ArticleThe international journal of neuropsychopharmacology2016
The CB1 Neutral Antagonist AM4113 Retains the Therapeutic Efficacy of the Inverse Agonist Rimonabant for Nicotine Dependence and Weight Loss with Better Psychiatric Tolerability.
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Article in The international journal of neuropsychopharmacology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers, 1 of them a synthesis that pooled it.
0numbers the graph read from it
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42citing papers in PubMed, 1 pooled it
8.9field-weighted citation impact, top 2% of its field
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Who cites it
42 citing papers in PubMed, 1 synthesis or guideline pooled it, 73 citations in OpenAlex.
- Modulating the endocannabinoid system in alcohol use disorder: A translational systematic review and meta-analysis of preclinical and human studies.Molecular psychiatry · 2026Pooled it
- Heroin-induced neuroadaptations of CB1 receptors and their involvement in conditioned place preference.Psychopharmacology · 2026Article
- Cannabinoid-based Pharmacology for the Management of Substance Use Disorders.Current topics in behavioral neurosciences · 2026Review
- Involvement of CB1R and CB2R Ligands in Sleep Disorders and Addictive Behaviors in the Last 25 Years.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Cannabis use disorder: from neurobiology to treatment.The Journal of clinical investigation · 2024Review
- 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
- Neurobiology of Stress-Induced Nicotine Relapse.International journal of molecular sciences · 2024Review
- Dysregulation of the endogenous cannabinoid system following opioid exposure.Psychiatry research · 2023Review
- 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
- Development of a membrane-based Gi-CASE biosensor assay for profiling compounds at cannabinoid receptors.Frontiers in pharmacology · 2023Article
- Review
- Therapeutic potential of PIMSR, a novel CB1 receptor neutral antagonist, for cocaine use disorder: evidence from preclinical research.Translational psychiatry · 2022Article
- Tobacco and nicotine use.Nature reviews. Disease primers · 2022Review
- Off-label and investigational drugs in the treatment of alcohol use disorder: A critical review.Frontiers in pharmacology · 2022Review
- New Insights in the Involvement of the Endocannabinoid System and Natural Cannabinoids in Nicotine Dependence.International journal of molecular sciences · 2021Review
- CB1 receptor neutral antagonist treatment epigenetically increases neuropeptide Y expression and decreases alcohol drinking.Neuropharmacology · 2021Article
- The Endocannabinoid System: A Potential Target for the Treatment of Various Diseases.International journal of molecular sciences · 2021Review
- Cannabis use and cannabis use disorder.Nature reviews. Disease primers · 2021Review
Corrections and comments
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Authors and funding
11 authors at 4 institutions in 2 countries.
Aliou B GueyeTranslational Addiction Research Laboratory (Dr Gueye, Mr Pryslawsky, Dr Trigo, and Dr Le Foll), Alcohol Research and Treatment Clinic, Addiction Medicine Services, Ambulatory Care and Structured Treatments (Dr Le Foll), and Campbell Family Mental Health Research Institute (Dr Le Foll), Centre for Addiction and Mental Health, Toronto, ON, Canada; Department of Family and Community Medicine, Department of Pharmacology, and Department of Psychiatry, Division of Brain and Therapeutics, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Institute of Medical Sciences, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Department of Pharmacology, Faculty of Medicine, School of Health Sciences, University of Ioannina, Greece (Ms Poulia and Drs Delis and Antoniou); Department of Anatomy and Cell Biology, The Schulich School of Medicine and Dentistry, University of Western Ontario, London, ON, Canada (Drs Loureiro and Laviolette); Center for Drug Discovery, Department of Pharmaceutical Sciences and Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA (Drs Vemuri and Makriyannis).
