Cited by 255Nicotinic Acetylcholine Receptors StudySmoking Behavior and CessationNeuroscience and Neuropharmacology Research

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Nicotine addiction: the possible role of functional upregulation

Buisson, Bruno, Bertrand, Daniel·2002·Trends in Pharmacological Sciences

DOI 10.1016/s0165-6147(00)01979-9

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Abstract

Upregulation of binding to nicotinic acetylcholine receptors (nAChRs) is observed in the brains of both smokers and animals chronically exposed to nicotine, although whether this in vivo change is accompanied by an increase in receptor function is unknown. In vitro recordings indicate that alpha4beta2- and alpha7-subtypes of nAChRs, which are the most abundant subtypes in the brain, are functionally upregulated following prolonged exposure to nicotine. The possible consequences of functional upregulation for nicotine addiction are discussed. Moreover, we propose a new paradigm that describes the unusual behavior of these neuronal nAChRs and helps to explain the effects of nicotine in the CNS and the diffuse effects of ACh.

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Authors: Buisson, B., & Bertrand, D.
Affiliations: University of Geneva (CH)
Corresponding author: Buisson, Bruno
ORCID: Bertrand, Daniel
Venue: Trends in Pharmacological Sciences
Publisher: Elsevier BV
Published: 2002-03
Volume: 23
Issue: 3
Pages: 130-136
ISSN: 0165-6147 (ISSN-L)
DOI: 10.1016/s0165-6147(00)01979-9
OpenAlex: W2042529247
Cited by: 254
References: 55
Citations by year: 2026: 3 · 2025: 2 · 2024: 2 · 2023: 4 · 2022: 2 · 2021: 5 · 2020: 3 · 2019: 4 · 2018: 7 · 2017: 6 · 2016: 6 · 2015: 4 · 2014: 10 · 2013: 8 · 2012: 7
FWCI: 1.27
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Trends in Pharmacological Sciences (publishedVersion)
PubMed (publishedVersion)
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 › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords: nicotine dependence, nicotinic acetylcholine receptors, receptor up-regulation, alpha4beta2 nAChR, alpha7 nAChR, chronic nicotine exposure, receptor function, cholinergic system
MeSH terms: Animals, Binding Sites, Brain, Cells, Cultured, Humans, Neurons, Nicotine, Receptors, Nicotinic, Tobacco Use Disorder, Up-Regulation, Smoking Cessation

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Nicotine addiction: the possible role of functional upregulation

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