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The diverse CB1and CB2receptor pharmacology of three plant cannabinoids: Δ9‐tetrahydrocannabinol, cannabidiol and Δ9‐tetrahydrocannabivarin
Open accessAbstract
Cannabis sativa is the source of a unique set of compounds known collectively as plant cannabinoids or phytocannabinoids. This review focuses on the manner with which three of these compounds, (−)‐trans‐Δ 9‐tetrahydrocannabinol (Δ 9‐THC), (−)‐cannabidiol (CBD) and (−)‐trans‐Δ 9‐tetrahydrocannabivarin (Δ 9‐THCV), interact with cannabinoid CB 1 and CB 2 receptors. Δ 9‐THC, the main psychotropic constituent of cannabis, is a CB 1 and CB 2 receptor partial agonist and in line with classical pharmacology, the responses it elicits appear to be strongly influenced both by the expression level and signalling efficiency of cannabinoid receptors and by ongoing endogenous cannabinoid release. CBD displays unexpectedly high potency as an antagonist of CB 1/CB 2 receptor agonists in CB 1‐ and CB 2‐expressing cells or tissues, the manner with which it interacts with CB 2 receptors providing a possible explanation for its ability to inhibit evoked immune cell migration. Δ 9‐THCV behaves as a potent CB 2 receptor partial agonist in vitro. In contrast, it antagonizes cannabinoid receptor agonists in CB 1‐expressing tissues. This it does with relatively high potency and in a manner that is both tissue and ligand dependent. Δ 9‐THCV also interacts with CB 1 receptors when administered in vivo, behaving either as a CB 1 antagonist or, at higher doses, as a CB 1 receptor agonist. Brief mention is also made in this review, first of the production by Δ 9‐THC of pharmacodynamic tolerance, second of current knowledge about the extent to which Δ 9‐THC, CBD and Δ 9‐THCV interact with pharmacological targets other than CB 1 or CB 2 receptors, and third of actual and potential therapeutic applications for each of these cannabinoids. British Journal of Pharmacology(2008)153, 199–215; doi:10.1038/sj.bjp.0707442; published online 10 September 2007
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“THC and CBD have been found to have opposing neuropharmacological actions - the former is an partial agonist while the latter is an antagonist at CB1 and CB2 receptors (Pertwee, 2008).”
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Novel Agents for the Pharmacological Treatment of Alcohol Use Disorder
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“In this study we confirmed low affinity interactions with CB1 and CB2, as previously reported (reviewed in Pertwee, 2008b).”
BackgroundResultInfluentialA Systematic Review and Meta-Analysis of the Haemodynamic Effects of Cannabidiol
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Metadata
- Authors
- Pertwee, R. G.
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 2008-01
- Volume
- 153
- Issue
- 2
- Pages
- 199-215
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- OpenAlex
- W2168111104
- Cited by
- 1,935
- References
- 14
- FWCI
- 21.16
- Type
- journal article
- Language
- en
- Open access
- bronze
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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.
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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.