ArticleThe Journal of pharmacology and experimental therapeutics2013
Cannabinoid discrimination and antagonism by CB(1) neutral and inverse agonist antagonists.
Article in The Journal of pharmacology and experimental therapeutics, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers, 1 of them a synthesis that pooled it.
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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
34 citing papers in PubMed, 1 synthesis or guideline pooled it, 46 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
- Neural effects of cannabinoid CB1 neutral antagonist tetrahydrocannabivarin on food reward and aversion in healthy volunteers.The international journal of neuropsychopharmacology · 2014Trial
- Pharmacotherapy for Cannabis Use Disorder: Preclinical and Clinical Models.Current topics in behavioral neurosciences · 2026Review
- Chronic ΔNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2025Article
- Effects of cannabinoid agonists and antagonists in male rats discriminating the synthetic cannabinoid AM2201.European journal of pharmacology · 2023Article
- Rimonabant-Based Compounds Bearing Hydrophobic Amino Acid Derivatives as Cannabinoid Receptor Subtype 1 Ligands.ACS medicinal chemistry letters · 2023Article
- Review
- Antiemetic Effects of Cannabinoid Agonists in Nonhuman Primates.The Journal of pharmacology and experimental therapeutics · 2020Article
- Cannabinoid Antagonist Drug Discrimination in Nonhuman Primates.The Journal of pharmacology and experimental therapeutics · 2020Article
- Review
- Cannabinoid CBActa pharmacologica Sinica · 2019Article
- Overcoming the Psychiatric Side Effects of the Cannabinoid CB1 Receptor Antagonists: Current Approaches for Therapeutics Development.Current topics in medicinal chemistry · 2019Review
- Cannabinoid-1 receptor neutral antagonist reduces binge-like alcohol consumption and alcohol-induced accumbal dopaminergic signaling.Neuropharmacology · 2018Article
- Long-Lasting In Vivo Effects of the Cannabinoid CB1 Antagonist AM6538.The Journal of pharmacology and experimental therapeutics · 2018Article
- Cannabinoid CBThe Journal of pharmacology and experimental therapeutics · 2017Article
- Synthetic Pot: Not Your Grandfather's Marijuana.Trends in pharmacological sciences · 2017Review
- Metabolic Profiling of CB1 Neutral Antagonists.Methods in enzymology · 2017Article
- The CB1 Neutral Antagonist AM4113 Retains the Therapeutic Efficacy of the Inverse Agonist Rimonabant for Nicotine Dependence and Weight Loss with Better Psychiatric Tolerability.The international journal of neuropsychopharmacology · 2016Article
- Drug Discrimination and the Analysis of Private Events.Behavior analysis (Washington, D.C.) · 2016Article
- A high efficacy cannabinergic ligand (AM4054) used as a discriminative stimulus: Generalization to other adamantyl analogs and Δ(9)-THC in rats.Pharmacology, biochemistry, and behavior · 2016Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
Abstract
Cannabinoid receptor 1 (CB(1)) inverse agonists (e.g., rimonabant) have been reported to produce adverse effects including nausea, emesis, and anhedonia that limit their clinical applications. Recent laboratory studies suggest that the effects of CB(1) neutral antagonists differ from those of such inverse agonists, raising the possibility of improved clinical utility. However, little is known regarding the antagonist properties of neutral antagonists. In the present studies, the CB(1) inverse agonist SR141716A (rimonabant) and the CB(1) neutral antagonist AM4113 were compared for their ability to modify CB(1) receptor-mediated discriminative stimulus effects in nonhuman primates trained to discriminate the novel CB(1) full agonist AM4054. Results indicate that AM4054 serves as an effective CB(1) discriminative stimulus, with an onset and time course of action comparable with that of the CB(1) agonist Δ(9)-tetrahydrocannabinol, and that the inverse agonist rimonabant and the neutral antagonist AM4113 produce dose-related rightward shifts in the AM4054 dose-effect curve, indicating that both drugs surmountably antagonize the discriminative stimulus effects of AM4054. Schild analyses further show that rimonabant and AM4113 produce highly similar antagonist effects, as evident in comparable pA(2) values (6.9). Taken together with previous studies, the present data suggest that the improved safety profile suggested for CB(1) neutral antagonists over inverse agonists is not accompanied by a loss of antagonist action at CB(1) receptors.
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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.