Cannabidiol displays unexpectedly high potency as an antagonist of CB1 and CB2 receptor agonists in vitro

By A. Thomas, G. Baillie, A. Phillips, R. Razdan, R. Ross, R. Pertwee. British Journal of Pharmacology, 2007

765 citations recorded by the source corpus.

Subfields: Endocrine and Autonomic Systems, Molecular Biology, Pharmacology

View Paper: https://www.semanticscholar.org/paper/b0901caec38834abcca2c91723936a7399da0aff

How researchers see this paper

The researchers whose trusted networks rank it highest, strongest advocate first. Every researcher gets a different order.

In Endocrine and Autonomic Systems

1. R. Pertwee
2. V. Di Marzo

In Molecular Biology

1. E. Denovan‐Wright
2. M. Kelly
3. R. Ross
4. A. Bagher
5. R. Laprairie
6. R. Pertwee

In Pharmacology

1. R. Pertwee
2. V. Di Marzo
3. George Kunos
4. R. Ross
5. R. Mechoulam
6. K. Mackie
7. Allyn C. Howlett
8. P. Greasley

Citations in the corpus

• International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid Receptors and Their Ligands: Beyond CB1 and CB2 (2010, background): “Cannabidiol has also been reported to display significant potency in vitro as a CB 2 receptor antagonist/inverse agonist (for review, see Thomas et al., 2007).”
• The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: Δ9‐tetrahydrocannabinol, cannabidiol and Δ9‐tetrahydrocannabivarin (2008, methodology): “In contrast to SR141716A and CBD (Thomas et al., 2007), D9-THCV (O-4394) lacks detectable inverse agonist activity in the [35S]GTPgS-binding assay performed with mouse whole-brain membranes and also fails to produce any detectable stimulation of [35S]GTPgS binding to such membranes (Pertwee et al.,…”
• Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor (2015, methodology): “…model the major output of the indirect motor pathway of the striatum where CB1 receptor levels are highest, relative to other regions of the brain (Trettel et al., 2000; Laprairie et al., 2013, 2014a), making this cell line ideally suited to studying endocannabinoid signalling in a more…”
• The orphan receptor GPR55 is a novel cannabinoid receptor (2007, result): “The finding that cannabidiol is an antagonist of GPR55 is interesting since until recently (Thomas et al., 2007) it has not been shown to have any significant effect on CB1 and CB2 receptor signalling (Pertwee, 1997), as confirmed by our studies (Table 1).”
• Effects of cannabinoids and cannabinoid‐enriched Cannabis extracts on TRP channels and endocannabinoid metabolic enzymes (2011, background): “This compound has little or negligible affinity at CB1 and CB2 cannabinoid receptors (Pertwee, 2004), and might behave as a functional antagonist of CB receptor-mediated agonist effects in mouse brain and in membranes from cells transfected with human CB2 receptors (Thomas et al., 2007).”