Cannabidiol displays unexpectedly high potency as an antagonist of CB1 and CB2 receptor agonists in vitro
TLDR
This study aimed to investigate whether the properties of cannabidiol extend to CB1 receptors expressed in mouse brain and to human CB2 receptors that have been transfected into CHO cells.Abstract:
Background and purpose:
A nonpsychoactive constituent of the cannabis plant, cannabidiol has been demonstrated to have low affinity for both cannabinoid CB1 and CB2 receptors. We have shown previously that cannabidiol can enhance electrically evoked contractions of the mouse vas deferens, suggestive of inverse agonism. We have also shown that cannabidiol can antagonize cannabinoid receptor agonists in this tissue with a greater potency than we would expect from its poor affinity for cannabinoid receptors. This study aimed to investigate whether these properties of cannabidiol extend to CB1 receptors expressed in mouse brain and to human CB2 receptors that have been transfected into CHO cells.read more
Citations
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The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: Δ9-tetrahydrocannabinol, cannabidiol and Δ9-tetrahydrocannabivarin
TL;DR: This review focuses on the manner with which three of these compounds, (−)‐trans‐Δ 9‐tetrahydrocannabinol (Δ9‐THC), (−]‐cannabidiol (CBD) and (−)-trans‐ Δ9‐TetrahYDrocannabivarin (Γ‐THCV), interact with cannabinoid CB1 and CB2 receptors.
Journal ArticleDOI
International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid Receptors and Their Ligands: Beyond CB1 and CB2
Roger G. Pertwee,Allyn C. Howlett,Mary E. Abood,Stephen P.H. Alexander,V. Di Marzo,Maurice R. Elphick,Peter J. Greasley,Harald S. Hansen,George Kunos,Ken Mackie,Raphael Mechoulam,Ruth Alexandra Ross +11 more
TL;DR: This review summarizes current data indicating the extent to which cannabinoid receptor ligands undergo orthosteric or allosteric interactions with non- CB1, non-CB2 established GPCRs, deorphanized receptors such as GPR55, ligand-gated ion channels, transient receptor potential (TRP) channels, and other ion channels or peroxisome proliferator-activated nuclear receptors.
Journal ArticleDOI
The orphan receptor GPR55 is a novel cannabinoid receptor
Erik Ryberg,Niklas Larsson,S. Sjögren,Stephan Hjorth,Nils-Olov Hermansson,J. Leonova,Thomas Elebring,Karolina Nilsson,Tomas Drmota,Peter J. Greasley +9 more
TL;DR: The endocannabinoid system functions through two well characterized receptor systems, the CB1 and CB2 receptors, and work by a number of groups in recent years has provided evidence that the system is more complicated and additional receptor types should exist to explain ligand activity in anumber of physiological processes.
Journal Article
The orphan receptor GPR55 is a novel cannabinoid receptor. Commentary
R. G. Pertwee,Erik Ryberg,Niklas Larsson,S. Sjögren,Stephan Hjorth,Nils-Olov Hermansson,J. Leonova,Thomas Elebring,Karolina Nilsson,Tomas Drmota,Peter J. Greasley +10 more
TL;DR: In this paper, the authors demonstrate that GPR55 is a novel cannabinoid receptor and its ligand profile with respect to CB 1 and CB 2 described here will permit delineation of its physiological function(s).
Journal ArticleDOI
Taming THC: potential cannabis synergy and phytocannabinoid‐terpenoid entourage effects
TL;DR: Particular focus will be placed on phytocannabinoid‐terpenoid interactions that could produce synergy with respect to treatment of pain, inflammation, depression, anxiety, addiction, epilepsy, cancer, fungal and bacterial infections (including methicillin‐resistant Staphylococcus aureus).
References
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Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.
TL;DR: The analysis described shows K I does not equal I 50 when competitive inhibition kinetics apply; however, K I is equal to I 50 under conditions of either noncompetitive or uncompetitive kinetics.
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Molecular targets for cannabidiol and its synthetic analogues: effect on vanilloid VR1 receptors and on the cellular uptake and enzymatic hydrolysis of anandamide.
Tiziana Bisogno,Lumir Hanus,Luciano De Petrocellis,Susanna Tchilibon,Datta E. Ponde,Ines Brandi,Aniello Schiano Moriello,John B. Davis,Raphael Mechoulam,Vincenzo Di Marzo +9 more
TL;DR: Results suggest that VR1 receptors, or increased levels of endogenous AEA, might mediate some of the pharmacological effects of CBD and its analogues, and (−)‐5′‐DMH‐CBD represents a valuable candidate for further investigation as inhibitor of AEA uptake and a possible new therapeutic agent.
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Chemical constituents of marijuana: The complex mixture of natural cannabinoids
Mahmoud A. ElSohly,Desmond Slade +1 more
TL;DR: The chemical constituents of the plant are discussed with particular emphasis on the cannabinoids as the class of compounds responsible for the drug's psychological properties.
Journal Article
Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands.
TL;DR: Although most of the chosen compounds did not discriminate between CB1 and CB2, several ligands were identified that showed selectivity and can now serve as a basis for the design of compounds with even greater selectivity.
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Evidence for a New G Protein-Coupled Cannabinoid Receptor in Mouse Brain
TL;DR: Assays of different central nervous system (CNS) regions demonstrated significant activity of cannabinoids in CB(1)(-/-) membranes from brain stem, cortex, hippocampus, diencephalon, midbrain, and spinal cord, but not basal ganglia or cerebellum.