Emerging strategies for exploiting cannabinoid receptor agonists as medicines
Open accessAbstract
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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Behavioural and neurochemical effects of combined MDMA and THC administration in mice
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Contribution of CB1 blockade to the management of high-risk abdominal obesity
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Self-citationDirect suppression of autoreactive lymphocytes in the central nervous system via the CB2 receptor
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Self-citationTherapeutic Applications for Agents that Act at CB1 and CB2 Receptors
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Khan (2000) · doi:10.1002/1531-8249(200008)48:2
Flagged first, then by citations
Research works printed but not linked: 3
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- Authors
- Pertwee, R. G.
- Affiliations
- University of Aberdeen (GB)
- Corresponding author
- Pertwee, Roger G
- ORCID
- 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
- PMC
- PMC2697681
- 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
- bronze
- doi.org
- 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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