ArticleBritish journal of pharmacology2010
A novel peripherally restricted cannabinoid receptor antagonist, AM6545, reduces food intake and body weight, but does not cause malaise, in rodents.
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 102 papers, 1 of them a synthesis that pooled it.
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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.
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Who cites it
102 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Cannabinoid Receptors: An Update on Cell Signaling, Pathophysiological Roles and Therapeutic Opportunities in Neurological, Cardiovascular, and Inflammatory Diseases.International journal of molecular sciences · 2020Pooled it
- Peripheral selectivity of the novel cannabinoid receptor antagonist TM38837 in healthy subjects.British journal of clinical pharmacology · 2013Trial
- The Role of Cannabinoids and the Endocannabinoid System in the Treatment and Regulation of Nausea and Vomiting.Current topics in behavioral neurosciences · 2026Review
- Article
- The Endocannabinoid System: Implications in Gastrointestinal Physiology and Pathology.International journal of molecular sciences · 2025Review
- Cannabinoid type-1 receptors in CaMKII neurons drive impulsivity in pathological eating behavior.Molecular metabolism · 2025Article
- AM6527, a neutral CB1 receptor antagonist, suppresses opioid taking and seeking, as well as cocaine seeking in rodents without aversive effects.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2024Article
- Novel Peripherally Selective Cannabinoid Receptor 1 Neutral Antagonist Improves Metabolic Dysfunction-Associated Steatotic Liver Disease in Mice.ACS pharmacology & translational science · 2024Article
- Cholinergic Neurotransmission Controls Orexigenic Endocannabinoid Signaling in the Gut in Diet-Induced Obesity.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2024Article
- The intervention of cannabinoid receptor in chronic and acute kidney disease animal models: a systematic review and meta-analysis.Diabetology & metabolic syndrome · 2024Review
- Cannabinoids Block Fat-induced Incretin Release via CBGastro hep advances · 2024Article
- Effects of cannabinoid agonists and antagonists in male rats discriminating the synthetic cannabinoid AM2201.European journal of pharmacology · 2023Article
- Effects of the CB1 receptor antagonists AM6545 and AM4113 on metabolic syndrome-induced prostatic hyperplasia in rats.Biomolecules & biomedicine · 2023Article
- Goods and Bads of the Endocannabinoid System as a Therapeutic Target: Lessons Learned after 30 Years.Pharmacological reviews · 2023Review
- Exploring the Therapeutic Potential of Cannabinoid Receptor Antagonists in Inflammation, Diabetes Mellitus, and Obesity.Biomedicines · 2023Review
- Cannabinoid Signaling in Kidney Disease.Cells · 2023Review
- Peripheral CB1 receptor blockade acts as a memory enhancer through a noradrenergic mechanism.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2023Article
- Article
- Review
- Role of CBAmerican journal of physiology. Gastrointestinal and liver physiology · 2022Article
42 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
background and purposeCannabinoid CB(1) receptor antagonists reduce food intake and body weight, but clinical use in humans is limited by effects on the CNS. We have evaluated a novel cannabinoid antagonist (AM6545) designed to have limited CNS penetration, to see if it would inhibit food intake in rodents, without aversive effects. EXPERIMENTAL APPROACH: Cannabinoid receptor binding studies, cAMP assays, brain penetration studies and gastrointestinal motility studies were carried out to assess the activity profile of AM6545. The potential for AM6545 to induce malaise in rats and the actions of AM6545 on food intake and body weight were also investigated. KEY
resultsAM6545 binds to CB(1) receptors with a K(i) of 1.7 nM and CB(2) receptors with a K(i) of 523 nM. AM6545 is a neutral antagonist, having no effect on cAMP levels in transfected cells and was less centrally penetrant than AM4113, a comparable CB(1) receptor antagonist. AM6545 reversed the effects of WIN55212-2 in an assay of colonic motility. In contrast to AM251, AM6545 did not produce conditioned gaping or conditioned taste avoidance in rats. In rats and mice, AM6545 dose-dependently reduced food intake and induced a sustained reduction in body weight. The effect on food intake was maintained in rats with a complete subdiaphragmatic vagotomy. AM6545 inhibited food intake in CB(1) receptor gene-deficient mice, but not in CB(1)/CB(2) receptor double knockout mice. CONCLUSIONS AND IMPLICATIONS: Peripherally active, cannabinoid receptor antagonists with limited brain penetration may be useful agents for the treatment of obesity and its complications.
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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.