The DOI matches its Crossref record.
Pharmacology of Cannabinoid Receptor Ligands
Abstract
Mammalian tissues contain at least two types of cannabinoid receptor, CB 1 and CB 2 , both coupled to G proteins. CB 1 receptors are expressed mainly by neurones of the central and peripheral nervous system whereas CB 2 receptors occur in certain non-neuronal tissues, particularly in immune cells. The existence of endogenous ligands for cannabinoid receptors has also been demonstrated. The discovery of this 'endogenous cannabinoid system' has been paralleled by a renewed interest in possible therapeutic applications of cannabinoids, for example in the management of pain and in the suppression of muscle spasticity/spasm associated with multiple sclerosis or spinal cord injury. It has also prompted the development of a range of novel cannabinoid receptor ligands, including several that show marked selectivity for CB 1 or CB 2 receptors. This review summarizes current knowledge about the in vitro pharmacological properties of important CB 1 and CB 2 receptor ligands. Particular attention is paid to the binding properties of these ligands, to the efficacies of cannabinoid receptor agonists, as determined using cyclic AMP or [35 S]GTPγS binding assays, and to selected examples of how these pharmacological properties can be influenced by chemical structure. The in vitro pharmacological properties of ligands that can potently and selectively oppose the actions of CB 1 or CB 2 receptor agonists are also described. When administered by themselves, some of these ligands produce effects in certain tissue preparations that are opposite in direction to those produced by cannabinoid receptor agonists and the possibility that the ligands producing such 'inverse cannabimimetic effects' are inverse agonists rather than pure antagonists is discussed.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cited by
International Union of Pharmacology. XXVII. Classification of Cannabinoid Receptors
Howlett, A. C., Barth, F., Bonner, T. I., Cabral, G., Casellas, P., Devane, W. A., Felder, C. C., Herkenham, M., Mackie, K., Martin, B. R., et al. (2002) · Pharmacological Reviews · doi:10.1124/pr.54.2.161 · Cited by 2,819
Self-citationD'Souza, D. C., Perry, E., MacDougall, L., Ammerman, Y., Cooper, T., Wu, Y.-T., Braley, G., Gueorguieva, R., & Krystal, J. H. (2004) · Neuropsychopharmacology · doi:10.1038/sj.npp.1300496 · Cited by 1,024
Cannabinoid receptors and pain
Pertwee, R. G. (2001) · Progress in Neurobiology · doi:10.1016/s0301-0082(00)00031-9 · Cited by 741
Self-citationCannabinoid physiology and pharmacology: 30 years of progress
Howlett, A. C., Breivogel, C. S., Childers, S. R., Deadwyler, S. A., Hampson, R. E., & Porrino, L. J. (2004) · Neuropharmacology · doi:10.1016/j.neuropharm.2004.07.030 · Cited by 608
Mitochondrial CB1 receptors regulate neuronal energy metabolism
Bénard, G., Massa, F., Puente, N., Lourenço, J., Bellocchio, L., Soria-Gómez, E., Matias, I., Delamarre, A., Metna-Laurent, M., Cannich, A., et al. (2012) · Nature Neuroscience · doi:10.1038/nn.3053 · Cited by 588
Emerging strategies for exploiting cannabinoid receptor agonists as medicines
Pertwee, R. G. (2009) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2008.00048.x · Cited by 436
Self-citationEarly phytocannabinoid chemistry to endocannabinoids and beyond
Mechoulam, R., Hanuš, L. O., Pertwee, R., & Howlett, A. C. (2014) · Nature Reviews Neuroscience · doi:10.1038/nrn3811 · Cited by 393
Self-citationCB1 and CB2 cannabinoid receptors are implicated in inflammatory pain
Clayton, N., Marshall, F. H., Bountra, C., & O'Shaughnessy, C. T. (2002) · Pain · doi:10.1016/s0304-3959(01)00454-7 · Cited by 247
Ross, R. A., Gibson, T. M., Brockie, H. C., Leslie, M., Pashmi, G., Craib, S. J., Di Marzo, V., & Pertwee, R. G. (2001) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0703850 · Cited by 237
Goods and Bads of the Endocannabinoid System as a Therapeutic Target: Lessons Learned after 30 Years
Maccarrone, M., Di Marzo, V., Gertsch, J., Grether, U., Howlett, A. C., Hua, T., Makriyannis, A., Piomelli, D., Ueda, N., & van der Stelt, M. (2023) · Pharmacological Reviews · doi:10.1124/pharmrev.122.000600 · Cited by 183
Bidirectional cannabinoid modulation of social behavior in adolescent rats
Trezza, V., & Vanderschuren, L. J. M. J. (2008) · Psychopharmacology · doi:10.1007/s00213-007-1025-3 · Cited by 159
McKallip, R. J., Lombard, C., Martin, B. R., Nagarkatti, M., & Nagarkatti, P. S. (2002) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.102.033506 · Cited by 143
Sacerdote, P., Massi, P., Panerai, A. E., & Parolaro, D. (2000) · Journal of Neuroimmunology · doi:10.1016/s0165-5728(00)00307-6 · Cited by 124
Costa, B., Trovato, A. E., Colleoni, M., Giagnoni, G., Zarini, E., & Croci, T. (2005) · Pain · doi:10.1016/j.pain.2005.03.043 · Cited by 104
Guindon, J., & Beaulieu, P. (2006) · Neuropharmacology · doi:10.1016/j.neuropharm.2005.12.002 · Cited by 90
Endocannabinoids and pregnancy.
Taylor, A. H., Amoako, A. A., Bambang, K., Karasu, T., Gebeh, A., Lam, P. M. W., Marzcylo, T. H., & Konje, J. C. (2010) · Clinica Chimica Acta · doi:10.1016/j.cca.2010.03.012 · Cited by 89
De Vry, J., Denzer, D., Reissmueller, E., Eijckenboom, M., Heil, M., Meier, H., & Mauler, F. (2004) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.103.062836 · Cited by 63
Cannabinoid receptor systems: therapeutic targets for tumour intervention.
Jones, S., & Howl, J. (2003) · Expert Opinion on Therapeutic Targets · doi:10.1517/14728222.7.6.749 · Cited by 13
Metadata
- Authors
- Pertwee, R. G.
- Venue
- Current Medicinal Chemistry
- Publisher
- Bentham Science Publishers Ltd.
- Published
- 1999-08
- Volume
- 6
- Issue
- 8
- Pages
- 635-664
- ISSN
- 0929-8673 (ISSN-L)
- OpenAlex
- W4292304406
- Cited by
- 526
- References
- 0
- FWCI
- 17.37
- Type
- journal article
- Language
- en
- Open access
- closed
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
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.
