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Varenicline Is a Partial Agonist at α4β2 and a Full Agonist at α7 Neuronal Nicotinic Receptors
Abstract
Varenicline, a new nicotinic ligand based on the structure of cytisine, has recently been approved by the U.S. Food and Drug Administration for use as a smoking cessation aid. Varenicline has been shown to be a partial agonist of alpha4beta2 receptors, and in equilibrium binding assays, it is highly selective for the alpha4beta2 receptor. In this study, we have examined the functional activity of varenicline at a variety of rat neuronal nicotinic receptors expressed in Xenopus laevis oocytes and assayed under two-electrode voltage clamp. We also find that varenicline is a potent, partial agonist at alpha4beta2 receptors, with an EC50 of 2.3 +/- 0.3 microM and an efficacy (relative to acetylcholine) of 13.4 +/- 0.4%. Varenicline has lower potency and higher efficacy at alpha3beta4 receptors, with an EC50 of 55 +/- 8 microM and an efficacy of 75 +/- 6%. Varenicline also seems to be a weak partial agonist at alpha3beta2 and alpha6-containing receptors, with an efficacy <10%. It is remarkable that varenicline is a potent, full agonist at alpha7 receptors with an EC50 of 18 +/- 6 microM and an efficacy of 93 +/- 7% (relative to acetylcholine). Thus, whereas varenicline is a partial agonist at some heteromeric neuronal nicotinic receptors, it is a full agonist at the homomeric alpha7 receptor. Some combination of these actions may be involved in the mechanism of varenicline as a smoking cessation aid.
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In the citing paper
“Varenicline is a partial agonist of α4/β2* nAChRs (Coe et al., 2005), but also activates α7-type nAChRs (Mihalak et al., 2006).”
From It is not “either/or”: Activation and desensitization of nicotinic acetylcholine receptors both contribute to behaviors related to nicotine addiction and mood (2008) · cites this paper as Mihalak et al., 2006
In the citing paper
“Varenicline (Chantix; Pfizer, Groton, CT) is a potent partial agonist at ␣42 nAChRs, with 40 to 60% of the agonist efficacy of nicotine (Rollema et al., 2007), and it is a less potent partial agonist at ␣34 and a full agonist at ␣7 nAChRs (Mihalak et al., 2006;Rollema et al., 2007Rollema et al., , 2009b)).”
From Nicotinic Partial Agonists Varenicline and Sazetidine-A Have Differential Effects on Affective Behavior (2010) · cites this paper as Mihalak et al., 2006
In the citing paper
“the high-affinity ␣42 partial agonist varenicline also has moderate affinity for other nAChRs and acts as a partial agonist at ␣34 and a full agonist at ␣7 nAChRs (Mihalak et al., 2006;Rollema et al., 2007).”
From Nicotinic Partial Agonists Varenicline and Sazetidine-A Have Differential Effects on Affective Behavior (2010) · cites this paper as Mihalak et al., 2006
In the citing paper
“Varenicline, a partial agonist at the α4β2 nAChRs, and a full agonist at the α7 nAChRs, is a new, efficacious treatment for nicotine dependence (4–6).”
From Varenicline improves mood and cognition during smoking abstinence (2009) · cites this paper as [6]
In the citing paper
“Varenicline, a partial agonist at the α4β2 nAChRs, and a full agonist at the α7 nAChRs, is a new, efficacious treatment for nicotine dependence (4–6).”
From Varenicline improves mood and cognition during smoking abstinence (2009) · cites this paper as [6]
In the citing paper
“It acts as a partial agonist at α3β4-, α2-, and α6-containing nAChRs, and a full agonist at α7 nAChRs [238].”
From Mechanistic insights into nicotine withdrawal (2011) · cites this paper as [238]
In the citing paper
“It is a derivative of cytisine, a plant alkaloid with selective affinity and partial agonism for α4β2 nAChRs [236–238].”
From Mechanistic insights into nicotine withdrawal (2011) · cites this paper as [238]
In the citing paper
“It is a derivative of cytisine, a plant alkaloid with selective affinity and partial agonism for α4β2 nAChRs [236–238].”
From Mechanistic insights into nicotine withdrawal (2011) · cites this paper as [237]
In the citing paper
“subsequent work showed that varenicline had a significant effect at ␣7 nAChRs, ␣34* nAChRs, and 5-hydroxytryptamine type 3 receptors”
From Varenicline Is a Potent Partial Agonist at α6β2* Nicotinic Acetylcholine Receptors in Rat and Monkey Striatum (2012) · cites this paper as Mihalak et al., 2006
In the citing paper
“varenicline, a partial agonist of the α4β2 nAChRs and a full α7 agonist developed to aid smoking cessation in humans (Mihalak, Carroll, & Luetje, 2006), has also been found to have antidepressant effects in the FST (Rollema et al., 2009).”
From Nicotine addiction and psychiatric disorders (2015) · cites this paper as Mihalak et al., 2006
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Metadata
- Authors
- Mihalak, K. B., Carroll, F. I., & Luetje, C. W.
- Affiliations
- University of Miami (US)
- RTI International (US)
- Venue
- Molecular Pharmacology
- Publisher
- Elsevier BV
- Published
- 2006-09
- Volume
- 70
- Issue
- 3
- Pages
- 801-805
- ISSN
- 0026-895X (ISSN-L)
- OpenAlex
- W2141246891
- Cited by
- 558
- References
- 26
- Citations by year
- 2026: 12 · 2025: 8 · 2024: 7 · 2023: 23 · 2022: 14 · 2021: 15 · 2020: 20 · 2019: 19 · 2018: 22 · 2017: 32 · 2016: 41 · 2015: 40 · 2014: 44 · 2013: 48 · 2012: 36
- FWCI
- 10.88
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Molecular Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Funders
- University of Miami
- U.S. Food and Drug Administration
- National Heart, Lung, and Blood Institute (T32HL007188)
- National Institute of Mental Health (MH-66038, R01MH066038)
- National Institute on Drug Abuse (R01DA012001, DA12001, DA08102, R01DA008102)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Smoking Behavior and Cessation
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Keywords
- varenicline, neuronal nicotinic acetylcholine receptors, alpha4beta2 receptor, partial agonists, full agonists, receptor selectivity, smoking cessation, cytisine derivatives
- MeSH terms
- Varenicline, Animals, Benzazepines, Neurons, Oocytes, Quinoxalines, Receptors, Nicotinic, Xenopus laevis, Nicotinic Agonists, Rats, alpha7 Nicotinic Acetylcholine Receptor
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