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Cited by 349

The DOI matches its Crossref record; 11 of the 11 references it cites were found in a registry or an index.

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

Open access
Soethoudt, Marjolein, Grether, Uwe, Fingerle, Jürgen, Grim, Travis W., Fezza, Filomena, de Petrocellis, Luciano, Ullmer, Christoph, Rothenhäusler, Benno, Perret, Camille, van Gils, Noortje, Finlay, David, MacDonald, Christa, Chicca, Andrea, Gens, Marianela Dalghi, Stuart, Jordyn, de Vries, Henk, Mastrangelo, Nicolina, Xia, Lizi, Alachouzos, Georgios, Baggelaar, Marc P., Martella, Andrea, Mock, Elliot D., Deng, Hui, Heitman, Laura H., Connor, Mark, Di Marzo, Vincenzo, Gertsch, Jürg, Lichtman, Aron H., Maccarrone, Mauro, Pacher, Pal, Glass, Michelle, van der Stelt, Mario·2017·Nature Communications
DOI 10.1038/ncomms13958
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Abstract

The cannabinoid CB 2 receptor (CB 2 R) represents a promising therapeutic target for various forms of tissue injury and inflammatory diseases. Although numerous compounds have been developed and widely used to target CB 2 R, their selectivity, molecular mode of action and pharmacokinetic properties have been poorly characterized. Here we report the most extensive characterization of the molecular pharmacology of the most widely used CB 2 R ligands to date. In a collaborative effort between multiple academic and industry laboratories, we identify marked differences in the ability of certain agonists to activate distinct signalling pathways and to cause off-target effects. We reach a consensus that HU910, HU308 and JWH133 are the recommended selective CB 2 R agonists to study the role of CB 2 R in biological and disease processes. We believe that our unique approach would be highly suitable for the characterization of other therapeutic targets in drug discovery research.

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Metadata

Authors
Soethoudt, M., Grether, U., Fingerle, J., Grim, T. W., Fezza, F., de Petrocellis, L., Ullmer, C., Rothenhäusler, B., Perret, C., van Gils, N., Finlay, D., MacDonald, C., Chicca, A., Gens, M. D., Stuart, J., de Vries, H., Mastrangelo, N., Xia, L., Alachouzos, G., Baggelaar, M. P., Martella, A., Mock, E. D., Deng, H., Heitman, L. H., Connor, M., Di Marzo, V., Gertsch, J., Lichtman, A. H., Maccarrone, M., Pacher, P., Glass, M., & van der Stelt, M.
Venue
Nature Communications
Publisher
Springer Science and Business Media LLC
Published
2017-01-03
Volume
8
Issue
1
Pages
13958-13958
ISSN
2041-1723 (ISSN-L)
DOI
10.1038/ncomms13958
OpenAlex
W2566514911
Cited by
349
References
11
FWCI
23.71
Type
journal article
Language
en
Open access
gold

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CoChat. (2026). Citation check: Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity. https://app.cochat.ai/papers/10.1038/ncomms13958
The paper
Soethoudt, M., Grether, U., Fingerle, J., Grim, T. W., Fezza, F., de Petrocellis, L., Ullmer, C., Rothenhäusler, B., Perret, C., van Gils, N., Finlay, D., MacDonald, C., Chicca, A., Gens, M. D., Stuart, J., de Vries, H., Mastrangelo, N., Xia, L., Alachouzos, G., . . . van der Stelt, M. (2017). Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity. Nature Communications. https://doi.org/10.1038/ncomms13958

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.