Evidence that the plant cannabinoid cannabigerol is a highly potent alpha2-adrenoceptor agonist and moderately potent 5HT1A receptor antagonist.

Cascio Maria Grazia, et al.
British journal of pharmacology, 2010

Abstract

Background and

Purpose

Cannabis is the source of at least seventy phytocannabinoids. The pharmacology of most of these has been little investigated, three notable exceptions being Delta(9)-tetrahydrocannabinol, cannabidiol and Delta(9)-tetrahydrocannabivarin. This investigation addressed the question of whether the little-studied phytocannabinoid, cannabigerol, can activate or block any G protein-coupled receptor. Experimental approach: The [(35)S]GTPgammaS binding assay, performed with mouse brain membranes, was used to test the ability of cannabigerol to produce G protein-coupled receptor activation or blockade. Its ability to displace [(3)H]CP55940 from mouse CB(1) and human CB(2) cannabinoid receptors and to inhibit electrically evoked contractions of the mouse isolated vas deferens was also investigated. Key

Results

In the brain membrane experiments, cannabigerol behaved as a potent alpha(2)-adrenoceptor agonist (EC(50)= 0.2 nM) and antagonized the 5-HT(1A) receptor agonist, R-(+)-8-hydroxy-2-(di-n-propylamino)tetralin (apparent K(B)= 51.9 nM). At 10 microM, it also behaved as a CB(1) receptor competitive antagonist. Additionally, cannabigerol inhibited evoked contractions of the vas deferens in a manner that appeared to be alpha(2)-adrenoceptor-mediated (EC(50)= 72.8 nM) and displayed significant affinity for mouse CB(1) and human CB(2) receptors. Conclusions and implications: This investigation has provided the first evidence that cannabigerol can activate alpha(2)-adrenoceptors, bind to cannabinoid CB(1) and CB(2) receptors and block CB(1) and 5-HT(1A) receptors. It will now be important to investigate why cannabigerol produced signs of agonism more potently in the [(35)S]GTPgammaS binding assay than in the vas deferens and also whether it can inhibit noradrenaline uptake in this isolated tissue and in the brain.

The best supplements with Cannabigerol in Brain / Mental Clarity category:

• Absolute Nature - Full Spectrum 1000 mg CBG & CBD Oil Drops / Tincture – 30ml - Our top-quality beautifully golden full-spectrum CBG & CBD oil tincture contains not only a high amount of CBG & CBD, but other naturally-occurring cannabinoids, terpenes, flavonoids, plant proteins, mineral, vitamins, essential fatty acids and other beneficial compounds from the cannabis/hemp plant, providing the best possible benefits without the high. It contains among others: Cannabigerol.

Previous article

Pharmacological data of cannabidiol- and cannabigerol-type phytocannabinoids acting on cannabinoid CB 1, CB 2 and CB 1/CB 2 heteromer receptors.

Next article

A cannabigerol quinone alleviates neuroinflammation in a chronic model of multiple sclerosis.