ArticleBritish journal of pharmacology2018
Galantamine is not a positive allosteric modulator of human α4β2 or α7 nicotinic acetylcholine receptors.
Article in British journal of pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 50 citations in OpenAlex.
- Trial
- Nicotine in Neurodegenerative and Neuropsychiatric Disorders: Mechanisms and Clinical Evidence.Neurochemical research · 2026Review
- Docking Analysis of Drugs Used in the Treatment of Alzheimer's Disease, Using Cell Membrane Receptors and Enzymes of the Kynurenine Pathway: A Pilot Study.International journal of molecular sciences · 2026Article
- The Muscarinic Acetylcholine Receptor in Dermal Papilla Cells Regulates Hair Growth.International journal of molecular sciences · 2026Article
- Differential cognitive enhancer effects of acetylcholinesterase inhibitors and memantine on age-related deficits in vigilance and sustained attention: a preclinical validation study.Behavioral and brain functions : BBF · 2025Article
- Therapeutic Targeting of the α7 Nicotinic Receptor: Challenges and Prospects for Cognitive Improvement in Alzheimer's and Schizophrenia.Basic & clinical pharmacology & toxicology · 2025Review
- A New Era of Muscarinic Acetylcholine Receptor Modulators in Neurological Diseases, Cancer and Drug Abuse.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Galantamine-Memantine Combination in the Treatment of Parkinson's Disease Dementia.Brain sciences · 2024Review
- Radiosynthesis, Preclinical, and Clinical Positron Emission Tomography Studies of Carbon-11 Labeled Endogenous and Natural Exogenous Compounds.Chemical reviews · 2023Review
- Neuropharmacology of Alcohol Addiction with Special Emphasis on Proteomic Approaches for Identification of Novel Therapeutic Targets.Current neuropharmacology · 2023Article
- Unravelling Binding of Human Serum Albumin with Galantamine: Spectroscopic, Calorimetric, and Computational Approaches.ACS omega · 2022Article
- Gain-of-function variants in GABRD reveal a novel pathway for neurodevelopmental disorders and epilepsy.Brain : a journal of neurology · 2022Article
- Bibliometric analysis of nicotinic acetylcholine receptors channel research (2000-2020).Channels (Austin, Tex.) · 2021Review
- Treating disorders across the lifespan by modulating cholinergic signaling with galantamine.Journal of neurochemistry · 2021Review
- Acetylcholinesterase Inhibitors in the Treatment of Neurodegenerative Diseases and the Role of Acetylcholinesterase in their Pathogenesis.International journal of molecular sciences · 2021Review
- Therapeutic Targeting ofPharmacological reviews · 2021Review
- Acetylcholinesterase inhibitors targeting the cholinergic anti-inflammatory pathway: a new therapeutic perspective in aging-related disorders.Aging clinical and experimental research · 2021Review
- Concatemers to re-investigate the role of α5 in α4β2 nicotinic receptors.Cellular and molecular life sciences : CMLS · 2021Article
- Heterologous expression of concatenated nicotinic ACh receptors: Pros and cons of subunit concatenation and recommendations for construct designs.British journal of pharmacology · 2020Article
- Allosterism of Nicotinic Acetylcholine Receptors: Therapeutic Potential for Neuroinflammation Underlying Brain Trauma and Degenerative Disorders.International journal of molecular sciences · 2020Review
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeThe alkaloid galantamine was originally isolated from the green snowdrop Galanthus woronowii and is currently marketed as a drug for treatment of mild to moderate dementia in patients with Alzheimer's disease. In addition to a well-documented proficiency to inhibit acetylcholinesterase, galantamine has been reported to increase neuronal nicotinic ACh (nACh) receptor function by acting as a positive allosteric modulator. Yet there remains controversy regarding these findings in the literature. To resolve this conundrum, we evaluated galantamine actions at α4β2 and α7, which represent the nACh receptors most commonly associated with mammalian cognitive domains. EXPERIMENTAL APPROACH: α4β2 [in (α4) KEY
resultsIn concentrations ranging from 10 nM to 1 μM, galantamine did not display direct agonism nor positive modulatory effects at any receptor combination tested. At concentrations from 10 μM and above, galantamine inhibited the activity with a mechanism of action consistent with open-channel pore blockade at all receptor types. CONCLUSION AND IMPLICATIONS: Based on our data, we conclude that galantamine is not a positive allosteric modulator of α7 or α4β2 receptors, which represent the majority of nACh receptors in mammalian brain.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.