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Neuronal Nicotinic Acetylcholine Receptor Structure and Function and Response to Nicotine
Open accessAbstract
Nicotinic acetylcholine receptors (nAChRs) belong to the "Cys-loop" superfamily of ligand-gated ion channels that includes GABAA, glycine, and serotonin (5-HT3) receptors. There are 16 homologous mammalian nAChR subunits encoded by a multigene family. These subunits combine to form many different nAChR subtypes with various expression patterns, diverse functional properties, and differing pharmacological characteristics. Because cholinergic innervation is pervasive and nAChR expression is extremely broad, practically every area of the brain is impinged upon by nicotinic mechanisms. This review briefly examines the structural and functional properties of the receptor/channel complex itself. The review also summarizes activation and desensitization of nAChRs by the low nicotine concentrations obtained from tobacco. Knowledge of the three-dimensional structure and the structural characteristics of channel gating has reached an advanced stage. Likewise, the basic functional properties of the channel also are reasonably well understood. It is these receptor/channel properties that underlie the participation of nAChRs in nearly every anatomical region of the mammalian brain.
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“Nicotine mediates its effects via nicotinic cholinergic receptors (nAChRs), pentameric ligand-gated ion channels that are widely distributed throughout the brain (Dani, 2015; Zoli et al., 2015).”
From Unique, long-term effects of nicotine on adolescent brain. (2020) · cites this paper as Dani, 2015
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Metadata
- Authors
- Dani, J. A.
- Affiliations
- University of Pennsylvania (US)
- Corresponding author
- Dani, John A.
- ORCID
- Dani, John A.
- Venue
- International Review of Neurobiology
- Publisher
- Elsevier
- Published
- 2015
- Volume
- 124
- Pages
- 3-19
- ISSN
- 0074-7742 (ISSN-L)
- PMC
- PMC4795468
- OpenAlex
- W2427261560
- Cited by
- 309
- References
- 69
- Citations by year
- 2026: 24 · 2025: 28 · 2024: 41 · 2023: 38 · 2022: 27 · 2021: 46 · 2020: 41 · 2019: 28 · 2018: 22 · 2017: 10 · 2016: 4
- FWCI
- 19.11
- Type
- book chapter
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- International review of neurobiology (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Institutes of Health
- National Institute on Drug Abuse (DA09411, R01DA009411, R01DA036572)
- National Institute of Neurological Disorders and Stroke (NS 21229, R37NS021229, R01NS021229)
- 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
- Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Smoking Behavior and Cessation
- Keywords
- nicotinic acetylcholine receptors, Cys-loop ligand-gated ion channels, receptor structure, channel gating, receptor desensitization, nAChR subtypes
- MeSH terms
- Animals, Humans, Models, Molecular, Nicotine, Receptors, Nicotinic, Ion Channel Gating, Protein Subunits
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