ArticleCurrent neuropharmacology2013
Acetylcholinesterase inhibitors: pharmacology and toxicology.
Article in Current neuropharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 726 papers, 4 of them syntheses that pooled it.
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Who cites it
726 citing papers in PubMed, 4 syntheses or guidelines pooled it, 2,491 citations in OpenAlex.
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- Efficacy of acetylcholinesterase inhibitors on reducing hippocampal atrophy rate: a systematic review and meta-analysis.BMC neurology · 2025Pooled it
- Galantamine for dementia due to Alzheimer's disease and mild cognitive impairment.The Cochrane database of systematic reviews · 2024Pooled it
- Exploring the efficacy of cholinergic agents for the treatment of psychostimulant use disorder: a systematic review.Psychopharmacology · 2024Pooled it
- Safety, tolerability, pharmacokinetic and pharmacodynamic effects of the muscarinic MAlzheimer's research & therapy · 2025Trial
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- From bench to brain: novel thieno-oxazine hybrids as potent pleiotropic anti-Alzheimer's agents withJournal of enzyme inhibition and medicinal chemistry · 2026Article
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- Early Neuroprotective Effects of Erucic Acid and Gentisic Acid on Hippocampal Glutamate Concentrations and Alzheimer-like Molecular Alterations in an Intracerebroventricular Streptozotocin Rat Model.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Structural and Biological Evidence for Acetylcholinesterase-Targeted Insecticidal Activity in Musca domestica: A 4.5 Å Distance Correlation From Novel Benzenesulfonamide Derivatives.Molecular informatics · 2026Article
- Quinoline and Phthalimide Substituted Silicon Phthalocyanines as Multi-Target Inhibitors of Cholinesterases and Carbonic Anhydrases.Journal of biochemical and molecular toxicology · 2026Article
- Saccadic Oscillations After Donepezil Administration in Patients with Dementia: Time Course and Clinical Correlates.Journal of eye movement research · 2026Article
- Uncertainty Quantification with Domain Classification Models for Acetylcholinesterase Inhibition.Journal of chemical information and modeling · 2026Article
- Rhodanine and 2,4-dioxothiazolidine-based amides: synthesis and evaluation as dual-action cholinesterase inhibitors and antioxidants.RSC medicinal chemistry · 2026Article
- ADMET-XSpec: A Tool for Systematic Cross-Species Data Integration in ADMET Prediction.Chemical research in toxicology · 2026Article
- Rational Design of Multifunctional Tacrine Derivatives as Candidates for the Treatment of Alzheimer and Parkinson Diseases.ChemMedChem · 2026Article
- Metabolite-Driven Biological Activity of Mandragora autumnalis and Spartium junceum: A Comparative LC-MS/MS Study on Antioxidant, Cholinesterase, and Carbonic Anhydrase Inhibition.ChemistryOpen · 2026Article
666 more citing papers are in PubMed but not listed here.
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Acetylcholinesterase is involved in the termination of impulse transmission by rapid hydrolysis of the neurotransmitter acetylcholine in numerous cholinergic pathways in the central and peripheral nervous systems. The enzyme inactivation, induced by various inhibitors, leads to acetylcholine accumulation, hyperstimulation of nicotinic and muscarinic receptors, and disrupted neurotransmission. Hence, acetylcholinesterase inhibitors, interacting with the enzyme as their primary target, are applied as relevant drugs and toxins. This review presents an overview of toxicology and pharmacology of reversible and irreversible acetylcholinesterase inactivating compounds. In the case of reversible inhibitors being commonly applied in neurodegenerative disorders treatment, special attention is paid to currently approved drugs (donepezil, rivastigmine and galantamine) in the pharmacotherapy of Alzheimer's disease, and toxic carbamates used as pesticides. Subsequently, mechanism of irreversible acetylcholinesterase inhibition induced by organophosphorus compounds (insecticides and nerve agents), and their specific and nonspecific toxic effects are described, as well as irreversible inhibitors having pharmacological implementation. In addition, the pharmacological treatment of intoxication caused by organophosphates is presented, with emphasis on oxime reactivators of the inhibited enzyme activity administering as causal drugs after the poisoning. Besides, organophosphorus and carbamate insecticides can be detoxified in mammals through enzymatic hydrolysis before they reach targets in the nervous system. Carboxylesterases most effectively decompose carbamates, whereas the most successful route of organophosphates detoxification is their degradation by corresponding phosphotriesterases.
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Registered trials
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.