ArticleNeuropharmacology2013
A role for O-1602 and G protein-coupled receptor GPR55 in the control of colonic motility in mice.
Article in Neuropharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
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Who cites it
36 citing papers in PubMed, 72 citations in OpenAlex.
- Trial
- Animal Models of Slow-Transit Constipation: Current Progress, Limitations, and Future Perspectives.Digestive diseases and sciences · 2026Review
- GPR55 negatively regulates CD8Journal of molecular histology · 2026Article
- The dual roles of natural cannabidiol in combating oxidative stress and inflammation: A potential intestinal guardian.Redox biology · 2026Review
- Gut sensory neurons as regulators of neuro-immune-microbial interactions: from molecular mechanisms to precision therapy for IBD/IBS.Journal of neuroinflammation · 2025Review
- Molecular targets of cannabinoids and their derivatives in epilepsy - a review with focus on CBD.Acta biochimica Polonica · 2025Review
- GPR55 Antagonist CID16020046 Attenuates Obesity-Induced Airway Inflammation by Suppressing Chronic Low-Grade Inflammation in the Lungs.International journal of molecular sciences · 2024Article
- GPR55 is expressed in glutamate neurons and functionally modulates drug taking and seeking in rats and mice.Translational psychiatry · 2024Article
- Cannabidiol and Intestinal Motility: a Systematic Review.Current developments in nutrition · 2023Review
- Pharmacohistory of Cannabis Use-A New Possibility in Future Drug Development for Gastrointestinal Diseases.International journal of molecular sciences · 2023Review
- The Polypharmacological Effects of Cannabidiol.Molecules (Basel, Switzerland) · 2023Review
- Involvement of the cannabinoid system in chronic inflammatory intestinal diseases: opportunities for new therapies.Intestinal research · 2022Review
- Receptor mechanisms underlying the CNS effects of cannabinoids: CBAdvances in pharmacology (San Diego, Calif.) · 2022Article
- Emerging Comorbidities in Inflammatory Bowel Disease: Eating Disorders, Alcohol and Narcotics Misuse.Journal of clinical medicine · 2021Review
- Review
- GPR119 and GPR55 as Receptors for Fatty Acid Ethanolamides, Oleoylethanolamide and Palmitoylethanolamide.International journal of molecular sciences · 2021Review
- Localization of cannabinoid and cannabinoid related receptors in the cat gastrointestinal tract.Histochemistry and cell biology · 2020Article
- Recommendations for evaluation of bladder and bowel function in pre-clinical spinal cord injury research.The journal of spinal cord medicine · 2020Review
- Irritable Bowel Syndrome: Manipulating the Endocannabinoid System as First-Line Treatment.Frontiers in neuroscience · 2020Article
- Cannabinoids and Opioids in the Treatment of Inflammatory Bowel Diseases.Clinical and translational gastroenterology · 2020Review
Corrections and comments
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Authors and funding
11 authors at 5 institutions in 6 countries.
Funding
Abstract
objectiveThe G protein-coupled receptor 55 (GPR55) is a novel cannabinoid (CB) receptor, whose role in the gastrointestinal (GI) tract remains unknown. Here we studied the significance of GPR55 in the regulation of GI motility.
designGPR55 mRNA and protein expression were measured by RT-PCR and immunohistochemistry. The effects of the GPR55 agonist O-1602 and a selective antagonist cannabidiol (CBD) were studied in vitro and in vivo and compared to a non-selective cannabinoid receptor agonist WIN55,212-2. CB1/2(-/-) and GPR55(-/-) mice were employed to identify the receptors involved.
resultsGPR55 was localized on myenteric neurons in mouse and human colon. O-1602 concentration-dependently reduced evoked contractions in muscle strips from the colon (∼60%) and weakly (∼25%) from the ileum. These effects were reversed by CBD, but not by CB1 or CB2 receptor antagonists. I.p. and i.c.v. injections of O-1602 slowed whole gut transit and colonic bead expulsion; these effects were absent in GPR55(-/-) mice. WIN55,212-2 slowed whole gut transit effects, which were counteracted in the presence of a CB1 antagonist AM251. WIN55,212-2, but not O-1602 delayed gastric emptying and small intestinal transit. Locomotion, as a marker for central sedation, was reduced following WIN55,212-2, but not O-1602 treatment.
conclusionGPR55 is strongly expressed on myenteric neurons of the colon and it is selectively involved in the regulation of colonic motility. Since activation of GPR55 receptors is not associated with central sedation, the GPR55 receptor may serve as a future target for the treatment of colonic motility disorders.
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Registered trials
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.