article Open AccessTop 1% cited
Cannabidiol is a negative allosteric modulator of the cannabinoid CB <sub>1</sub> receptor
British Journal of Pharmacology · 2015 · Vol. 172(20) · pp. 4790–4805
Robert B. Laprairie(Dalhousie University)Amina M. Bagher(Dalhousie University)Michael E. Kelly(Dalhousie University)Eileen M. Denovan‐Wright✉(Dalhousie University)
Abstract
Cannabidiol behaved as a non-competitive negative allosteric modulator of CB1 receptors. Allosteric modulation, in conjunction with effects not mediated by CB1 receptors, may explain the in vivo effects of cannabidiol. Allosteric modulators of CB1 receptors have the potential to treat CNS and peripheral disorders while avoiding the adverse effects associated with orthosteric agonism or antagonism of these receptors.
Cannabis and Cannabinoid ResearchPancreatic function and diabetesSleep and Wakefulness ResearchCannabidiolAllosteric regulationAllosteric modulatorReceptorCannabinoid receptorPharmacologyCannabinoidChemistryCannabinoid receptor type 2Functional selectivity
MeSH terms
AnimalsCannabidiolCell LineHumansArrestinsMAP Kinase Signaling SystemReceptor, Cannabinoid, CB1MicePhospholipase C betaHEK293 CellsCannabinoid Receptor Modulators
Funding
- Huntington Society of Canada
- Nova Scotia Health Research Foundation
- King Abdulaziz University
- Killam Trusts
- Canadian Institutes of Health Research
Citations
980
FWCI
36.29
field-weighted impact
References
47
Percentile
100%
vs. same field & year
Citations per year
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References
The orphan receptor GPR55 is a novel cannabinoid receptor
British Journal of Pharmacology · 2007 · 1,550 citations
Cannabidiol displays unexpectedly high potency as an antagonist of CB<sub>1</sub>and CB<sub>2</sub>receptor agonists<i>in vitro</i>
British Journal of Pharmacology · 2007 · 744 citations
Molecular targets for cannabidiol and its synthetic analogues: effect on vanilloid VR1 receptors and on the cellular uptake and enzymatic hydrolysis of anandamide
British Journal of Pharmacology · 2001 · 1,289 citations
Allosteric Modulation of the Cannabinoid CB1 Receptor
Molecular Pharmacology · 2005 · 443 citations
Dominant phenotypes produced by the HD mutation in STHdhQ111 striatal cells
Human Molecular Genetics · 2000 · 620 citations
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