The drug/molecular target nomenclature used in this review conforms with the British Journal of Pharmacology's Guide to Receptors and Channels (Alexander et al., 2008).
Emerging strategies for exploiting cannabinoid receptor agonists as medicines
Article first published online: 17 FEB 2009
© 2009 The Author. Journal compilation © 2009 The British Pharmacological Society
British Journal of Pharmacology
Volume 156, Issue 3, pages 397–411, February 2009
How to Cite
Pertwee, R. G. (2009), Emerging strategies for exploiting cannabinoid receptor agonists as medicines. British Journal of Pharmacology, 156: 397–411. doi: 10.1111/j.1476-5381.2008.00048.x
The British Journal of Pharmacology has previously published themed issues on Cannabinoid Pharmacology (2007) http://www3.interscience.wiley.com/journal/121667860/issue and CB2 Receptors (2008) http://www3.interscience.wiley.com/journal/121667727/issue.
- Issue published online: 17 FEB 2009
- Article first published online: 17 FEB 2009
- Received 26 September 2008; revised 30 September 2008; accepted 8 October 2008
- CB1 receptors;
- CB2 receptors;
- cannabinoid receptor agonism;
- clinical applications;
- clinical strategies;
- blood-brain barrier;
- synergistic interactions;
- endocannabinoid system
Mandarin translation of abstract
Medicines that activate cannabinoid CB1 and CB2 receptor are already in the clinic. These are Cesamet® (nabilone), Marinol® (dronabinol; Δ9-tetrahydrocannabinol) and Sativex® (Δ9-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 CB2 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.