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Pharmacology Research & Perspectives

Articles are published under the terms of the Creative Commons License as stated in the final article.

Cover image for Vol. 5 Issue 1

Editors: Darrell R. Abernethy & Andrew J. Lawrence

Online ISSN: 2052-1707

Associated Title(s): British Journal of Clinical Pharmacology, British Journal of Pharmacology

Translational Pharmacology Broadly Defined

This virtual issue of Pharmacology Research & Perspectives is a nice representation of the breadth of outstanding contributions in the area of translational pharmacology that we receive and publish. Studies evaluating potential therapeutic targets including coagulation factor IXa, mitochondrial fission, intestinal immune response and serotonin receptors for obesity demonstrate the broad range of pharmacology we publish. Mechanisms of drug toxicity and their representation as clinical adverse drug effects are the counterpart of drug efficacy, and also areas that are represented. Finally, an important component of clinical translational pharmacology is the determination of drug exposure and optimal drug dose via reporting of pharmacokinetic, pharmacodynamic, and drug interaction studies. The articles in this virtual issue of Pharmacology Research & Perspectives should be of considerable interest to the translational pharmacologist, we believe you will find them of interest and value.

Darrell R. Abernethy, MD, PhD

Andrew Lawrence, PhD
Deputy Editor-in-Chief

Role of endoplasmic reticulum stress in drug-induced toxicity
Fabienne Foufelle and Bernard Fromenty

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, Dietmar Seiffert and Patrick Andre

Mechanisms of the gabapentinoids and α2δ-1 calcium channel subunit in neuropathic pain
Ryan Patel and Anthony H. Dickenson

Mitochondrial fission – a drug target for cytoprotection or cytodestruction?
Ayeshah A. Rosdah, Jessica K. Holien, Lea M. D. Delbridge, Gregory J. Dusting and Shiang Y. Lim

Preclinical pharmacology and pharmacokinetics of CERC-301, a GluN2B-selective N-methyl-D-aspartate receptor antagonist
Rachel Garner, Shobha Gopalakrishnan, John A. McCauley, Rodney A. Bednar, Stanley L. Gaul, Scott D. Mosser, Laszlo Kiss, Joseph J. Lynch, Shil Patel, Christine Fandozzi, Armando Lagrutta, Richard Briscoe, Nigel J. Liverton, Blake M. Paterson, James J. Vornov and Reza Mazhari

In vitro and in vivo drug disposition of cilengitide in animals and human
Hugues Dolgos, Achim Freisleben, Elmar Wimmer, Holger Scheible, Friedrich Krätzer, Tetsuo Yamagata, Dieter Gallemann and Markus Fluck

Effect of CYP3A perpetrators on ibrutinib exposure in healthy participants
Jan de Jong, Donna Skee, Joe Murphy, Juthamas Sukbuntherng, Peter Hellemans, Johan Smit, Ronald de Vries, Juhui James Jiao, Jan Snoeys and Erik Mannaert

Natural compound methyl protodioscin protects against intestinal inflammation through modulation of intestinal immune responses
Rongli Zhang, Shila Gilbert, Xinsheng Yao, Jefferson Vallance, Kris Steinbrecher, Richard Moriggl, Dongsheng Zhang, Madhu Eluri, Haifeng Chen, Huiqing Cao, Noah Shroyer, Lee Denson and Xiaonan Han

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 and Linda Björkhem-Bergman

Characterization of the 5-HT2C receptor agonist lorcaserin on efficacy and safety measures in a rat model of diet-induced obesity
Guy A. Higgins, Jill Desnoyer, Annalise Van Niekerk, Leo B. Silenieks, Winnie Lau, Sandy Thevarkunnel, Julia Izhakova, Ines A.M. DeLannoy, Paul J. Fletcher, Josepha DeLay and Howard Dobson

Randomized pharmacokinetic and drug–drug interaction studies of ceftazidime, avibactam, and metronidazole in healthy subjects
Shampa Das, Jianguo Li, Jon Armstrong, Maria Learoyd and Timi Edeki

Prediction of clinical pharmacokinetics of AMG 181, a human anti-α4β7 monoclonal antibody for treating inflammatory bowel diseases
Hong Li, Kathleen Köck, John A. Wisler, William A. Rees, Peter J. Prince, Kai O. Reynhardt, Hailing Hsu, Zhigang Yu, Dominic C. Borie, David H. Salinger and Wei-Jian Pan

The discovery of a selective and potent A2a agonist with extended lung retention
Annika B. M. Åstrand, Eva Lamm Bergström, Hui Zhang, Lena Börjesson, Therese Söderdahl, Cecilia Wingren, Anne-Helene Jansson, Amir Smailagic, Camilla Johansson, Håkan Bladh, Igor Shamovsky, Anders Tunek and Tomas Drmota

Modeling the pharmacokinetic-pharmacodynamic relationship of the monoclonal anti-macaque-IL-15 antibody Hu714MuXHu in cynomolgus monkeys
Wei. J. Pan, Hong Li, Jim J. Xiao, Michelle J. Horner, Herve N. Lebrec, Eric A. Butz, Arunan Kaliyaperumal, Tsui C. Cheah, Robert C. Ortiz, Samantha P. Prokop, Sabina A. Buntich, Babette M. Boren, Suzanne T. Wolford, Wayne H. Tsuji, Larry C. Wienkers and Kathleen Köck

Antiallodynic effects of alpha lipoic acid in an optimized RR-EAE mouse model of MS-neuropathic pain are accompanied by attenuation of upregulated BDNF-TrkB-ERK signaling in the dorsal horn of the spinal cord
Nemat Khan, Richard Gordon, Trent M. Woodruff and Maree T. Smith

Studies of human pancreatic elastase treatment of rabbit and human vein rings to predict human therapeutic doses
Steven K. Burke, David Bunton, Karen Bingham, Emma Moss, Kimberly S. Bland, Barry Starcher, Marco D. Wong and F. Nicholas Franano

Characterization of a novel brain barrier ex vivo insect-based P-glycoprotein screening model
Olga Andersson, Liesbeth Badisco, Ane Håkansson Hansen, Steen Honoré Hansen, Karin Hellman, Peter Aadal Nielsen, Line Rørbæk Olsen, Rik Verdonck, N. Joan Abbott, Jozef Vanden Broeck and Gunnar Andersson

Applicability of second-generation upcyte® human hepatocytes for use in CYP inhibition and induction studies
Sarada D. Ramachandran, Aurélie Vivarès, Sylvie Klieber, Nicola J. Hewitt, Bernhard Muenst, Stefan Heinz, Heike Walles and Joris Braspenning