Sazetidine-A Is a Potent and Selective Agonist at Native and Recombinant α4β2 Nicotinic Acetylcholine Receptors

Zwart, Ruud; Carbone, Anna L.; Moroni, Mirko; Bermudez, Isabel; Mogg, Adrian J.; Folly, Elizabeth A.; Broad, Lisa M.; Williams, Andrew C.; Zhang, Deyi; Ding, Chunjin; Heinz, Beverly A.; Sher, Emanuele

doi:10.1124/mol.108.045104

Cited by 120Nicotinic Acetylcholine Receptors StudyNeuroscience and Neuropharmacology ResearchReceptor Mechanisms and Signaling

Sazetidine-A Is a Potent and Selective Agonist at Native and Recombinant α4β2 Nicotinic Acetylcholine Receptors

Zwart, Ruud, Carbone, Anna L., Moroni, Mirko, Bermudez, Isabel, Mogg, Adrian J., Folly, Elizabeth A., Broad, Lisa M., Williams, Andrew C. +4 more·2008·Molecular Pharmacology

DOI 10.1124/mol.108.045104

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Abstract

Sazetidine-A has been recently proposed to be a "silent desensitizer" of alpha4beta2 nicotinic acetylcholine receptors (nAChRs), implying that it desensitizes alpha4beta2 nAChRs without first activating them. This unusual pharmacological property of sazetidine-A makes it, potentially, an excellent research tool to distinguish between the role of activation and desensitization of alpha4beta2 nAChRs in mediating the central nervous system effects of nicotine itself, as well as those of new nicotinic drugs. We were surprised to find that sazetidine-A potently and efficaciously stimulated nAChR-mediated dopamine release from rat striatal slices, which is mediated by alpha4beta2(*) and alpha6beta2(*) subtypes of nAChR. The agonist effects on native striatal nAChRs prompted us to re-examine the effects of sazetidine-A on recombinant alpha4beta2 nAChRs in more detail. We expressed the two alternative stoichiometries of alpha4beta2 nAChR in Xenopus laevis oocytes and investigated the agonist properties of sazetidine-A on both alpha4(2)beta2(3) and alpha4(3)beta2(2) nAChRs. We found that sazetidine-A potently activated both stoichiometries of alpha4beta2 nAChR: it was a full agonist on alpha4(2)beta2(3) nAChRs, whereas it had an efficacy of only 6% on alpha4(3)beta2(2) nAChRs. In contrast to what has been published before, we therefore conclude that sazetidine-A is an agonist of native and recombinant alpha4beta2 nAChRs but shows differential efficacy on alpha4beta2 nAChRs subtypes.

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Sazetidine-A quickly and thoroughly desensitizes the receptor after brief partial agonism.
“Sazetidine-A is a recently developed nicotinic compound with high affinity and selectivity for a4b2 nAChRs, but not a3b4 or a7 nAChRs (Xiao et al, 2006), that quickly and thoroughly desensitizes the receptor after brief partial agonism (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 Zwart et al, 2008
Low concentrations of sazetidine-A profoundly desensitize α4β2 nAChRs for prolonged periods.
“In vitro studies show that low concentrations of sazetidine-A profoundly desensitize a4b2 nAChRs for prolonged periods (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 Zwart et al, 2008
Sazetidine-A binds with very low affinity to all other nicotinic receptor subtypes.
“A newly developed nicotinic partial agonist, sazetidine-A, potently and selectively desensitizes ␣4␤2 nicotinic acetylcholine receptors (Xiao et al., 2006), but it has very low affinities for all other nAChR subtypes (Xiao et al., 2006;Zwart et al., 2008).”
From Nicotinic Partial Agonists Varenicline and Sazetidine-A Have Differential Effects on Affective Behavior (2010) · cites this paper as Zwart et al., 2008
Saz-A is a partial agonist at α4β2 nAChRs that may show differential efficacy depending on receptor stoichiometry.
“Sazetidine-A [saz-A; 6-(5-(((S)-azetidin-2-yl)methoxy)pyridin-3-yl)hex-5-yn-l-ol] is a partial agonist at ␣4␤2 nAChRs that may show differential efficacy at this receptor subtype depending on the stoichiometry (Zwart et al., 2008).”
From Chronic Sazetidine-A at Behaviorally Active Doses Does Not Increase Nicotinic Cholinergic Receptors in Rodent Brain (2012) · cites this paper as Zwart et al., 2008

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AE Succinimide, an Analogue of Methyllycaconitine, When Bound Generates a Nonconducting Conformation of the α4β2 Nicotinic Acetylcholine Receptor
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Oral sazetidine-A, a selective α4β2* nicotinic receptor desensitizing agent, reduces nicotine self-administration in rats
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Sazetidine-A, A Novel Ligand That Desensitizes α4β2 Nicotinic Acetylcholine Receptors without Activating Them
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Sazetidine-A Is a Potent and Selective Agonist at Native and
Nicotinic, R., Receptors, A., Zwart, R., Carbone, A. L., Moroni, M., Bermúdez, I., Mogg, A. J., Folly, E. A., Broad, L. M., Williams, A. C., et al. (2008)
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Sazetidine-A, A Novel Ligand That Desensitizes 42 Nicotinic Acetylcholine Receptors without Activating Them
Xiao, Y., Fan, H., Musachio, J. L., Wei, Z.-L., Kozikowski, A. P., & Kellar, K. J. (2006)
Corresponding author:
Nicotinic, R., Receptors, A., Zwart, R., Carbone, A. L., Moroni, M., Bermúdez, I., Mogg, A. J., Folly, E. A., Broad, L. M., Williams, A. C., et al. (2013)
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Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors
Brown, J. L., & Wonnacott, S. (2014) · Neurochemical Research · doi:10.1007/s11064-014-1302-6 · Cited by 7 · see citing works

Authors: Zwart, R., Carbone, A. L., Moroni, M., Bermudez, I., Mogg, A. J., Folly, E. A., Broad, L. M., Williams, A. C., Zhang, D., Ding, C., Heinz, B. A., & Sher, E.
Affiliations: Eli Lilly (United Kingdom) (GB)
ORCID: Carbone, Anna L.
Moroni, Mirko
Mogg, Adrian J.
Zhang, Deyi
Sher, Emanuele
Venue: Molecular Pharmacology
Publisher: Elsevier BV
Published: 2008-06
Volume: 73
Issue: 6
Pages: 1838-1843
ISSN: 0026-895X (ISSN-L)
DOI: 10.1124/mol.108.045104
OpenAlex: W1982378333
Cited by: 111
References: 37
Citations by year: 2026: 3 · 2025: 2 · 2024: 1 · 2023: 2 · 2022: 6 · 2021: 5 · 2020: 7 · 2019: 3 · 2018: 5 · 2017: 2 · 2016: 12 · 2015: 10 · 2014: 15 · 2013: 11 · 2012: 7
FWCI: 2.74
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
Locations: Molecular Pharmacology (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Keywords: α4β2 nicotinic acetylcholine receptor, nicotinic agonists, receptor stoichiometry, striatal dopamine release
MeSH terms: Animals, Azetidines, Cell Line, Dose-Response Relationship, Drug, Female, Humans, Male, Pyridines, Receptors, Nicotinic, Recombinant Proteins, Xenopus laevis, Nicotinic Agonists, Rats

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Sazetidine-A Is a Potent and Selective Agonist at Native and Recombinant α4β2 Nicotinic Acetylcholine Receptors

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