Pharmacological data of cannabidiol- and cannabigerol-type phytocannabinoids acting on cannabinoid CB
Animals
Binding Sites
Binding, Competitive
Biosensing Techniques
CHO Cells
Cannabidiol
/ metabolism
Cannabinoids
/ metabolism
Cricetulus
Cyclic AMP
/ metabolism
Dose-Response Relationship, Drug
Drug Inverse Agonism
Extracellular Signal-Regulated MAP Kinases
/ metabolism
Fluorescence Resonance Energy Transfer
HEK293 Cells
Humans
Ligands
Phosphorylation
Protein Binding
Radioligand Assay
Receptor, Cannabinoid, CB1
/ agonists
Receptor, Cannabinoid, CB2
/ agonists
Signal Transduction
beta-Arrestins
/ metabolism
Biased signaling
Cytocrin
GPCR structure
Homogeneous binding
Phytocannabinoids
Radioligand binding
Journal
Pharmacological research
ISSN: 1096-1186
Titre abrégé: Pharmacol Res
Pays: Netherlands
ID NLM: 8907422
Informations de publication
Date de publication:
09 2020
09 2020
Historique:
received:
19
04
2020
revised:
13
05
2020
accepted:
15
05
2020
pubmed:
30
5
2020
medline:
7
7
2021
entrez:
30
5
2020
Statut:
ppublish
Résumé
Recent approved medicines whose active principles are Δ Cannabinoid CB Determination of the affinity of phytocannabinoids for cannabinoid receptors and functional assessment of effects promoted by these compounds when interacting with cannabinoid receptors. A heterologous system expressing the human versions of CB Affinity of cannabinoids depend on the ligand of reference and may be different in membranes and in living cells. All tested phytocannabinoids have agonist-like behavior but behaved as inverse-agonists in the presence of selective receptor agonists. CBGV displayed enhanced potency in many of the functional outputs. However, the most interesting result was a biased signaling that correlated with differential affinity, i.e. the overall results suggest that the binding mode of each ligand leads to specific receptor conformations underlying biased signaling outputs. Results here reported and the recent elucidation of the three-dimensional structure of CB
Sections du résumé
BACKGROUND
Recent approved medicines whose active principles are Δ
HYPOTHESIS/PURPOSE
Cannabinoid CB
STUDY DESIGN
Determination of the affinity of phytocannabinoids for cannabinoid receptors and functional assessment of effects promoted by these compounds when interacting with cannabinoid receptors.
METHODS
A heterologous system expressing the human versions of CB
RESULTS
Affinity of cannabinoids depend on the ligand of reference and may be different in membranes and in living cells. All tested phytocannabinoids have agonist-like behavior but behaved as inverse-agonists in the presence of selective receptor agonists. CBGV displayed enhanced potency in many of the functional outputs. However, the most interesting result was a biased signaling that correlated with differential affinity, i.e. the overall results suggest that the binding mode of each ligand leads to specific receptor conformations underlying biased signaling outputs.
CONCLUSION
Results here reported and the recent elucidation of the three-dimensional structure of CB
Identifiants
pubmed: 32470563
pii: S1043-6618(20)31248-2
doi: 10.1016/j.phrs.2020.104940
pii:
doi:
Substances chimiques
CNR1 protein, human
0
CNR2 protein, human
0
Cannabinoids
0
Ligands
0
Receptor, Cannabinoid, CB1
0
Receptor, Cannabinoid, CB2
0
beta-Arrestins
0
Cannabidiol
19GBJ60SN5
Cyclic AMP
E0399OZS9N
Extracellular Signal-Regulated MAP Kinases
EC 2.7.11.24
cannabigerol
J1K406072N
Types de publication
Comparative Study
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
104940Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.