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Cannabichromene is a cannabinoid CB2 receptor agonist

Michael Udoh, Marina Santiago, Steven Devenish, Iain S. McGregor, View ORCID ProfileMark Connor
doi: https://doi.org/10.1101/435057
Michael Udoh
Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Macquarie University
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Marina Santiago
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Steven Devenish
aLambert Initiative for Cannabinoid Therapeutics, Brain and Mind Centre, The University of Sydney; Sydney, Australia
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Iain S. McGregor
aLambert Initiative for Cannabinoid Therapeutics, Brain and Mind Centre, The University of Sydney; Sydney, Australia
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Mark Connor
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Abstract

BACKGROUND Cannabichromene (CBC) is one of the most abundant phytocannabinoids in Cannabis spp. It has modest anti-nociceptive and anti-inflammatory effects and potentiates some effects of Δ9-tetrahydrocannabinol (THC) in vivo. How CBC exerts these effects is poorly defined and there is little information about its efficacy at cannabinoid receptors. We sought to determine the functional activity of CBC at CB1 and CB2 receptors.

EXPERIMENTAL APPROACH AtT20 cells stably expressing HA-tagged human CB1 and CB2 receptors were used. Assays of cellular membrane potential and loss of cell surface receptors were performed.

KEY RESULTS CBC activated CB2 but not CB1 receptors to produce a hyperpolarization of AtT20 cells. Activation of CB2 receptors was antagonised by the CB2 antagonist AM630 and sensitive to pertussis toxin. Co-application of CBC reduced activation of CB2 receptors CP55,940, a potent CB1 and CB2 agonist. Continuous CBC application induced loss of cell surface CB2 receptors and desensitisation of the CB2-induced hyperpolarization.

CONCLUSIONS AND IMPLICATIONS Cannabichromene is a selective CB2 receptor agonist displaying higher efficacy than THC in hyperpolarising AtT20 cells. CBC may contribute to the potential therapeutic effectiveness of some cannabis preparations, potentially through CB2-mediated modulation of inflammation.

Abbreviations
2-AG
2-arachidonoyl-glycerol;
AEA
anandamide;
AtT20-CB1
Mouse pituitary tumour cells stably transfected with HA human CB1 cells;
AtT20-CB2
Mouse pituitary tumour cells stably transfected with HA human CB2 cells;
CB1
Cannabinoid receptor type 1
CB2
Cannabinoid receptor type 2;
CBC
cannabichromene;
CBD
Cannabidiol;
CBN
Cannabinol;
ECS
Endocannabinoid system;
GRK
G-protein coupled receptor kinase;
HA
Haemagglutinin
PTX
Pertussis toxin;
THC
Tetrahydrocannabinol;
THCV
Tetrahydrocannabivarin.
Copyright 
The copyright holder for this preprint is the author/funder, who has granted bioRxiv a license to display the preprint in perpetuity. It is made available under a CC-BY-NC-ND 4.0 International license.
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Posted November 27, 2018.
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Cannabichromene is a cannabinoid CB2 receptor agonist
Michael Udoh, Marina Santiago, Steven Devenish, Iain S. McGregor, Mark Connor
bioRxiv 435057; doi: https://doi.org/10.1101/435057
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Cannabichromene is a cannabinoid CB2 receptor agonist
Michael Udoh, Marina Santiago, Steven Devenish, Iain S. McGregor, Mark Connor
bioRxiv 435057; doi: https://doi.org/10.1101/435057

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