ArticlePsychopharmacology2007
Ligands selective for alpha4beta2 but not alpha3beta4 or alpha7 nicotinic receptors generalise to the nicotine discriminative stimulus in the rat.
Article in Psychopharmacology, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 52 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
52 citing papers in PubMed, 93 citations in OpenAlex.
- Discriminative stimulus and locomotor activity profiles of nicotine and varenicline.Pharmacology, biochemistry, and behavior · 2026Article
- Evidence for AlphaThe Journal of pharmacology and experimental therapeutics · 2022Article
- The importance of acquisition learning on nicotine and varenicline drug substitution in a drug-discriminated goal-tracking task.Pharmacology, biochemistry, 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
- Nicotine drug discrimination and nicotinic acetylcholine receptors in differentially reared rats.Psychopharmacology · 2018Article
- Nicotine- and cocaine-triggered methamphetamine reinstatement in female and male Sprague-Dawley rats.Pharmacology, biochemistry, and behavior · 2017Article
- The contribution of α4β2 and non-α4β2 nicotinic acetylcholine receptors to the discriminative stimulus effects of nicotine and varenicline in mice.Psychopharmacology · 2017Article
- The effect of sazetidine-A and other nicotinic ligands on nicotine controlled goal-tracking in female and male rats.Neuropharmacology · 2017Article
- Attenuated nicotine-like effects of varenicline but not other nicotinic ACh receptor agonists in monkeys receiving nicotine daily.British journal of pharmacology · 2016Article
- Adolescent alcohol exposure decreased sensitivity to nicotine in adult Wistar rats.Addiction biology · 2016Article
- The effects of varenicline on methamphetamine self-administration and drug-primed reinstatement in female rats.Behavioural brain research · 2016Article
- Repeated administration of an acetylcholinesterase inhibitor attenuates nicotine taking in rats and smoking behavior in human smokers.Translational psychiatry · 2016Article
- The effect of switching pharmacological intervention during extinction on nicotine-evoked conditioned responding in rats.Psychopharmacology · 2015Article
- Evaluation of the cardiovascular effects of varenicline in rats.Drug design, development and therapy · 2015Article
- The cytisine derivatives, CC4 and CC26, reduce nicotine-induced conditioned place preference in zebrafish by acting on heteromeric neuronal nicotinic acetylcholine receptors.Psychopharmacology · 2014Article
- Donepezil, an acetylcholinesterase inhibitor, attenuates nicotine self-administration and reinstatement of nicotine seeking in rats.Addiction biology · 2014Article
- Effects of chronic varenicline treatment on nicotine, cocaine, and concurrent nicotine+cocaine self-administration.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2014Article
- Methamphetamine-like discriminative-stimulus effects of nicotinic agonists.The Journal of pharmacology and experimental therapeutics · 2014Article
- Discriminative-stimulus effects of NS9283, a nicotinic α4β2* positive allosteric modulator, in nicotine-discriminating rats.Psychopharmacology · 2014Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
rationaleNicotine produces behavioural effects that are potentially related to its interaction with diverse nicotinic acetylcholine receptor populations. Evidence from gene deletion studies suggests that the interoceptive stimulus properties of nicotine are mediated by heteromeric high-affinity receptors containing alpha4beta2 subunits. Mice lacking beta2 subunits do not discriminate nicotine (Shoaib et al., Neuropharmacology, 42:530-539, 2002), and nicotine does not elicit dopamine release in these animals (Grady et al., J Neurochem, 76:258-268, 2001). The stimulus properties of nicotine can be detected in rats using a two-lever operant drug discrimination paradigm, allowing them to be classified pharmacologically using ligands with selectivity for receptors containing alpha4beta2, alpha3beta4 or alpha7 subunits. MATERIALS AND
methodsRats trained to discriminate 0.4 mg/kg nicotine from vehicle were given the nicotinic receptor agonists, cytisine, varenicline, TC2559, ABT-594, A-85380 (all having high affinity but varying selectivity for alpha4beta2-containing receptors), and WO 03/062224 and WO 01/60821A1 (selective for beta4- and alpha7-containing receptors, respectively). In separate studies, WO 03/062224 was used as the training stimulus.
resultsNicotine, TC-2559, A-85380 and ABT-594 showed dose-dependent and complete stimulus substitution, whilst WO 03/062224 and WO 01/60821A1 were completely without effect. Cytisine and varenicline showed partial generalisation, consistent with their partial agonist activity at nicotinic receptors eliciting dopamine release in rat striatal slices. After almost 50 training sessions with WO 03/062224, there was no clear evidence that an alpha3beta4 receptor agonist could sustain a discriminable stimulus.
conclusionSubstitution to the nicotine discriminative stimulus required high-affinity and high intrinsic activity at beta2 but not at beta4- or at alpha7-containing nicotinic receptors.
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