Yaroslaw PryslawskyTranslational Addiction Research Laboratory (Dr Gueye, Mr Pryslawsky, Dr Trigo, and Dr Le Foll), Alcohol Research and Treatment Clinic, Addiction Medicine Services, Ambulatory Care and Structured Treatments (Dr Le Foll), and Campbell Family Mental Health Research Institute (Dr Le Foll), Centre for Addiction and Mental Health, Toronto, ON, Canada; Department of Family and Community Medicine, Department of Pharmacology, and Department of Psychiatry, Division of Brain and Therapeutics, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Institute of Medical Sciences, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Department of Pharmacology, Faculty of Medicine, School of Health Sciences, University of Ioannina, Greece (Ms Poulia and Drs Delis and Antoniou); Department of Anatomy and Cell Biology, The Schulich School of Medicine and Dentistry, University of Western Ontario, London, ON, Canada (Drs Loureiro and Laviolette); Center for Drug Discovery, Department of Pharmaceutical Sciences and Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA (Drs Vemuri and Makriyannis).
Jose M TrigoTranslational Addiction Research Laboratory (Dr Gueye, Mr Pryslawsky, Dr Trigo, and Dr Le Foll), Alcohol Research and Treatment Clinic, Addiction Medicine Services, Ambulatory Care and Structured Treatments (Dr Le Foll), and Campbell Family Mental Health Research Institute (Dr Le Foll), Centre for Addiction and Mental Health, Toronto, ON, Canada; Department of Family and Community Medicine, Department of Pharmacology, and Department of Psychiatry, Division of Brain and Therapeutics, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Institute of Medical Sciences, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Department of Pharmacology, Faculty of Medicine, School of Health Sciences, University of Ioannina, Greece (Ms Poulia and Drs Delis and Antoniou); Department of Anatomy and Cell Biology, The Schulich School of Medicine and Dentistry, University of Western Ontario, London, ON, Canada (Drs Loureiro and Laviolette); Center for Drug Discovery, Department of Pharmaceutical Sciences and Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA (Drs Vemuri and Makriyannis).
Nafsika PouliaTranslational Addiction Research Laboratory (Dr Gueye, Mr Pryslawsky, Dr Trigo, and Dr Le Foll), Alcohol Research and Treatment Clinic, Addiction Medicine Services, Ambulatory Care and Structured Treatments (Dr Le Foll), and Campbell Family Mental Health Research Institute (Dr Le Foll), Centre for Addiction and Mental Health, Toronto, ON, Canada; Department of Family and Community Medicine, Department of Pharmacology, and Department of Psychiatry, Division of Brain and Therapeutics, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Institute of Medical Sciences, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Department of Pharmacology, Faculty of Medicine, School of Health Sciences, University of Ioannina, Greece (Ms Poulia and Drs Delis and Antoniou); Department of Anatomy and Cell Biology, The Schulich School of Medicine and Dentistry, University of Western Ontario, London, ON, Canada (Drs Loureiro and Laviolette); Center for Drug Discovery, Department of Pharmaceutical Sciences and Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA (Drs Vemuri and Makriyannis).
Foteini DelisTranslational Addiction Research Laboratory (Dr Gueye, Mr Pryslawsky, Dr Trigo, and Dr Le Foll), Alcohol Research and Treatment Clinic, Addiction Medicine Services, Ambulatory Care and Structured Treatments (Dr Le Foll), and Campbell Family Mental Health Research Institute (Dr Le Foll), Centre for Addiction and Mental Health, Toronto, ON, Canada; Department of Family and Community Medicine, Department of Pharmacology, and Department of Psychiatry, Division of Brain and Therapeutics, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Institute of Medical Sciences, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Department of Pharmacology, Faculty of Medicine, School of Health Sciences, University of Ioannina, Greece (Ms Poulia and Drs Delis and Antoniou); Department of Anatomy and Cell Biology, The Schulich School of Medicine and Dentistry, University of Western Ontario, London, ON, Canada (Drs Loureiro and Laviolette); Center for Drug Discovery, Department of Pharmaceutical Sciences and Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA (Drs Vemuri and Makriyannis).
