soave, Leigh A. Stoddart, Alastair Brown, Jeanette Woolard, Stephen J. Hill

February (4:1)

Preclinical and translational evaluation of coagulation factor IXa as a novel therapeutic target
Wendy Ankrom, Harold B. Wood, Jiayi Xu, Wayne Geissler, Tom Bateman, Manash S. Chatterjee, Kung‐I Feng, Joseph M. Metzger, Walter R. Strapps, Marija Tadin‐Strapps, et al

Anti-inflammatory effects of the novel inhaled phosphodiesterase type 4 inhibitor CHF6001 on virus-inducible cytokines
Michael R. Edwards, Fabrizio Facchinetti, Maurizio Civelli, Gino Villetti, Sebastian L. Johnston

2015

December (3:6)

miRNA-27b levels are associated with CYP3A activity in vitro and in vivo
Lena Ekström, Ilona Skilving, Marie‐Louise Ovesjö, Eleni Aklillu, Hanna Nylén, Anders Rane, Ulf Diczfalusy, Linda Björkhem‐Bergman

Chronic P-glycoprotein inhibition increases the brain concentration of escitalopram: potential implications for treating depression
Fionn E. O'Brien, Gerard M. Moloney, Karen A. Scott, Richard M. O'Connor, Gerard Clarke, Timothy G. Dinan, Brendan T. Griffin, John F. Cryan

October (3:5)

β1 Adrenoceptor antagonistic effects of the supposedly selective β2 adrenoceptor antagonist ICI 118,551 on the positive inotropic effect of adrenaline in murine hearts
Simon Pecha, Frederik Flenner, Klaus‐Dieter Söhren, Kristina Lorenz, Thomas Eschenhagen, Torsten Christ

Modeling effects of dexamethasone on disease progression of bone mineral density in collagen-induced arthritic rats
Hoi‐Kei Lon, Debra C. DuBois, Justin C. Earp, Richard R. Almon, William J. Jusko

August (3:4)

Themed Section on Replication Studies in Pharmacology

Pharmacology and physiology of gastrointestinal enteroendocrine cells
O. J. Mace, B. Tehan, F. Marshall

Pharmacodynamic assays to facilitate preclinical and clinical development of pre-mRNA splicing modulatory drug candidates
Yihui Shi, Amanda S. Joyner, William Shadrick, Gustavo Palacios, Chandraiah Lagisetti, Philip M. Potter, Lidia C. Sambucetti, Stefan Stamm, Thomas R. Webb

June (3:3)

Simvastatin mitigates increases in risk factors for and the occurrence of cardiac disease following 10 Gy total body irradiation
Marek Lenarczyk, Jidong Su, Steven T. Haworth, Richard Komorowski, Brian L. Fish, Raymond Q. Migrino, Leanne Harmann, John W. Hopewell, Amy Kronenberg, Shailendra Patel, et al

March (3:2)

A neuroligin-1-derived peptide stimulates phosphorylation of the NMDA receptor NR1 subunit and rescues MK-801-induced decrease in long-term potentiation and memory impairment
Irina Korshunova, Michelle D. Gjørlund, Sylwia Owczarek, Anders V. Petersen, Jean‐François Perrier, Casper René Gøtzsche, Vladimir Berezin

Metformin protects primary rat hepatocytes against oxidative stress-induced apoptosis
Laura Conde de la Rosa, Titia E. Vrenken, Manon Buist‐Homan, Klaas Nico Faber, Han Moshage

February (3:1)

Functional desensitization of the β2 adrenoceptor is not dependent on agonist efficacy
Elizabeth M. Rosethorne, Michelle E. Bradley, Toby C. Kent, Steven J. Charlton

Oxytocin does not directly alter cardiac repolarization in rabbit or human cardiac myocytes
Yusheng Qu, Mei Fang, BaoXi Gao, Shanti Amagasu, William J. Crumb, Hugo M. Vargas