ArticlePsychopharmacology2014
Differentiation between low- and high-efficacy CB1 receptor agonists using a drug discrimination protocol for rats.
Article in Psychopharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- Indazole partial agonists targeting peripheral cannabinoid receptors.Bioorganic & medicinal chemistry · 2025Article
- Investigation of Cannabidiol in the Mouse Drug Discrimination Paradigm.Cannabis and cannabinoid research · 2024Article
- A critical assessment of the abuse, dependence and associated safety risks of naturally occurring and synthetic cannabinoids.Frontiers in psychiatry · 2024Review
- Effects of cannabinoid agonists and antagonists in male rats discriminating the synthetic cannabinoid AM2201.European journal of pharmacology · 2023Article
- Discovery of 1,3-disubstituted pyrazole peripheral cannabinoid receptor partial agonists.Bioorganic & medicinal chemistry letters · 2023Article
- Structure-Activity Relationship Development Efforts towards Peripherally Selective Analogs of the Cannabinoid Receptor Partial Agonist BAY 59-3074.Molecules (Basel, Switzerland) · 2022Article
- Molecular Mechanism and Cannabinoid Pharmacology.Handbook of experimental pharmacology · 2020Article
- Discriminative Stimulus Properties of Phytocannabinoids, Endocannabinoids, and Synthetic Cannabinoids.Current topics in behavioral neurosciences · 2018Review
- Cannabinoid CBThe Journal of pharmacology and experimental therapeutics · 2017Article
- Apparent CBThe Journal of pharmacology and experimental therapeutics · 2017Article
- Comparison of the discriminative stimulus and response rate effects ofDrug and alcohol dependence · 2017Article
- 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
- Baths salts, spice, and related designer drugs: the science behind the headlines.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2014Review
- Synthetic cannabinoids: epidemiology, pharmacodynamics, and clinical implications.Drug and alcohol dependence · 2014Review
- Cross-substitution of Δ9-tetrahydrocannabinol and JWH-018 in drug discrimination in rats.Pharmacology, biochemistry, and behavior · 2014Article
- Human Drug Discrimination: Elucidating the Neuropharmacology of Commonly Abused Illicit Drugs.Current topics in behavioral neurosciencesReview
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
rationaleThe "subjective high" from marijuana ingestion is likely due to Δ(9)-tetrahydrocannabinol (THC) activating the central cannabinoid receptor type 1 (CB1R) of the endocannabinoid signaling system. THC is a weak partial agonist according to in vitro assays, yet THC mimics the behavioral effects induced by more efficacious cannabinergics. This distinction may be important for understanding similarities and differences in the dose-effect spectra produced by marijuana/THC and designer cannabimimetics ("synthetic marijuana").
objectiveWe evaluated if drug discrimination is able to functionally detect/differentiate between a full, high-efficacy CB1R agonist [(±)AM5983] and the low-efficacy agonist THC in vivo. MATERIALS AND
methodsRats were trained to discriminate between four different doses of AM5983 (0.10 to 0.56 mg/kg), and vehicle and dose generalization curves were determined for both ligands at all four training doses of AM5983. The high-efficacy WIN55,212-2 and the lower-efficacy (R)-(+)-methanandamide were examined at some AM5983 training conditions. Antagonism tests involved rimonabant and WIN55,212-2 and AM5983. The separate (S)- and (R)-isomers of (±)AM5983 were tested at one AM5983 training dose (0.30 mg/kg). The in vitro cyclic adenosine monophosphate (cAMP) assay examined AM5983 and the known CB1R agonist CP55,940.
resultsDose generalization ed50 values increased as a function of the training dose of AM5983, but more so for the partial agonists. The order of potency was (R)-isomer > (±)AM5983 > (S)-isomer and AM5983 > WIN55,212-2 ≥ THC > (R)-(+)-methanandamide. Surmountable antagonism of AM5983 and WIN55,212-2 occurred with rimonabant. The cAMP assay confirmed the cannabinergic nature of AM5983 and CP55,940.
conclusionsDrug discrimination using different training doses of a high-efficacy, full CB1R agonist differentiated between low- and high-efficacy CB1R agonists.
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