Katerina AntoniouTranslational Addiction Research Laboratory (Dr Gueye, Mr Pryslawsky, Dr Trigo, and Dr Le Foll), Alcohol Research and Treatment Clinic, Addiction Medicine Services, Ambulatory Care and Structured Treatments (Dr Le Foll), and Campbell Family Mental Health Research Institute (Dr Le Foll), Centre for Addiction and Mental Health, Toronto, ON, Canada; Department of Family and Community Medicine, Department of Pharmacology, and Department of Psychiatry, Division of Brain and Therapeutics, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Institute of Medical Sciences, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Department of Pharmacology, Faculty of Medicine, School of Health Sciences, University of Ioannina, Greece (Ms Poulia and Drs Delis and Antoniou); Department of Anatomy and Cell Biology, The Schulich School of Medicine and Dentistry, University of Western Ontario, London, ON, Canada (Drs Loureiro and Laviolette); Center for Drug Discovery, Department of Pharmaceutical Sciences and Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA (Drs Vemuri and Makriyannis).
Michael LoureiroTranslational Addiction Research Laboratory (Dr Gueye, Mr Pryslawsky, Dr Trigo, and Dr Le Foll), Alcohol Research and Treatment Clinic, Addiction Medicine Services, Ambulatory Care and Structured Treatments (Dr Le Foll), and Campbell Family Mental Health Research Institute (Dr Le Foll), Centre for Addiction and Mental Health, Toronto, ON, Canada; Department of Family and Community Medicine, Department of Pharmacology, and Department of Psychiatry, Division of Brain and Therapeutics, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Institute of Medical Sciences, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Department of Pharmacology, Faculty of Medicine, School of Health Sciences, University of Ioannina, Greece (Ms Poulia and Drs Delis and Antoniou); Department of Anatomy and Cell Biology, The Schulich School of Medicine and Dentistry, University of Western Ontario, London, ON, Canada (Drs Loureiro and Laviolette); Center for Drug Discovery, Department of Pharmaceutical Sciences and Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA (Drs Vemuri and Makriyannis).
Steve R LavioletteTranslational Addiction Research Laboratory (Dr Gueye, Mr Pryslawsky, Dr Trigo, and Dr Le Foll), Alcohol Research and Treatment Clinic, Addiction Medicine Services, Ambulatory Care and Structured Treatments (Dr Le Foll), and Campbell Family Mental Health Research Institute (Dr Le Foll), Centre for Addiction and Mental Health, Toronto, ON, Canada; Department of Family and Community Medicine, Department of Pharmacology, and Department of Psychiatry, Division of Brain and Therapeutics, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Institute of Medical Sciences, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Department of Pharmacology, Faculty of Medicine, School of Health Sciences, University of Ioannina, Greece (Ms Poulia and Drs Delis and Antoniou); Department of Anatomy and Cell Biology, The Schulich School of Medicine and Dentistry, University of Western Ontario, London, ON, Canada (Drs Loureiro and Laviolette); Center for Drug Discovery, Department of Pharmaceutical Sciences and Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA (Drs Vemuri and Makriyannis).
Kiran VemuriTranslational Addiction Research Laboratory (Dr Gueye, Mr Pryslawsky, Dr Trigo, and Dr Le Foll), Alcohol Research and Treatment Clinic, Addiction Medicine Services, Ambulatory Care and Structured Treatments (Dr Le Foll), and Campbell Family Mental Health Research Institute (Dr Le Foll), Centre for Addiction and Mental Health, Toronto, ON, Canada; Department of Family and Community Medicine, Department of Pharmacology, and Department of Psychiatry, Division of Brain and Therapeutics, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Institute of Medical Sciences, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Department of Pharmacology, Faculty of Medicine, School of Health Sciences, University of Ioannina, Greece (Ms Poulia and Drs Delis and Antoniou); Department of Anatomy and Cell Biology, The Schulich School of Medicine and Dentistry, University of Western Ontario, London, ON, Canada (Drs Loureiro and Laviolette); Center for Drug Discovery, Department of Pharmaceutical Sciences and Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA (Drs Vemuri and Makriyannis).
