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Cited by 304Nicotinic Acetylcholine Receptors StudyCholinesterase and Neurodegenerative DiseasesAlzheimer's disease research and treatments

The DOI matches its Crossref record; 77 of the 80 references it cites were found in a registry or an index.

Allosteric sensitization of nicotinic receptors by galantamine, a new treatment strategy for Alzheimer’s disease

Maelicke, Alfred, Samochocki, Marek, Jostock, Ruth, Fehrenbacher, Andreas, Ludwig, Jürgen, Albuquerque, Edson X, Zerlin, Marion·2001·Biological Psychiatry
DOI 10.1016/s0006-3223(00)01109-4
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Abstract

Cholinesterase inhibitors are the only approved drug treatment for patients with mild to moderately severe Alzheimer's disease. Interestingly, the clinical potency of these drugs does not correlate well with their activity as cholinesterase inhibitors, nor is their action as short lived as would be expected from purely symptomatic treatment. A few cholinesterase inhibitors, including galantamine, produce beneficial effects even after drug treatment has been terminated. These effects assume modes of action other than mere esterase inhibition and are capable of inducing systemic changes. We have recently discovered a mechanism that could account, at least in part, for the above-mentioned unexpected properties of some cholinesterase inhibitors. We have found that a subgroup of cholinesterase inhibitors, including galantamine but excluding tacrine, directly interacts with nicotinic acetylcholine receptors. These compounds, named allosterically potentiating ligands, sensitize nicotinic receptors by increasing the probability of channel opening induced by acetylcholine and nicotinic agonists and by slowing down receptor desensitization. The allosterically potentiating ligand action, which is not necessarily associated with cholinesterase inhibition, has been demonstrated by whole-cell patch-clamp recordings to occur in natural murine and human neurons and in murine and human cell lines expressing various subtypes of neuronal nicotinic acetylcholine receptors.

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Crossref · 10.1016/s0006-3223(00)01109-4

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Citations

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Research works printed but not linked: 5

  1. Inestrosa NC, De Ferrari GV (2000): Acetylcholinesterase-induced β-amyloid aggregation and neurotoxicity. In: Sixth Stockholm/Springfield Symposium on Advances in Alzheimer Therapy, Abstract 87.
  2. Lahiri DK, Farlow MR, Ge Y, Utsuki T, Greig NH (2000): Regulation of βAPP processing with cholinesterase inhibitors in neuronal cell lines. In: Sixth Stockholm/Springfield Symposium on Advances in Alzheimer Therapy, Abstract 96.
  3. Pereira, 1994, Physostigmine and galantamine, J Pharmacol Exp Ther, 270, 768
  4. Perry, 1999, Increased nicotinic receptors in brains from smokers, J Pharmacol Exp Ther, 289, 1545
  5. Soreq H, Sternfeld M, Flores-Flores C, Salmon A, Ginzberg D, Seidman S (2000): Multifaced role of acetylcholinesterase in Alzheimer’s disease. In: Sixth Stockholm/Springfield Symposium on Advances in Alzheimer Therapy, Abstract 146.

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Metadata

Authors
Maelicke, A., Samochocki, M., Jostock, R., Fehrenbacher, A., Ludwig, J., Albuquerque, E. X., & Zerlin, M.
Affiliations
Johannes Gutenberg University Mainz (DE)
Corresponding author
Maelicke, Alfred
ORCID
Jostock, Ruth
Venue
Biological Psychiatry
Publisher
Elsevier BV
Published
2001-02
Volume
49
Issue
3
Pages
279-288
ISSN
0006-3223 (ISSN-L)
DOI
10.1016/s0006-3223(00)01109-4
OpenAlex
W2043467860
Cited by
303
References
80
Citations by year
2026: 7 · 2025: 3 · 2024: 4 · 2023: 1 · 2022: 6 · 2021: 9 · 2020: 17 · 2019: 10 · 2018: 13 · 2017: 6 · 2016: 11 · 2015: 11 · 2014: 6 · 2013: 11 · 2012: 9
FWCI
1.65
Type
journal article
Language
en
Open access
closed
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations
  • Biological Psychiatry (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
  • Health Sciences › Medicine › Pharmacology (medical) › Cholinesterase and Neurodegenerative Diseases
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Alzheimer's disease research and treatments
Keywords
galantamine, nicotinic acetylcholine receptors, Alzheimer's disease, cholinesterase inhibitors, tacrine, receptor desensitization, acetylcholine, off-target effects
MeSH terms
Allosteric Regulation, Allosteric Site, Alzheimer Disease, Animals, Cell Line, Cholinesterase Inhibitors, Galantamine, Humans, Neurons, Receptors, Nicotinic, Patch-Clamp Techniques, Nootropic Agents, Mice

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