Journal ArticleDOI
Agonistic Properties of Cannabidiol at 5-HT1a Receptors
TLDR
These studies demonstrate that CBD is a modest affinity agonist at the human 5-HT1a receptor, and indicate that cannabidiol may have interesting and useful potential beyond the realm of cannabinoid receptors.Abstract:
Cannabidiol (CBD) is a major, biologically active, but psycho-inactive component of cannabis. In this cell culture-based report, CBD is shown to displace the agonist, [3H]8-OHDPAT from the cloned human 5-HT1a receptor in a concentration-dependent manner. In contrast, the major psychoactive component of cannabis, tetrahydrocannabinol (THC) does not displace agonist from the receptor in the same micromolar concentration range. In signal transduction studies, CBD acts as an agonist at the human 5-HT1a receptor as demonstrated in two related approaches. First, CBD increases [35S]GTPcS binding in this G protein coupled receptor system, as does the known agonist serotonin. Second, in this GPCR system, that is negatively coupled to cAMP production, both CBD and 5-HT decrease cAMP concentration at similar apparent levels of receptor occupancy, based upon displacement data. Preliminary comparative data is also presented from the cloned rat 5-HT2a receptor suggesting that CBD is active, but less so, relative to the human 5-HT1a receptor, in binding analyses. Overall, these studies demonstrate that CBD is a modest affinity agonist at the human 5-HT1a receptor. Additional work is required to compare CBD’s potential at other serotonin receptors and in other species. Finally, the results indicate that cannabidiol may have interesting and useful potential beyond the realm of cannabinoid receptors.read more
Citations
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Journal ArticleDOI
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
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).
Journal ArticleDOI
Cannabidiol enhances anandamide signaling and alleviates psychotic symptoms of schizophrenia
F. M. Leweke,Daniele Piomelli,Daniele Piomelli,Franziska Pahlisch,Franziska Pahlisch,D Muhl,D Muhl,C.W. Gerth,Carolin Hoyer,Carolin Hoyer,Joachim Klosterkötter,Martin Hellmich,Dagmar Koethe,Dagmar Koethe +13 more
TL;DR: It is suggested that inhibition of anandamide deactivation may contribute to the antipsychotic effects of cannabidiol potentially representing a completely new mechanism in the treatment of schizophrenia.
Journal ArticleDOI
Effects of cannabinoids and cannabinoid-enriched Cannabis extracts on TRP channels and endocannabinoid metabolic enzymes
Luciano De Petrocellis,Alessia Ligresti,Aniello Schiano Moriello,Marco Allarà,Tiziana Bisogno,Stefania Petrosino,Colin Stott,Vincenzo Di Marzo +7 more
TL;DR: CBD and Δ9‐tetrahydrocannabinol interact with transient receptor potential (TRP) channels and enzymes of the endocannabinoid system to explore its role in Cannabidiol-like properties.
Journal ArticleDOI
Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor.
TL;DR: It is hypothesized that cannabidiol would inhibit cannabinoid agonist activity through negative allosteric modulation of CB1 receptors through positive allosterics modulation ofCB1 receptors.
References
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A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding
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A review of central 5-HT receptors and their function
Nicholas M. Barnes,Trevor Sharp +1 more
TL;DR: A number of 5-HT receptor ligands are currently utilised, or are in clinical development, to reduce the symptoms of CNS dysfunction and the functional responses attributed to each receptor in the brain are reviewed.
Journal ArticleDOI
International Union of Pharmacology. XXVII. Classification of Cannabinoid Receptors
Allyn C. Howlett,Francis Barth,Tom I. Bonner,Guy A. Cabral,Pierre Casellas,William A. Devane,Christian C. Felder,Miles Herkenham,Ken Mackie,Billy R. Martin,Raphael Mechoulam,Roger G. Pertwee +11 more
TL;DR: It is considered premature to rename cannabinoid receptors after an endogenous agonist as is recommended by the International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification, because pharmacological evidence for the existence of additional types of cannabinoid receptor is emerging and other kinds of supporting evidence are still lacking.
Journal ArticleDOI
Pharmacology of cannabinoid cb1 and cb2 receptors
TL;DR: This review focuses on the classification, binding properties, effector systems and distribution of cannabinoid receptors, and describes the various cannabinoid receptor agonists and antagonists now available and considers the main in vivo and in vitro bioassay methods that are generally used.
Journal ArticleDOI
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.