Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity.

• Soethoudt M Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.
• Grether U Roche Innovation Center Basel, F. Hoffman-La Roche Ltd., Grenzachterstrasse 124, Basel 4070, Switzerland.
• Fingerle J Department of Biochemistry, NMI, University Tübingen, Markwiesenstrasse 55, Reutlingen 72770, Germany.
• Grim TW Department of Pharmacology and Toxicology, 1220 East Broad Street, PO Box 980613, Richmond, Virginia 23298-0613, USA.
• Fezza F Department of Experimental Medicine and Surgery, Tor Vergata University of Rome, Via Montpellier 1, Rome 00133, Italy.
• de Petrocellis L Endocannabinoid Research Group, Institute of Biomolecular Chemistry, C.N.R., Via Campi Flegrei 34, Comprensorio Olivetti, Pozzuoli 80078, Italy.
• Ullmer C Roche Innovation Center Basel, F. Hoffman-La Roche Ltd., Grenzachterstrasse 124, Basel 4070, Switzerland.
• Rothenhäusler B Roche Innovation Center Basel, F. Hoffman-La Roche Ltd., Grenzachterstrasse 124, Basel 4070, Switzerland.
• Perret C Roche Innovation Center Basel, F. Hoffman-La Roche Ltd., Grenzachterstrasse 124, Basel 4070, Switzerland.
• van Gils N Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.
• Finlay D Department of Pharmacology and Clinical Pharmacology, Faculty of Medical and Health Sciences, University of Auckland, 85 Park road, Grafton, Auckland 1023, New Zealand.
• MacDonald C Department of Pharmacology and Clinical Pharmacology, Faculty of Medical and Health Sciences, University of Auckland, 85 Park road, Grafton, Auckland 1023, New Zealand.
• Chicca A Institute of Biochemistry and Molecular Medicine, University of Bern, Bühlstrasse 28, Bern CH-3012, Switzerland.
• Gens MD Institute of Biochemistry and Molecular Medicine, University of Bern, Bühlstrasse 28, Bern CH-3012, Switzerland.
• Stuart J Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Macquarie University, North Ryde, New South Wales 2109, Australia.
• de Vries H Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.
• Mastrangelo N Department of Medicine, Campus Bio-Medico University of Rome, Via Alvaro del Portillo 21, Rome 00128, Italy.
• Xia L Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.
• Alachouzos G Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.
• Baggelaar MP Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.
• Martella A Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.
• Mock ED Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.
• Deng H Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.
• Heitman LH Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.
• Connor M Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Macquarie University, North Ryde, New South Wales 2109, Australia.
• Di Marzo V Endocannabinoid Research Group, Institute of Biomolecular Chemistry, C.N.R., Via Campi Flegrei 34, Comprensorio Olivetti, Pozzuoli 80078, Italy.
• Gertsch J Institute of Biochemistry and Molecular Medicine, University of Bern, Bühlstrasse 28, Bern CH-3012, Switzerland.
• Lichtman AH Department of Pharmacology and Toxicology, 1220 East Broad Street, PO Box 980613, Richmond, Virginia 23298-0613, USA.
• Maccarrone M European Center for Brain Research/IRCCS Santa Lucia Foundation, via del Fosso del Fiorano 65, Rome 00143, Italy.
• Pacher P Laboratory of Cardiovascular Physiology and Tissue Injury, National Institute of Health/NIAAA, 5625 Fishers Lane, Rockville, Maryland 20852, USA.
• Glass M Department of Pharmacology and Clinical Pharmacology, Faculty of Medical and Health Sciences, University of Auckland, 85 Park road, Grafton, Auckland 1023, New Zealand.
• van der Stelt M Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.

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Animals

Bridged Bicyclo Compounds

CHO Cells

Cannabinoid Receptor Agonists

Cannabinoids

Cell Line, Tumor

Cricetulus

Gene Expression

HEK293 Cells

High-Throughput Screening Assays

Humans

Keratinocytes

Kinetics

Ligands

Macrophages

Mice

Neurons

Protein Binding

Receptor, Cannabinoid, CB1

Receptor, Cannabinoid, CB2

Signal Transduction