Cited by 436Cannabis and Cannabinoid ResearchReceptor Mechanisms and SignalingPain Mechanisms and Treatments

Emerging strategies for exploiting cannabinoid receptor agonists as medicines

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Pertwee, Roger G·2009·British Journal of Pharmacology

Abstract

Mandarin translation of abstract: Medicines that activate cannabinoid CB 1 and CB 2 receptor are already in the clinic. These are Cesamet ® (nabilone), Marinol ® (dronabinol; Δ 9 ‐tetrahydrocannabinol) and Sativex ® (Δ 9 ‐tetrahydrocannabinol with cannabidiol). The first two of these medicines can be prescribed to reduce chemotherapy‐induced nausea and vomiting. Marinol ® can also be prescribed to stimulate appetite, while Sativex ® is prescribed for the symptomatic relief of neuropathic pain in adults with multiple sclerosis and as an adjunctive analgesic treatment for adult patients with advanced cancer. One challenge now is to identify additional therapeutic targets for cannabinoid receptor agonists, and a number of potential clinical applications for such agonists are mentioned in this review. A second challenge is to develop strategies that will improve the efficacy and/or the benefit‐to‐risk ratio of a cannabinoid receptor agonist. This review focuses on five strategies that have the potential to meet either or both of these objectives. These are strategies that involve: (i) targeting cannabinoid receptors located outside the blood‐brain barrier; (ii) targeting cannabinoid receptors expressed by a particular tissue; (iii) targeting up‐regulated cannabinoid receptors; (iv) targeting cannabinoid CB 2 receptors; or (v) ‘multi‐targeting’. Preclinical data that justify additional research directed at evaluating the clinical importance of each of these strategies are also discussed. Mandarin translation of abstract

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  1. [1]1. Adam L, Salois D, Rihakova L, Lapointe S, St-Onge S, Labrecque J et al. (2007). Positive allosteric modulators of CB1 receptors. Symposium on the Cannabinoids. Burlington, Vermont, USA. International Can- nabinoid Research Society, p.
  2. [53]53. Jafari MR, Ghiasvand F, Golmohammadi S, Zarrindast MR, Djah- Strategies for using cannabinoids as medicines 408 RG Pertwee British Journal of Pharmacology (2009) 156 397-411 14765381, 2009, 3,
  3. [134]134. Van Sickle MD, Duncan M, Kingsley PJ, Mouihate A, Urbani P, Mackie Strategies for using cannabinoids as medicines 410 RG Pertwee British Journal of Pharmacology (2009) 156 397-411 14765381, 2009, 3,

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Authors
Pertwee, R. G.
Affiliations
University of Aberdeen (GB)
Corresponding author
Pertwee, Roger G
Venue
British Journal of Pharmacology
Publisher
Wiley
Published
2009-02
Volume
156
Issue
3
Pages
397-411
ISSN
  • 0007-1188 (ISSN-L)
  • 1476-5381
OpenAlex
W1967922769
Cited by
436
References
155
Citations by year
2026: 6 · 2025: 10 · 2024: 32 · 2023: 10 · 2022: 12 · 2021: 18 · 2020: 27 · 2019: 14 · 2018: 24 · 2017: 30 · 2016: 37 · 2015: 19 · 2014: 27 · 2013: 36 · 2012: 39
FWCI
4.78
Type
journal article
Language
en
Open access
Locations
  • British Journal of Pharmacology (publishedVersion)
  • PubMed Central (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • GW Pharmaceuticals
  • National Institute on Drug Abuse (R37DA003672, P01DA009789, DA‐03672, R01DA003672)
Topics
  • Health Sciences › Medicine › Pharmacology › Cannabis and Cannabinoid Research
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
  • Health Sciences › Medicine › Physiology › Pain Mechanisms and Treatments
Keywords
cannabinoid receptor agonists, CB1 receptor, CB2 receptor, nabilone, dronabinol, Sativex, chemotherapy-induced nausea and vomiting, appetite stimulation, neuropathic pain, multiple sclerosis, cancer pain, blood-brain barrier, receptor up-regulation, multi-targeting, therapeutic target, risk-benefit ratio
MeSH terms
Blood-Brain Barrier, Cannabidiol, Drug Combinations, Drug Interactions, Humans, Ligands, Plant Extracts, Dronabinol, Receptor, Cannabinoid, CB1, Receptor, Cannabinoid, CB2

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