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Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
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Cannabichromene is a cannabinoid CB2 receptor agonist.
Michael Udoh1, Marina Santiago1, Steven Devenish2
1Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Macquarie University, Sydney, NSW, Australia.
British Journal of Pharmacology
|August 2, 2019
Summary
Cannabichromene (CBC) selectively activates CB2 receptors, not CB1, and may contribute to cannabis
Area of Science:
- Pharmacology
- Cannabinoid Science
Background:
- Cannabichromene (CBC) is a prevalent phytocannabinoid in Cannabis spp.
- CBC exhibits anti-inflammatory and analgesic properties, but its mechanism of action at cannabinoid receptors is unclear.
Purpose of the Study:
- To investigate the functional activity of CBC at cannabinoid CB1 and CB2 receptors.
- To determine CBC's efficacy and interaction with cannabinoid receptors.
Main Methods:
- Utilized AtT20 cells expressing human CB1 and CB2 receptors.
- Assayed cellular membrane potential and cell surface receptor levels.
Main Results:
- CBC activated CB2 receptors, causing cell hyperpolarization, but not CB1 receptors.
- CBC's action on CB2 receptors was antagonized by AM630 and sensitive to Pertussis toxin.
- CBC application led to CB2 receptor desensitization and reduced cell surface receptor levels.
Conclusions:
- CBC acts as a selective CB2 receptor agonist with higher efficacy than THC in this model.
- CBC can modulate CB2 receptor regulation, including desensitization.
- CBC may contribute to the therapeutic potential of cannabis preparations via CB2 receptor-mediated anti-inflammatory effects.
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