ArticleBritish journal of pharmacology2005
Effect of galantamine on the human alpha7 neuronal nicotinic acetylcholine receptor, the Torpedo nicotinic acetylcholine receptor and spontaneous cholinergic synaptic activity.
Article in British journal of pharmacology, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 46 citations in OpenAlex.
- Nicotine in Neurodegenerative and Neuropsychiatric Disorders: Mechanisms and Clinical Evidence.Neurochemical research · 2026Review
- A novel process driving Alzheimer's disease validated in a mouse model: Therapeutic potential.Alzheimer's & dementia (New York, N. Y.) · 2022Article
- Treating disorders across the lifespan by modulating cholinergic signaling with galantamine.Journal of neurochemistry · 2021Review
- CaCells · 2020Review
- Therapeutic potential of α7 nicotinic acetylcholine receptor agonists to combat obesity, diabetes, and inflammation.Reviews in endocrine & metabolic disorders · 2020Review
- Allosterism of Nicotinic Acetylcholine Receptors: Therapeutic Potential for Neuroinflammation Underlying Brain Trauma and Degenerative Disorders.International journal of molecular sciences · 2020Review
- Galantamine protects against synaptic, axonal, and vision deficits in experimental neurotrauma.Neurobiology of disease · 2020Article
- Novel Approach for the Search for Chemical Scaffolds with Dual Activity with Acetylcholinesterase and the α7 Nicotinic Acetylcholine Receptor-A Perspective for the Treatment of Neurodegenerative Disorders.Molecules (Basel, Switzerland) · 2019Article
- Galantamine is not a positive allosteric modulator of human α4β2 or α7 nicotinic acetylcholine receptors.British journal of pharmacology · 2018Article
- Acetylcholine nicotinic receptor subtypes in chromaffin cells.Pflugers Archiv : European journal of physiology · 2018Review
- Review
- Central cholinergic activation of a vagus nerve-to-spleen circuit alleviates experimental colitis.Mucosal immunology · 2014Article
- Physostigmine and galanthamine bind in the presence of agonist at the canonical and noncanonical subunit interfaces of a nicotinic acetylcholine receptor.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2013Article
- CHRNA7 polymorphisms and response to cholinesterase inhibitors in Alzheimer's disease.PloS one · 2013Article
- Human α4β2 nicotinic acetylcholine receptor as a novel target of oligomeric α-synuclein.PloS one · 2013Article
- Structural answers and persistent questions about how nicotinic receptors work.Frontiers in bioscience : a journal and virtual library · 2008Review
- [Therapy of cognitive deficits in schizophrenia with acetylcholinesterase inhibitors. A systematic overview].Der Nervenarzt · 2008Review
- Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators.Proceedings of the National Academy of Sciences of the United States of America · 2007Article
- Keynote review: allosterism in membrane receptors.Drug discovery today · 2006Review
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. Various types of anticholinesterasic agents have been used to improve the daily activities of Alzheimer's disease patients. It was recently demonstrated that Galantamine, described as a molecule with anticholinesterasic properties, is also an allosteric enhancer of human alpha4beta2 neuronal nicotinic receptor activity. We explored its effect on the human alpha7 neuronal nicotinic acetylcholine receptor (nAChR) expressed in Xenopus oocytes. 2. Galantamine, at a concentration of 0.1 microM, increased the amplitude of acetylcholine (ACh)-induced ion currents in the human alpha7 nAChR expressed in Xenopus oocytes, but caused inhibition at higher concentrations. The maximum effect of galantamine, an increase of 22% in the amplitude of ACh-induced currents, was observed at a concentration of 250 microM Ach. 3. The same enhancing effect was obtained in oocytes transplanted with Torpedo nicotinic acetylcholine receptor (AChR) isolated from the electric organ, but in this case the optimal concentration of galantamine was 1 microM. In this case, the maximum effect of galantamine, an increase of 35% in the amplitude of ACh-induced currents, occurred at a concentration of 50 microM ACh. 4. Galantamine affects not only the activity of post-synaptic receptors but also the activity of nerve terminals. At a concentration of 1 microM, quantal spontaneous events, recorded in a cholinergic synapse, increased their amplitude, an effect which was independent of the anticholinesterasic activity associated with this compound. The anticholinesterasic effect was recorded in preparations treated with a galantamine concentration of 10 microM. 5. In conclusion, our results show that galantamine enhances human alpha7 neuronal nicotinic ACh receptor activity. It also enhances muscular AChRs and the size of spontaneous cholinergic synaptic events. However, only a very narrow range of galantamine concentrations can be used for enhancing effects.
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