Alexandros MakriyannisTranslational Addiction Research Laboratory (Dr Gueye, Mr Pryslawsky, Dr Trigo, and Dr Le Foll), Alcohol Research and Treatment Clinic, Addiction Medicine Services, Ambulatory Care and Structured Treatments (Dr Le Foll), and Campbell Family Mental Health Research Institute (Dr Le Foll), Centre for Addiction and Mental Health, Toronto, ON, Canada; Department of Family and Community Medicine, Department of Pharmacology, and Department of Psychiatry, Division of Brain and Therapeutics, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Institute of Medical Sciences, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Department of Pharmacology, Faculty of Medicine, School of Health Sciences, University of Ioannina, Greece (Ms Poulia and Drs Delis and Antoniou); Department of Anatomy and Cell Biology, The Schulich School of Medicine and Dentistry, University of Western Ontario, London, ON, Canada (Drs Loureiro and Laviolette); Center for Drug Discovery, Department of Pharmaceutical Sciences and Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA (Drs Vemuri and Makriyannis).
Bernard Le FollTranslational Addiction Research Laboratory (Dr Gueye, Mr Pryslawsky, Dr Trigo, and Dr Le Foll), Alcohol Research and Treatment Clinic, Addiction Medicine Services, Ambulatory Care and Structured Treatments (Dr Le Foll), and Campbell Family Mental Health Research Institute (Dr Le Foll), Centre for Addiction and Mental Health, Toronto, ON, Canada; Department of Family and Community Medicine, Department of Pharmacology, and Department of Psychiatry, Division of Brain and Therapeutics, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Institute of Medical Sciences, University of Toronto, Toronto, ON, Canada (Dr Le Foll); Department of Pharmacology, Faculty of Medicine, School of Health Sciences, University of Ioannina, Greece (Ms Poulia and Drs Delis and Antoniou); Department of Anatomy and Cell Biology, The Schulich School of Medicine and Dentistry, University of Western Ontario, London, ON, Canada (Drs Loureiro and Laviolette); Center for Drug Discovery, Department of Pharmaceutical Sciences and Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA (Drs Vemuri and Makriyannis). Bernard.LeFoll@camh.ca.
University of Toronto · CAUniversity of Ioannina · GRCentre for Addiction and Mental Health · CAWestern University · CA
Funding
Cannabinergic Medications for Methamphetamine AddictionR37DA023142 · NIDA · NORTHEASTERN UNIVERSITY · PI MAKRIYANNIS, ALEXANDROS · 2007 to 2016
$7.1MCIHRNIDA NIH HHS R37 DA023142
Abstract
backgroundMultiple studies suggest a pivotal role of the endocannabinoid system in regulating the reinforcing effects of various substances of abuse. Rimonabant, a CB
methodsRats were trained to self-administer nicotine under a fixed-ratio 5 or progressive-ratio schedules of reinforcement. A control group was trained to self-administer food. The acute/chronic effects of AM4113 pretreatment were evaluated on nicotine taking, motivation for nicotine, and cue-, nicotine priming- and yohimbine-induced reinstatement of nicotine-seeking. The effects of AM4113 in the basal firing and bursting activity of midbrain dopamine neurons were evaluated in a separate group of animals treated with nicotine. Anxiety/depression-like effects of AM4113 and rimonabant were evaluated 24h after chronic (21 days) pretreatment (0, 1, 3, and 10mg/kg, 1/d).
resultsAM4113 significantly attenuated nicotine taking, motivation for nicotine, as well as cue-, priming- and stress-induced reinstatement of nicotine-seeking behavior. These effects were accompanied by a decrease of the firing and burst rates in the ventral tegmental area dopamine neurons in response to nicotine. On the other hand, AM4113 pretreatment did not have effects on operant responding for food. Importantly, AM4113 did not have effects on anxiety and showed antidepressant-like effects.
conclusionOur results indicate that AM4113 could be a promising therapeutic option for the prevention of relapse to nicotine-seeking while lacking anxiety/depression-like side effects.
Indexed as
Tobacco Use Cessation DevicesAnimalsAnxietyBehavior, AddictiveBehavior, AnimalCannabinoid Receptor AntagonistsCuesDepressionDisease Models, AnimalDopaminergic NeuronsDose-Response Relationship, DrugDrug Inverse AgonismDrug-Seeking BehaviorMaleMaze LearningMesencephalonAM4113Cannabinoid Receptor AntagonistsCnr1 protein, ratPiperidinesPyrazolesReceptor, Cannabinoid, CB1RimonabantanxietyCB1 antagonismdepressiondopaminenicotine reward
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