ArticleBritish journal of pharmacology2015
AM841, a covalent cannabinoid ligand, powerfully slows gastrointestinal motility in normal and stressed mice in a peripherally restricted manner.
Article in British journal of pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
What it found
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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.
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.
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Who cites it
15 citing papers in PubMed, 33 citations in OpenAlex.
- The Endocannabinoid System in the Development and Treatment of Obesity: Searching for New Ideas.International journal of molecular sciences · 2025Review
- Efficacy of multimodal rehabilitation strategies on gastrointestinal function recovery in postoperative aortic dissection patients: a narrative review.Frontiers in physiology · 2025Review
- The Endocannabinoid System of the Nervous and Gastrointestinal Systems Changes after a Subnoxious Cisplatin Dose in Male Rats.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Supporting gut health with medicinal cannabis in people with advanced cancer: potential benefits and challenges.British journal of cancer · 2024Review
- Discovery of the cyclotide caripe 11 as a ligand of the cholecystokinin-2 receptor.Scientific reports · 2022Article
- Novel Psychoactive Substances: The Razor's Edge between Therapeutical Potential and Psychoactive Recreational Misuse.Medicines (Basel, Switzerland) · 2022Review
- The Microbiome and Gut Endocannabinoid System in the Regulation of Stress Responses and Metabolism.Frontiers in cellular neuroscience · 2022Review
- The Peripheral Cannabinoid Receptor Type 1 (CBMolecules (Basel, Switzerland) · 2021Review
- Endocannabinoid regulation of homeostatic feeding and stress-induced alterations in food intake in male rats.British journal of pharmacology · 2019Article
- Role of Cannabinoid Receptor Type 1 in Insulin Resistance and Its Biological Implications.International journal of molecular sciences · 2019Review
- Overcoming the Psychiatric Side Effects of the Cannabinoid CB1 Receptor Antagonists: Current Approaches for Therapeutics Development.Current topics in medicinal chemistry · 2019Review
- Cannabinoids and GI Disorders: Endogenous and Exogenous.Current treatment options in gastroenterology · 2016Review
- The Role of the Endocannabinoid System in the Brain-Gut Axis.Gastroenterology · 2016Review
- Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).Journal of medicinal chemistry · 2016Article
- In vitro and non-invasive in vivo effects of the cannabinoid-1 receptor agonist AM841 on gastrointestinal motor function in the rat.Neurogastroenterology and motility · 2015Article
Corrections and comments
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Authors and funding
13 authors at 4 institutions in 4 countries.
Funding
Abstract
background and purposeCannabinoid (CB) ligands have been demonstrated to have utility as novel therapeutic agents for the treatment of pain, metabolic conditions and gastrointestinal (GI) disorders. However, many of these ligands are centrally active, which limits their usefulness. Here, we examine a unique novel covalent CB receptor ligand, AM841, to assess its potential for use in physiological and pathophysiological in vivo studies. EXPERIMENTAL APPROACH: The covalent nature of AM841 was determined in vitro using electrophysiological and receptor internalization studies on isolated cultured hippocampal neurons. Mouse models were used for behavioural analysis of analgesia, hypothermia and hypolocomotion. The motility of the small and large intestine was assessed in vivo under normal conditions and after acute stress. The brain penetration of AM841 was also determined. KEY
resultsAM841 behaved as an irreversible CB1 receptor agonist in vitro. AM841 potently reduced GI motility through an action on CB1 receptors in the small and large intestine under physiological conditions. AM841 was even more potent under conditions of acute stress and was shown to normalize accelerated GI motility under these conditions. This compound behaved as a peripherally restricted ligand, showing very little brain penetration and no characteristic centrally mediated CB1 receptor-mediated effects (analgesia, hypothermia or hypolocomotion). CONCLUSIONS AND IMPLICATIONS: AM841, a novel peripherally restricted covalent CB1 receptor ligand that was shown to be remarkably potent, represents a new class of potential therapeutic agents for the treatment of functional GI 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.