ArticleThe Journal of pharmacology and experimental therapeutics2011
Patterns of nicotinic receptor antagonism: nicotine discrimination studies.
Article in The Journal of pharmacology and experimental therapeutics, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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Who cites it
43 citing papers in PubMed, 49 citations in OpenAlex.
- Discriminative stimulus and locomotor activity profiles of nicotine and varenicline.Pharmacology, biochemistry, and behavior · 2026Article
- The effects of chronic neuropathic pain states on the discriminative stimulus effect of fentanyl and other MOR agonists.bioRxiv : the preprint server for biology · 2024Article
- Assessment of Abuse-Related Discriminative Stimulus Effects of Nicotine Aerosol in Rodents.The Journal of pharmacology and experimental therapeutics · 2023Article
- Nicotinic aspects of the discriminative stimulus effects of arecoline.Behavioural pharmacology · 2021Article
- Pharmacological Comparison of Mitragynine and 7-Hydroxymitragynine: In Vitro Affinity and Efficacy forThe Journal of pharmacology and experimental therapeutics · 2021Article
- The discriminative stimulus effects of epibatidine in C57BL/6J mice.Behavioural pharmacology · 2020Article
- Comparison of the muscarinic antagonist effects of scopolamine and L-687,306.Behavioural pharmacology · 2020Article
- More than Smoke and Patches: The Quest for Pharmacotherapies to Treat Tobacco Use Disorder.Pharmacological reviews · 2020Review
- Unexpected loss of sensitivity to the nicotinic acetylcholine receptor antagonist activity of mecamylamine and dihydro-β-erythroidine in nicotine-tolerant mice.Brain and behavior · 2020Article
- Differential cross-tolerance to the effects of nicotinic acetylcholine receptor drugs in C57BL/6J mice following chronic varenicline.Behavioural pharmacology · 2019Article
- Exploring the interoceptive stimulus effects of nicotine and varenicline.Pharmacology, biochemistry, and behavior · 2019Article
- Discriminative stimulus effects of mecamylamine and nicotine in rhesus monkeys: Central and peripheral mechanisms.Pharmacology, biochemistry, and behavior · 2019Article
- Green tobacco sickness: mecamylamine, varenicline, and nicotine vaccine as clinical research tools and potential therapeutics.Expert review of clinical pharmacology · 2019Review
- Rapid nicotine tolerance and cross-tolerance to varenicline in rhesus monkeys: Drug discrimination.Experimental and clinical psychopharmacology · 2018Article
- Role of trace amine-associated receptor 1 in nicotine's behavioral and neurochemical effects.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2018Article
- Involvement of Nicotinic Receptor Subtypes in the Behavioral Effects of Nicotinic Drugs in Squirrel Monkeys.The Journal of pharmacology and experimental therapeutics · 2018Article
- In vivo effects of μ-opioid receptor agonist/δ-opioid receptor antagonist peptidomimetics following acute and repeated administration.British journal of pharmacology · 2018Article
- Nicotine drug discrimination and nicotinic acetylcholine receptors in differentially reared rats.Psychopharmacology · 2018Article
- GABAergic Neurons as Putative Neurochemical Substrate Mediating Aversive Effects of Nicotine.Journal of alcoholism and drug dependence · 2018Article
- Nicotine as a discriminative stimulus for ethanol use.Drug and alcohol dependence · 2018Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
Evaluation of the discriminative stimulus effects of drugs is a useful procedure for identification of receptor mediation of in vivo drug effects. This assay can be enhanced when the stimulus effects of different doses of agonist are evaluated. In the present study, rats were trained to discriminate small or large doses of nicotine from saline, and interactions of these effects with nicotinic receptor antagonists and partial agonists were determined. The insurmountable nicotine antagonist mecamylamine blocked both the discriminative stimulus and response rate-reducing effects of nicotine but was less effective against the large dose of nicotine. The α4β2*-selective, competitive antagonist dihydro-β-erythrodine (DHβE) antagonized the discriminative stimulus effects of both doses but was less effective against the larger training dose of nicotine. Schild analyses of DHβE suggested that different nicotinic receptor populations may be mediating the stimulus effects of large and small doses of nicotine. This suggestion was supported by observations that the discriminative stimulus effects of the partial agonist cytisine were more like those of the large dose than of the small dose of nicotine and that cytisine antagonized the effects of only the small nicotine dose. Varenicline produced nicotine-like effects in both training dose groups but reduced the discriminative stimulus effects of intermediate doses of nicotine in the group trained to the small dose of nicotine. Overall, these results suggest that small doses of nicotine produce their stimulus effects via α4β2* nicotine receptors, whereas larger doses of nicotine recruit additional nicotine receptor subtypes, as revealed by drug discrimination assays in rats.
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