Evidence map›Paper›PMID 20002104›Full record

ArticleBritish journal of pharmacology2010

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

M G Cascio, L A Gauson, L A Stevenson, R A Ross, R G Pertwee

Open access · bronzeAbstract read
In one paragraph

Article in British journal of pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 126 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
126citing papers in PubMed, 1 pooled it
3.8field-weighted citation impact, top 8% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

126 citing papers in PubMed, 1 synthesis or guideline pooled it, 229 citations in OpenAlex.

  1. Pooled it
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  5. Review
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  8. Minor cannabinoids CBD, CBG, CBN, and CBC differentially modulate sensory neuron activation.The Journal of pharmacology and experimental therapeutics · 2026
    Article
  9. Review
  10. Article
  11. Concomitant activation of DResearch square · 2026
    Article
  12. Review
  13. The Pharmacological Profile of Plant-Derived Cannabinoids In Vitro.Current topics in behavioral neurosciences · 2026
    Review
  14. Review
  15. Concomitant activation of DDiscover pharmaceutical sciences · 2026
    Article
  16. Cannabigerol ExertsJournal of microbiology and biotechnology · 2025
    Article
  17. Article
  18. Article
  19. Article
  20. Article

66 more citing papers are in PubMed but not listed here.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

5 authors at 1 institution in 1 country.

M G CascioSchool of Medical Sciences, Institute of Medical Sciences, University of Aberdeen, Foresterhill, Aberdeen, UK.
L A Gauson
L A Stevenson
R A Ross
R G Pertwee
University of Aberdeen · GB

Funding

THC RECEPTORSR01DA003672 · NIDA · VIRGINIA COMMONWEALTH UNIVERSITY · PI WILEY, JENNY L. · 1985 to 2018
$4.9M
THC RECEPTORSR37DA003672 · NIDA · VIRGINIA COMMONWEALTH UNIVERSITY · PI MARTIN, BILLY R · 1997 to 2006
$2.8M
NIDA NIH HHS DA-03672NIDA NIH HHS R01 DA003672NIDA NIH HHS R37 DA003672
6 · The paper itself

Abstract

background and purposeCannabis 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

resultsIn 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.

Indexed as

Serotonin 5-HT1 Receptor AntagonistsAdrenergic alpha-2 Receptor AgonistsAdrenergic alpha-AgonistsAnimalsCannabinoidsCannabisCHO CellsCricetinaeCricetulusDose-Response Relationship, DrugHumansMaleMiceMice, Inbred C57BLMice, KnockoutMuscle ContractionAdrenergic alpha-2 Receptor AgonistsAdrenergic alpha-AgonistscannabigerolCannabinoidsReceptor, Cannabinoid, CB1Receptor, Cannabinoid, CB2Serotonin 5-HT1 Receptor AntagonistsSerotonin Antagonists

Identifiers

PMID20002104
PMCPMC2823359
OpenAlexW1898835919

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.