scholarly journals Cannabinoid Receptor 1 Binding Activity and Quantitative Analysis of Cannabis sativa L. Smoke and Vapor

2010 ◽  
Vol 58 (2) ◽  
pp. 201-207 ◽  
Author(s):  
Justin Fischedick ◽  
Frank Van Der Kooy ◽  
Robert Verpoorte
Keyword(s):  
Quantitative Analysis ◽  
Cannabis Sativa ◽  
Cannabinoid Receptor ◽  
Binding Activity ◽  
Cannabinoid Receptor 1

scholarly journals Pharmacophore-based Virtual Screening From Phytocannabinoids for Anti-obesity Activity

2021 ◽  
Author(s):  
Lenir C. Correia ◽  
Jaderson V. Ferreira ◽  
Henrique B. Lima ◽  
Guilherme M. Silva ◽  
Carlos H. T. P. da Silva ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Cannabis Sativa ◽  
Cannabinoid Receptor ◽  
Binding Free Energy ◽  
Endocannabinoid System ◽  
Mean Square ◽  
Cannabinoid Receptor 1 ◽  
Long Period ◽  
Cannabinoid Compounds ◽  
Pharmacological Target

Abstract Search for new pharmacological alternatives for obesity is based on the design and development of compounds that can aid in weight loss so that they can be used safely and effectively over a long period while maintaining their function. The endocannabinoid system is related to obesity by increasing orexigenic signals and reducing satiety signals. Cannabis sativa is a medicinal plant of polypharmaceutical potential that has been widely studied for various medicinal purposes. The in silico evaluation of their natural cannabinoids (also called phytocannabinoids) for anti-obesity purpose stems from the existence of synthetic cannabinoid compounds that have already presented this result, but which did not guarantee patient safety. In order to find new molecules from C. sativa phytocannabinoids, with the potential to interact with the pharmacological target cannabinoid receptor 1, a pharmacophore-based virtual screening was performed, including the evaluation of physicochemical, pharmacokinetic, toxicological predictions and molecular docking. The results obtained from the ZINC12 database pointed to Zinc 69 (ZINC33053402) and Zinc 70 (ZINC19084698) molecules as promising anti-obesity agents. Molecular Dynamics (MD) studies discloses that both complexes were stable by analyzing the RMSD (Root Mean Square Deviation) values, and the binding free energy values demonstrate that the selected structures can interact and inhibit their catalytic activity.

scholarly journals Absence of entourage: Terpenoids commonly found in Cannabis sativa do not modulate the functional activity of Δ9-THC at human CB1and CB2 receptors

2019 ◽  
Author(s):  
Marina Santiago ◽  
Shivani Sachdev ◽  
Jonathon C Arnold ◽  
Iain S McGregor ◽  
Mark Connor
Keyword(s):  
Membrane Potential ◽  
Potassium Channels ◽  
Cannabis Sativa ◽  
Cannabinoid Receptor ◽  
Somatostatin Receptors ◽  
Therapeutic Effects ◽  
Cannabinoid Receptor 1 ◽  
Cannabinoid Receptor 2 ◽  
Potassium Channel Activity

AbstractIntroductionCompounds present in Cannabis sativa such as phytocannabinoids and terpenoids, may act in concert to elicit therapeutic effects. Cannabinoids such as Δ9-tetrahydrocannabinol (Δ9-THC) directly activate cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2), however, it is not known if terpenoids present in Cannabis also affect cannabinoid receptor signalling. Therefore, we examined 6 common terpenoids alone, and in combination with cannabinoid receptor agonists, on CB1 and CB2 signalling in vitro.Materials and MethodsPotassium channel activity in AtT20 FlpIn cells transfected with human CB1 or CB2 receptors was measured in real-time using FLIPR® membrane potential dye in a FlexStation 3 plate reader. Terpenoids were tested individually and in combination for periods up to 30 minutes. Endogenous somatostatin receptors served as a control for direct effects of drugs on potassium channels.Resultsα-Pinene, β-pinene, β-caryophyllene, linalool, limonene and β-myrcene (up to 30-100 µM) did not change membrane potential in AtT20 cells expressing CB1 or CB2, or affect the response to a maximally effective concentration of the synthetic cannabinoid CP55,940. The presence of individual or a combination of terpenoids did not affect the hyperpolarization produced by Δ9-THC (10µM): (CB1: control, 59±7%; with terpenoids (10 µM each) 55±4%; CB2: Δ9-THC 16±5%, with terpenoids (10 µM each) 17±4%). To investigate possible effect on desensitization of CB1 responses, all six terpenoids were added together with Δ9-THC and signalling measured continuously over 30 min. Terpenoids did not affect desensitization, after 30 minutes the control hyperpolarization recovered by 63±6%, in the presence of the terpenoids recovery was 61±5%.DiscussionNone of the six of the most common terpenoids in Cannabis directly activated CB1 or CB2, or modulated the signalling of the phytocannabinoid agonist Δ9-THC. These results suggest that if a phytocannabinoid-terpenoid entourage effect exists, it is not at the CB1 or CB2 receptor level. It remains possible that terpenoids activate CB1 and CB2 signalling pathways that do not involve potassium channels, however, it seems more likely that they may act at different molecular target(s) in the neuronal circuits important for the behavioural effect of Cannabis.

Mitochondrial energy metabolism is negatively regulated by cannabinoid receptor 1 in intact human epidermis

2020 ◽  
Vol 29 (7) ◽  
pp. 616-622 ◽  
Author(s):  
Attila Oláh ◽  
Majid Alam ◽  
Jérémy Chéret ◽  
Nikolett Gréta Kis ◽  
Zoltán Hegyi ◽  
...  
Keyword(s):  
Energy Metabolism ◽  
Cannabinoid Receptor ◽  
Human Epidermis ◽  
Cannabinoid Receptor 1 ◽  
Mitochondrial Energy Metabolism
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