Nature Communications (Jan 2017)
Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity
- Marjolein Soethoudt,
- Uwe Grether,
- Jürgen Fingerle,
- Travis W. Grim,
- Filomena Fezza,
- Luciano de Petrocellis,
- Christoph Ullmer,
- Benno Rothenhäusler,
- Camille Perret,
- Noortje van Gils,
- David Finlay,
- Christa MacDonald,
- Andrea Chicca,
- Marianela Dalghi Gens,
- Jordyn Stuart,
- Henk de Vries,
- Nicolina Mastrangelo,
- Lizi Xia,
- Georgios Alachouzos,
- Marc P. Baggelaar,
- Andrea Martella,
- Elliot D. Mock,
- Hui Deng,
- Laura H. Heitman,
- Mark Connor,
- Vincenzo Di Marzo,
- Jürg Gertsch,
- Aron H. Lichtman,
- Mauro Maccarrone,
- Pal Pacher,
- Michelle Glass,
- Mario van der Stelt
Affiliations
- Marjolein Soethoudt
- Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University
- Uwe Grether
- Roche Innovation Center Basel, F. Hoffman-La Roche Ltd.
- Jürgen Fingerle
- Department of Biochemistry, NMI, University Tübingen
- Travis W. Grim
- Department of Pharmacology and Toxicology
- Filomena Fezza
- Department of Experimental Medicine and Surgery, Tor Vergata University of Rome
- Luciano de Petrocellis
- Endocannabinoid Research Group, Institute of Biomolecular Chemistry, C.N.R.
- Christoph Ullmer
- Roche Innovation Center Basel, F. Hoffman-La Roche Ltd.
- Benno Rothenhäusler
- Roche Innovation Center Basel, F. Hoffman-La Roche Ltd.
- Camille Perret
- Roche Innovation Center Basel, F. Hoffman-La Roche Ltd.
- Noortje van Gils
- Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University
- David Finlay
- Department of Pharmacology and Clinical Pharmacology, Faculty of Medical and Health Sciences, University of Auckland
- Christa MacDonald
- Department of Pharmacology and Clinical Pharmacology, Faculty of Medical and Health Sciences, University of Auckland
- Andrea Chicca
- Institute of Biochemistry and Molecular Medicine, University of Bern
- Marianela Dalghi Gens
- Institute of Biochemistry and Molecular Medicine, University of Bern
- Jordyn Stuart
- Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Macquarie University, North Ryde
- Henk de Vries
- Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University
- Nicolina Mastrangelo
- Department of Medicine, Campus Bio-Medico University of Rome
- Lizi Xia
- Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University
- Georgios Alachouzos
- Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University
- Marc P. Baggelaar
- Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University
- Andrea Martella
- Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University
- Elliot D. Mock
- Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University
- Hui Deng
- Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University
- Laura H. Heitman
- Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University
- Mark Connor
- Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Macquarie University, North Ryde
- Vincenzo Di Marzo
- Endocannabinoid Research Group, Institute of Biomolecular Chemistry, C.N.R.
- Jürg Gertsch
- Institute of Biochemistry and Molecular Medicine, University of Bern
- Aron H. Lichtman
- Department of Pharmacology and Toxicology
- Mauro Maccarrone
- European Center for Brain Research/IRCCS Santa Lucia Foundation
- Pal Pacher
- Laboratory of Cardiovascular Physiology and Tissue Injury, National Institute of Health/NIAAA
- Michelle Glass
- Department of Pharmacology and Clinical Pharmacology, Faculty of Medical and Health Sciences, University of Auckland
- Mario van der Stelt
- Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University
- DOI
- https://doi.org/10.1038/ncomms13958
- Journal volume & issue
-
Vol. 8,
no. 1
pp. 1 – 14
Abstract
CB2 receptor agonists are developed as potential analgesics or immune-modulatory compounds. Here, the authors characterize the pharmacological properties of widely used CB2 receptor agonists and antagonists, recommending three that appear most suitable for in vitro and in vivostudies.
