The DOI matches its Crossref record; 51 of the 51 references it cites were found in a registry or an index.
Dissociation between duration of action in the forced swim test in mice and nicotinic acetylcholine receptor occupancy with sazetidine, varenicline, and 5-I-A85380
Open accessAbstract
Rationale Nicotinic acetylcholine receptor (nAChR) agonists, partial agonists, and antagonists have antidepressant-like effects in rodents and reduce symptoms of depression in humans.Objectives The study determined whether the antidepressant-like effect of the nAChR β2* partial agonist sazetidine-A (sazetidine) in the forced swim test was due to activation or desensitization of β2* nAChRs. The study also determined if sazetidine's behavioral responses in the forced swim test corresponded to β2* nAChRs receptor occupancy and drug bioavailability.Results Acute antidepressant-like effects in the forced swim test were seen with sazetidine and the full β2* agonist 5-I-A8350 (BALB/cJ mice) and the less selective β2* partial agonist varenicline in C57BL/6J but not BALB/cJ mice. The role of β2* nAChRs was confirmed by results showing: (1) reversal of sazetidine's antidepressant-like effects in the forced swim test by nAChR antagonists mecamylamine and dihydro-β-erythroidine; (2) absence of sazetidine's effect in mice lacking the β2 subunit of the nAChR; and (3) a high correspondence between behaviorally active doses of sazetidine and β2* receptor occupancy. β2* receptor occupancy following acute sazetidine, varenicline, and 5-I-A8350 lasted beyond the duration of action in the forced swim test. Sazetidine's long lasting receptor occupancy did not diminish behavioral efficacy in the forced swim test following repeated dosing.Conclusions Results demonstrate that activation of a small population of β2* nAChRs (10-40%) is sufficient to elicit sazetidine's antidepressant-like actions without producing tolerance and suggest that ligands that activate β2* nAChRs would be promising targets for the development of a new class of antidepressant.
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“Both the antagonist mecamylamine (Rabenstein et al. 2006) and the partial agonist sazetidine (Caldarone et al. 2011), as well as the classical antidepressant amitriptyline (Caldarone et al. 2004), are ineffective in mice lacking the β2 subunit”
From Mechanisms of Nicotine Addiction (2021) · cites this paper as Caldarone et al. 2011
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“the effects of the partial agonist sazetidine could be blocked with mecamylamine (Caldarone et al. 2011)”
From Mechanisms of Nicotine Addiction (2021) · cites this paper as Caldarone et al. 2011
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“nicotinic partial agonists, that would be expected to decrease activity of acetylcholine at endogenous nAChRs when cholinergic tone is high but increase activity of nAChRs when cholinergic tone is low, are effective in mouse models of antidepressant efficacy (Mineur et al. 2007(Mineur et al. , 2009b(Mineur et al. , 2011a;;Rollema et al. 2009;Caldarone et al. 2011)”
From Mechanisms of Nicotine Addiction (2021) · cites this paper as Caldarone et al. 2011
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“both varenicline and sazetidine-A have shown antidepres- sant efficacy in the forced swim test (Caldarone et al, 2011; Kozikowski et al, 2009; Mineur et al, 2011; Rollema et al, 2009; Turner et al, 2010).”
From Divergent Functional Effects of Sazetidine-A and Varenicline During Nicotine Withdrawal (2013) · cites this paper as Caldarone et al, 2011
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“Therefore, these results may be due to differential effects of varenicline and sazetidine-A on nAChR activation and desensitization (Caldarone et al, 2011; Rollema et al, 2010; Xiao et al, 2006; Zwart et al, 2008).”
From Divergent Functional Effects of Sazetidine-A and Varenicline During Nicotine Withdrawal (2013) · cites this paper as Caldarone et al, 2011
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“in preclinical tests saz-A produces behavior indicative of potential antidepressant and/or antianxiety effects (Kozikowski et al., 2009;Turner et al., 2010Turner et al., , 2011;;Caldarone et al., 2011).”
From Chronic Sazetidine-A at Behaviorally Active Doses Does Not Increase Nicotinic Cholinergic Receptors in Rodent Brain (2012) · cites this paper as Caldarone et al., 2011
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“which agrees with a recent study that measured brain and blood concentrations of saz-A in mice after a single intraperitoneal injection (Caldarone et al., 2011).”
From Chronic Sazetidine-A at Behaviorally Active Doses Does Not Increase Nicotinic Cholinergic Receptors in Rodent Brain (2012) · cites this paper as Caldarone et al., 2011
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Self-citationVarenicline Is a Partial Agonist at α4β2 and a Full Agonist at α7 Neuronal Nicotinic Receptors
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Mechanisms of Nicotine Addiction
Picciotto, M. R., & Kenny, P. J. (2021) · Cold Spring Harbor Perspectives in Medicine · doi:10.1101/cshperspect.a039610 · Cited by 161
Self-citationNicotinic acetylcholine receptors in neurological and psychiatric diseases
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Divergent Functional Effects of Sazetidine-A and Varenicline During Nicotine Withdrawal
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Metadata
- Authors
- Caldarone, B. J., Wang, D., Paterson, N. E., Manzano, M., Fedolak, A., Cavino, K., Kwan, M., Hanania, T., Chellappan, S. K., Kozikowski, A. P., Olivier, B., Picciotto, M. R., & Ghavami, A.
- Affiliations
- Psychogenics (United States) (US)
- University of Illinois Chicago (US)
- Utrecht University (NL)
- Yale University (US)
- Corresponding author
- Caldarone, Barbara J.
- ORCID
- Venue
- Psychopharmacology
- Published
- 2011-04-13
- Volume
- 217
- Issue
- 2
- Pages
- 199-210
- ISSN
- 0033-3158 (ISSN-L)
- 1432-2072
- PMC
- PMC3266849
- OpenAlex
- W1968544134
- Cited by
- 47
- References
- 51
- Citations by year
- 2026: 1 · 2024: 1 · 2023: 1 · 2022: 1 · 2020: 2 · 2019: 2 · 2018: 2 · 2017: 1 · 2016: 3 · 2015: 6 · 2014: 7 · 2013: 4 · 2012: 12
- FWCI
- 4.29
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Psychopharmacology (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Institute of Mental Health (MH077681, MH085193, U19MH085193, R01MH077681)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Health Sciences › Medicine › Pharmacology (medical) › Treatment of Major Depression
- Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Smoking Behavior and Cessation
- Keywords
- nicotinic acetylcholine receptors, varenicline, antidepressant-like effects, forced swim test, receptor occupancy, receptor desensitization, mecamylamine, dihydro-beta-erythroidine, drug tolerance
- MeSH terms
- Varenicline, Animals, Antidepressive Agents, Azetidines, Behavior, Animal, Benzazepines, Brain, Data Interpretation, Statistical, Dose-Response Relationship, Drug, Ligands, Male, Mice, Inbred BALB C, Mice, Inbred C57BL, Motor Activity, Protein Binding, Pyridines, Quinoxalines, Receptors, Nicotinic, Swimming, Time Factors, Molecular Structure, Nicotinic Agonists, Mice
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