ArticlePsychopharmacology2010
Discriminative stimulus functions of methanandamide and delta(9)-THC in rats: tests with aminoalkylindoles (WIN55,212-2 and AM678) and ethanol.
Article in Psychopharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- Discriminating evidence - use and misuse of the drug-discrimination test in abuse potential assessment of novel CNS drugs.Journal of psychopharmacology (Oxford, England) · 2025Review
- A critical assessment of the abuse, dependence and associated safety risks of naturally occurring and synthetic cannabinoids.Frontiers in psychiatry · 2024Review
- Molecular and Behavioral Pharmacological Characterization of Abused Synthetic Cannabinoids MMB- and MDMB-FUBINACA, MN-18, NNEI, CUMYL-PICA, and 5-Fluoro-CUMYL-PICA.The Journal of pharmacology and experimental therapeutics · 2018Article
- Discriminative Stimulus Properties of Phytocannabinoids, Endocannabinoids, and Synthetic Cannabinoids.Current topics in behavioral neurosciences · 2018Review
- Tripping with Synthetic Cannabinoids ("Spice"): Anecdotal and Experimental Observations in Animals and Man.Current topics in behavioral neurosciences · 2017Review
- Ketamine and MAG Lipase Inhibitor-Dependent Reversal of Evolving Depressive-Like Behavior During Forced Abstinence From Alcohol Drinking.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2016Article
- Preclinical studies on the reinforcing effects of cannabinoids. A tribute to the scientific research of Dr. Steve Goldberg.Psychopharmacology · 2016Review
- [INCREMENT]9-Tetrahydrocannabinol discriminative stimulus effects of AM2201 and related aminoalkylindole analogs in rats.Behavioural pharmacology · 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
- JWH-018 in rhesus monkeys: differential antagonism of discriminative stimulus, rate-decreasing, and hypothermic effects.European journal of pharmacology · 2014Article
- Cross-substitution of Δ9-tetrahydrocannabinol and JWH-018 in drug discrimination in rats.Pharmacology, biochemistry, and behavior · 2014Article
- Synthetic Cannabinoids: Pharmacology, Behavioral Effects, and Abuse Potential.Current addiction reports · 2014Article
- "Herbal incense": designer drug blends as cannabimimetics and their assessment by drug discrimination and other in vivo bioassays.Life sciences · 2014Review
- Distinct pharmacology and metabolism of K2 synthetic cannabinoids compared to Δ(9)-THC: mechanism underlying greater toxicity?Life sciences · 2014Review
- Differentiation between low- and high-efficacy CB1 receptor agonists using a drug discrimination protocol for rats.Psychopharmacology · 2014Article
- JWH-018 and JWH-073: Δ⁹-tetrahydrocannabinol-like discriminative stimulus effects in monkeys.The Journal of pharmacology and experimental therapeutics · 2012Article
- Endocannabinoid influence in drug reinforcement, dependence and addiction-related behaviors.Pharmacology & therapeutics · 2011Review
- Cannabinergic aminoalkylindoles, including AM678=JWH018 found in 'Spice', examined using drug (Δ(9)-tetrahydrocannabinol) discrimination for rats.Behavioural pharmacology · 2011Article
- Central mediation and differential blockade by cannabinergics of the discriminative stimulus effects of the cannabinoid CB1 receptor antagonist rimonabant in rats.Psychopharmacology · 2011Article
- The endogenous cannabinoid anandamide shares discriminative stimulus effects with ∆(9)-tetrahydrocannabinol in fatty acid amide hydrolase knockout mice.European journal of pharmacology · 2011Article
Corrections and comments
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Authors and funding
4 authors.
Funding
Abstract
objectiveThe aim of the study was to characterize in vivo the aminoalkylindoles WIN55,212-2 (WIN) and AM678 (naphthalen-1-yl(1-pentyl-1H-indol-3-yl)methanone) as cannabinoid receptor (CB(1)R) ligands using drug discrimination. Tests also involved delta(9)-tetrahydrocannabinol (THC) and R-(+)-methanandamide (mAEA), a metabolically stable analog of the endogenous ligand anandamide, as well as the CB(1)R selective antagonist/inverse agonist rimonabant; tests with ethanol assessed pharmacological specificity. We used two different drug discriminations (mAEA and THC) allowing us to explore potential differences in CB(1)R activation which could be attributed to variations in their respective CB(1)R signaling mechanisms.
methodsThere were two concurrently trained groups of rats. One group discriminated between i.p. injected vehicle and 10 mg/kg mAEA. The other group was trained to discriminate between vehicle and 1.8 mg/kg THC.
resultsDose generalization curves for AM678, WIN55,212-2, THC, and mAEA suggested the following rank order of potency: AM678 > WIN55,212-2 > or = THC > mAEA in both drug discrimination groups. Challenge by 1 mg/kg rimonabant resulted in shifts to the right of the generalization curves for the two aminoalkylindoles (4.4-fold for AM678 and 11.3-fold for WIN in the mAEA group, whereas for the THC group, the corresponding values were 13 and 2.6, respectively), suggesting surmountable antagonism. Ethanol did not generalize in either of the two groups, suggesting pharmacological specificity.
conclusionData are congruent with the general observation that there is substantial overlap in the discriminative stimulus effects of CB(1)R ligands across different chemical classes. However, the quantitative differences in the interactions between the two aminoalkylindoles and rimonabant in the two discrimination groups suggest subtle variations in the ligand-receptor activation(s).
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