A comparison of brain and behavioral effects of varenicline and nicotine in rats

King, Jean A.; Huang, Wei; Chen, Wei; Heffernan, Meghan E.; Shields, Jessica; Rane, Pallavi; Bircher, Rhiannon; DiFranza, Joseph R.

doi:10.1016/j.bbr.2011.04.012

Cited by 15 publications

(36 citation statements)

References 32 publications

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“…Similar to the actions of selective α7-nAChR and α4β2-nAChR ligands, varenicline also facilitated cognitive flexibility in both vehicle- and ketamine-treated rats. The beneficial profile of varenicline in the current ASST study was in line with the previously demonstrated procognitive effects of this drug (King et al, 2011; Lange-Asschenfeldt et al, 2016; Rollema et al, 2009; Terry et al, 2016). For example, in the novel object recognition task, varenicline (0.32–3.2 mg/kg) improved rats’ recognition memory (Rollema et al, 2009).…”

Section: Discussionsupporting

confidence: 89%

“…The drug (3 mg/kg × 14 days) also prevented scopolamine-induced impairments in mice (Lange-Asschenfeldt et al, 2016). Moreover, the improvement in rats’ sustained attention (Rollema et al, 2009) and enhancement of spatial learning using the Morris Water Maze (King et al, 2011) were observed after varenicline treatment. Nevertheless, the preclinical efficacy of varenicline has not been widely assessed in conditions of schizophrenia-like cognitive decline.…”

Section: Discussionmentioning

confidence: 99%

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Procognitive effects of varenicline in the animal model of schizophrenia depend on α4β2- and α7-nicotinic acetylcholine receptors

et al. 2018

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Background: Varenicline, a partial agonist of the α4β2 nicotinic acetylcholine receptor (α4β2-nAChR), is currently used to facilitate smoking cessation. Preclinical and clinical studies have suggested that this compound may also be effective in treating cognitive impairments in schizophrenia. However, it is unclear which nicotinic acetylcholine receptor subtypes may be involved because varenicline is not only a partial agonist for α4β2-nAChRs but also a full agonist for α7 nicotinic acetylcholine receptors (α7-nAChRs). Aim: We investigated the effects of varenicline, compared to the α4β2-nAChR partial agonist TC-2403 and the α7-nAChR full agonist PNU-282987, in a ketamine-based model of schizophrenia-like cognitive deficits on the attentional set-shifting task in rats. The second goal was to elucidate whether the procognitive efficacy of varenicline was due to the compound’s action on α4β2-nAChRs or α7-nAChRs. Methods: Ketamine was administered to rats for 10 consecutive days and the test was performed 14 days following the last injection. The tested compounds were administered 30 min prior to the attentional set-shifting task. Results: Varenicline, TC-2403 and PNU-282987 ameliorated ketamine-evoked set-shifting deficits. While the α4β2-nAChR antagonist dihydro-β-erythroidine and the α7-nAChR antagonist methyllycaconitine completely prevented the procognitive actions of TC-2403 and PNU-282987, respectively, varenicline’s effect was only partially blocked by any given antagonist. Moreover, the combined treatment with TC-2403 and PNU-282987 more effectively facilitated rats’ set-shifting ability than activation of either type of nicotinic acetylcholine receptor alone. Conclusion: The present findings demonstrated that varenicline’s actions on both α7-nAChRs and α4β2-nAChRs may be necessary to produce its full procognitive effect in the present experimental setting.

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Section: Discussionsupporting

confidence: 89%

Section: Discussionmentioning

confidence: 99%

Procognitive effects of varenicline in the animal model of schizophrenia depend on α4β2- and α7-nicotinic acetylcholine receptors

et al. 2018

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“…Varenicline increased basal locomotor activity in rats [114]. Varenicline also enhanced the cognitive function of mice [115, 116] and rats [117]. Further, varenicline showed antidepressant-like activity [118], and anxiolytic effects [119].…”

Section: Discussionmentioning

confidence: 99%

Targeting the Cholinergic System to Develop a Novel Therapy for Huntington’s Disease

D’Souza

Waldvogel

2016

JHD

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In this review, we outline the role of the cholinergic system in Huntington’s disease, and briefly describe the dysfunction of cholinergic transmission, cholinergic neurons, cholinergic receptors and cholinergic survival factors observed in post-mortem human brains and animal models of Huntington’s disease. We postulate how the dysfunctional cholinergic system can be targeted to develop novel therapies for Huntington’s disease, and discuss the beneficial effects of cholinergic therapies in pre-clinical and clinical studies.

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“…In a subsequent study, varenicline, a partial agonist at the α4β2 nicotinic acetylcholine receptor used to treat nicotine addiction, was tested in awake rats, and was shown to produce a pattern of brain activity not unlike nicotine alone. However, repeated exposure to varenicline failed to cause the sensitization effect of nicotine ( King et al, 2011 ) evidence in support of varenicline’s therapeutic efficacy. Adolescent male rats chronically exposed to nicotine with or without menthol show differences in functional connectivity ( Thompson et al, 2018 ).…”

Section: Applicationsmentioning

confidence: 99%

Applications in Awake Animal Magnetic Resonance Imaging

Ferris

2022

Front. Neurosci.

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There are numerous publications on methods and applications for awake functional MRI across different species, e.g., voles, rabbits, cats, dogs, and rhesus macaques. Each of these species, most obviously rhesus monkey, have general or unique attributes that provide a better understanding of the human condition. However, much of the work today is done on rodents. The growing number of small bore (≤30 cm) high field systems 7T- 11.7T favor the use of small animals. To that point, this review is primarily focused on rodents and their many applications in awake function MRI. Applications include, pharmacological MRI, drugs of abuse, sensory evoked stimuli, brain disorders, pain, social behavior, and fear.

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A comparison of brain and behavioral effects of varenicline and nicotine in rats

Cited by 15 publications

References 32 publications

Procognitive effects of varenicline in the animal model of schizophrenia depend on α4β2- and α7-nicotinic acetylcholine receptors

Procognitive effects of varenicline in the animal model of schizophrenia depend on α4β2- and α7-nicotinic acetylcholine receptors

Targeting the Cholinergic System to Develop a Novel Therapy for Huntington’s Disease

Applications in Awake Animal Magnetic Resonance Imaging

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