ArticlePsychopharmacology2012
Effects of the specific α4β2 nAChR antagonist, 2-fluoro-3-(4-nitrophenyl) deschloroepibatidine, on nicotine reward-related behaviors in rats and mice.
Article in Psychopharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 22 citations in OpenAlex.
- Bupropion increases activation in nucleus accumbens during anticipation of monetary reward.Psychopharmacology · 2019Trial
- Treatment for tobacco dependence: effect on brain nicotinic acetylcholine receptor density.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2013Trial
- Isolation and characterization of five novel disulfide-poor conopeptides fromThe journal of venomous animals and toxins including tropical diseases · 2022Article
- Nicotine-induced enhancement of a sensory reinforcer in adult rats: antagonist pretreatment effects.Psychopharmacology · 2021Article
- Highly Selective and Potent α4β2 nAChR Antagonist Inhibits Nicotine Self-Administration and Reinstatement in Rats.Journal of medicinal chemistry · 2017Article
- Comparison of effects produced by nicotine and the α4β2-selective agonist 5-I-A-85380 on intracranial self-stimulation in rats.Experimental and clinical psychopharmacology · 2016Article
- Discriminative stimulus and hypothermic effects of some derivatives of the nAChR agonist epibatidine in mice.Psychopharmacology · 2014Article
- Involvement of neuronal β2 subunit-containing nicotinic acetylcholine receptors in nicotine reward and withdrawal: implications for pharmacotherapies.Journal of clinical pharmacy and therapeutics · 2014Review
- Intracranial self-stimulation to evaluate abuse potential of drugs.Pharmacological reviews · 2014Review
- Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues.Journal of medicinal chemistry · 2014Article
- Nicotinic receptor modulation to treat alcohol and drug dependence.Frontiers in neuroscience · 2014Review
- Effects of blockade of α4β2 and α7 nicotinic acetylcholine receptors on cue-induced reinstatement of nicotine-seeking behaviour in rats.The international journal of neuropsychopharmacology · 2014Article
- Iptakalim attenuates self-administration and acquired goal-tracking behavior controlled by nicotine.Neuropharmacology · 2013Article
- Synthesis and nicotinic acetylcholine receptor in vitro and in vivo pharmacological properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues of 2'-fluoro-3'-(4-nitrophenyl)deschloroepibatidine.Journal of medicinal chemistry · 2012Article
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
Abstract
rationaleAlleviating addiction to tobacco products could prevent millions of deaths. Investigating novel compounds selectively targeting α4β2 nAChRs hypothesized to have a key role in the rewarding effects of nicotine may be a useful approach for future treatment.
objectivesThe present study was designed to evaluate 2-fluoro-3-(4-nitrophenyl) deschloroepibatidine (4-nitro-PFEB), a potent competitive antagonist of neuronal α4β2 nAChRs, in several animal models related to nicotine reward: drug discrimination, intracranial self-stimulation (ICSS), conditioned place preference, and limited access to self-administration.
methodsLong Evans rats were trained in a two-lever discrimination procedure to discriminate 0.4 mg/kg nicotine (s.c.) from saline. Male Sprague-Dawley rats were stereotaxically implanted with electrodes and trained to respond for direct electrical stimulation of the medial forebrain bundle. ICR mice were evaluated using an unbiased place preference paradigm, and finally, male Wistar rats were implanted with intrajugular catheters and tested for nicotine self-administration under limited access (1 h/day).
results4-Nitro-PFEB attenuated the discriminative stimulus effects of nicotine, but alone did not produce nicotine-like discriminative stimulus effects. Nicotine-induced facilitation of ICSS reward thresholds was reversed by 4-nitro-PFEB, which alone had no effect on thresholds. 4-Nitro-PFEB also blocked the conditioned place preference produced by nicotine, but alone had no effect on conditioned place preference. Finally, 4-nitro-PFEB dose-dependently decreased nicotine self-administration.
conclusionsThese results support the hypothesis that neuronal α4β2 nAChRs play a key role in mediating the rewarding effects of nicotine and further suggest that targeting α4β2 nAChRs may yield a potential candidate for the treatment of nicotine dependence.
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