ArticleBehavioural pharmacology2015
Modulation of food consumption and sleep-wake cycle in mice by the neutral CB1 antagonist ABD459.
Article in Behavioural pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 23 citations in OpenAlex.
- Involvement of CB1R and CB2R Ligands in Sleep Disorders and Addictive Behaviors in the Last 25 Years.Pharmaceuticals (Basel, Switzerland) · 2025Review
- 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
- DMSO potentiates the suppressive effect of dronabinol on sleep apnea and REM sleep in rats.Journal of cannabis research · 2023Article
- Article
- Cannabinoids and Sleep/Wake Control.Advances in experimental medicine and biology · 2021Article
- Effects of Cannabinoid Agonists and Antagonists on Sleep in Laboratory Animals.Advances in experimental medicine and biology · 2021Review
- Measuring Behavior in the Home Cage: Study Design, Applications, Challenges, and Perspectives.Frontiers in behavioral neuroscience · 2021Article
- Additive effect of 5-HT2C and CB1 receptor blockade on the regulation of sleep-wake cycle.BMC neuroscience · 2019Article
- Overcoming the Psychiatric Side Effects of the Cannabinoid CB1 Receptor Antagonists: Current Approaches for Therapeutics Development.Current topics in medicinal chemistry · 2019Review
- AM-251, A Cannabinoid Antagonist, Modifies the Dynamics of Sleep-Wake Cycles in Rats.Frontiers in pharmacology · 2019Article
- Synopsis of arachidonic acid metabolism: A review.Journal of advanced research · 2018Review
- Effects of Cannabinoid Agonists and Antagonists on Sleep and Breathing in Sprague-Dawley Rats.Sleep · 2017Article
- Dose-dependent cannabis use, depressive symptoms, and FAAH genotype predict sleep quality in emerging adults: a pilot study.The American journal of drug and alcohol abuse · 2016Article
- Endocannabinoid Signaling Regulates Sleep Stability.PloS one · 2016Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 3 countries.
Funding
Abstract
The brain endocannabinoid system is a potential target for the treatment of psychiatric and metabolic conditions. Here, a novel CB1 receptor antagonist (ABD459) was synthesized and assayed for pharmacological efficacy in vitro and for modulation of food consumption, vigilance staging and cortical electroencephalography in the mouse. ABD459 completely displaced the CB1 agonist CP99540 at a Ki of 8.6 nmol/l, and did not affect basal, but antagonized CP55940-induced GTPγS binding with a KB of 7.7 nmol/l. Acute ABD459 (3-20 mg/kg) reliably inhibited food consumption in nonfasted mice, without affecting motor activity. Active food seeking was reduced for 5-6 h postdrug, with no rebound after washout. Epidural recording of electroencephalogram confirmed that ABD459 (3 mg/kg) robustly reduced rapid eye movement (REM) sleep, with no alterations of wakefulness or non-REM sleep. Effects were strongest during 3 h postdrug, followed by a progressive washout period. The CB1 antagonist AM251 (3 mg/kg) and agonist WIN-55,212-2 (WIN-2: 3 mg/kg) also reduced REM, but variously affected other vigilance stages. WIN-2 caused a global suppression of normalized spectral power. AM251 and ABD459 lowered delta power and increased power in the theta band in the hippocampus, but not the prefrontal cortex. The neutral antagonist ABD459 thus showed a specific role of endocannabinoid release in attention and arousal, possibly through modulation of cholinergic activity.
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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.