What question did this study set out to answer?

To determine whether the phytocannabinoid cannabigerol can activate or block specific G protein-coupled receptors, particularly adrenoceptors, serotonin receptors, and cannabinoid receptors.

December 4, 2009British Journal of PharmacologyOpen Access

Evidence that the plant cannabinoid cannabigerol is a highly potent α2‐adrenoceptor agonist and moderately potent 5HT1Areceptor antagonist

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Authors

MCM. G. CascioCornell University LGLA Gauson LSL. A. StevensonUniversity of Aberdeen

Discussion

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Implication

In vitro study reveals cannabigerol acts as an alpha2-adrenoceptor agonist and 5-HT1A antagonist in rodent tissues, highlighting non-cannabinoid receptor therapeutic pathways.

Key Points

To determine whether the phytocannabinoid cannabigerol can activate or block specific G protein-coupled receptors, particularly adrenoceptors, serotonin receptors, and cannabinoid receptors.
Measured receptor activation and antagonism in mouse brain membranes using the [35S]GTPgammaS binding assay.
Assessed cannabinoid binding by measuring displacement of [3H]CP55940 from mouse CB1 and human CB2 receptors.
Evaluated functional contractile effects using electrically evoked muscle twitches in mouse isolated vas deferens preparations.
Cannabigerol acted as a highly potent alpha2-adrenoceptor agonist (EC50 = 0.2 nM) and an antagonist of the 5-HT1A agonist 8-OH-DPAT (apparent KB = 51.9 nM) in mouse brain membranes.
At 10 microM, cannabigerol functioned as a competitive CB1 receptor antagonist while demonstrating binding affinity for mouse CB1 and human CB2 receptors.
Cannabigerol inhibited electrically evoked contractions of the mouse vas deferens through apparent alpha2-adrenoceptor activation with an EC50 of 72.8 nM.

Cite This Study

Cascio et al. (2009) studied this question.

synapsesocial.com/papers/6a7cabb59e9691931e3f6e2d https://doi.org/10.1111/j.1476-5381.2009.00515.x

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Implication

In vitro study reveals cannabigerol acts as an alpha2-adrenoceptor agonist and 5-HT1A antagonist in rodent tissues, highlighting non-cannabinoid receptor therapeutic pathways.

Evidence that the plant cannabinoid cannabigerol is a highly potent α2‐adrenoceptor agonist and moderately potent 5HT1Areceptor antagonist

Discussion

Member takes

Implication

Key Points

Cite This Study

Evidence that the plant cannabinoid cannabigerol is a highly potent α2‐adrenoceptor agonist and moderately potent 5HT1Areceptor antagonist

Discussion

Member takes

Implication

Key Points

Cite This Study

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