Phytoplant | Cannabigerol Action at Cannabinoid CB1 and CB2 Receptors and at CB1

Cannabigerol Action at Cannabinoid CB1 and CB2 Receptors and at CB1–CB2 Heteroreceptor Complexes.

Introduction

Cannabigerol (CBG) is one of the major phytocannabinoids present in Cannabis sativa L. that is attracting pharmacological interest because it is non-psychotropic and is abundant in some industrial hemp varieties. The aim of this work was to investigate in parallel the binding properties of CBG to cannabinoid CB1 (CB1R) and CB2 (CB2R) receptors and the effects of the compound on agonist activation of those receptors and of CB1–CB2 heteroreceptor complexes.

Material and méthods

CBG was purified from the Cannabis variety AÍDA (CPVO/ 20160167) following a patented method described in the Phytoplant Patent: “Methods of purifying cannabinoids, compositions and kits thereof” with code 9765000 B2. The CBG has a purity > 95%. CANNA products were used for the variety cultivation.

Results

Using [3H]-CP-55940, CBG competed with low micromolar Ki values the binding to CB1R and CB2R. Homogeneous binding in living cells, which is only technically possible for the CB2R, provided a 152 nM Ki value. Also interesting, CBG competed the binding of [3H]-WIN-55,212-2 to CB2R but not to CB1R (Ki: 2.7 versus >30 μM). The phytocannabinoid modulated signaling mediated by receptors and receptor heteromers even at low concentrations of 0.1–1 μM. cAMP, pERK, β-arrestin recruitment and label-free assays in HEK-293T cells expressing the receptors and treated with endocannabinoids or selective agonists proved that CBG is a partial agonist of CB2R. The action on cells expressing heteromers was similar to that obtained in cells expressing the CB2R.

Discusion

The effect of CBG on CB1R was measurable but the underlying molecular mechanisms remain uncertain. The results indicate that CBG is indeed effective as regulator of endocannabinoid signaling.

Go to the publication

Other publications

First Report of Charcoal Rot Caused by Macrophomina phaseolina on Hemp (Cannabis sativa L.) Varieties Cultivated in Southern Spain

Development of ornamental Cannabis sativa L. cultivars: phytochemical, morphological, genetic characterization and propagation aspects

Influence of media composition and genotype for successful Cannabis sativa L. in vitro introduction

Yield of new hemp varieties for medical purposes in a semi-arid Mediterranean environment (Spain)

Cannabinoids and terpenoids yields of the ornamental Cannabis sativa L. cultivar ‘Divina’ characterized by a variegated foliage as morphological marker

Cannabidiol Prevents the Expression of the Locomotor Sensitization and the Metabolic Changes in the Nucleus Accumbent and Prefrontal Cortex Elicited by the Combined Administration of Cocaine and Caffeine in Rats.

Impact of Plant Density and Irrigation on Yield of Hemp (Cannabis sativa L.) in a Mediterranean Semi-arid Environment

Tetrahydrocannabinolic acid is a potent PPARγ agonist with neuroprotective activity.

Binding and Signaling Studies Disclose a Potential Allosteric Site for Cannabidiol in Cannabinoid CB2 Receptors.

Seeking suitable agronomical practices for industrial hemp (Cannabis sativa L.) cultivation for biomedical applications.

Cannabidiol skews biased agonism at cannabinoid CB1 and CB2 receptors with smaller effect in CB1-CB2 heteroreceptor complexes.

Potentiation of cannabinoid signaling in microglia by adenosine A2A receptor antagonists

Pharmacological potential of varinic-, minor-, and acidic phytocannabinoids

Pharmacological data of cannabidiol- and cannabigerol-type phytocannabinoids acting on cannabinoid CB1, CB2 and CB1/CB2 heteromer receptors.

The potential of near infrared spectroscopy to estimate the content of cannabinoids in Cannabis sativa L.: A comparative study.

Untargeted characterization of extracts from Cannabis sativa L. cultivars by gas and liquid chromatography coupled to mass spectrometry in high resolution mode.

A Comparative In Vitro Study of the Neuroprotective Effect Induced by Cannabidiol, Cannabigerol, and Their Respective Acid Forms: Relevance of the 5-HT1A Receptors.

Exploring the mysteries of cannabis through gas chromatography

Biological Activity of Cannabis sativa L. Extracts Critically Depends on Solvent Polarity and Decarboxylation.

Thermal desorption-ion mobility spectrometry: A rapid sensor for the detection of cannabinoids and discrimination of Cannabis sativa L. chemotypes

Similarities and differences upon binding of naturally occurring Δ9-tetrahydrocannabinol-derivatives to cannabinoid CB1 and CB2 receptors

Politica de Calidad

Ayudas de la Unión Europea para el autoconsumo fotovoltaico

Other services

Plant material

Check our Variety catalogue

Technical assistance

Experience and scientific rigor to walk by your side in your project.

Licensable technology

Use our varieties and patented technological processes.

Research

R+D+i in cultivation, breeding and extraction.

Ask for information

Can we be of help to you? Do you have any questions about us? Write to us and we will contact you as soon as possible.

To enable the functionality of sending messages from the website we need you to accept technical cookies, as we use Google's reCAPTCHA 3 to prevent messages from fraudulent bots.

Accept the use of technical cookies