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Acetylcholinesterase (AChE) inhibitors block the enzyme that breaks down acetylcholine at cholinergic synapses. By ending acetylcholine signaling within milliseconds, AChE controls transmission in the brain and at the neuromuscular junction. The 1991 crystal structure of AChE from Torpedo californica showed the active site at the base of a deep, narrow gorge. AChE also has non-catalytic roles, which broaden its interest beyond synaptic transmission. Inhibitors here include donepezil hydrochloride and galanthamine hydrobromide, which are reversible inhibitors. The carbamates rivastigmine tartrate and neostigmine bromide, used in studies of cholinergic signaling and neurodegeneration, are also listed.
AChE-IN-24 is a potent inhibitor of acetylcholinesterase (AChE), demonstrating remarkable ability to penetrate the blood-brain barrier. It exhibits strong inhibitory activity against human AChE, with an IC50 value of 0.053 μM. This compound is valuable for research in Alzheimer's disease, facilitating studies aimed at understanding the enzymatic mechanisms involved in neurodegeneration.
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Artanin is a coumarin derivative that functions as an acetylcholinesterase (AChE) inhibitor. It demonstrates significant biological activities relevant to Alzheimer's disease, including the inhibition of AChE and the prevention of amyloid beta (Aβ) aggregation, with IC50 values of 51 μM, 98 μM, and 124 μM, respectively. This compound is valuable for research focusing on neurodegenerative disorders and the mechanistic exploration of Alzheimer's pathology.
sEH/AChE-IN-2 is a dual inhibitor targeting soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). This compound demonstrates significant potential in mitigating neuroinflammation and addressing memory impairment. Its dual inhibitory action provides a valuable tool for investigating therapeutic strategies in Alzheimer's disease research.
AChE/BuChE/MAO-B-IN-1 is a potent inhibitor of human acetylcholinesterase (hAChE), butyrylcholinesterase (hBuChE), and monoamine oxidase-B (hMAO-B), with IC50 values of 4.8 μM, 13.7 μM, and 1.11 μM, respectively. This compound also demonstrates a high affinity for σ1 and σ2 receptors, with Ki values of 42.8 nM and 191 nM, respectively. AChE/BuChE/MAO-B-IN-1 is potentially useful in research focused on Alzheimer's disease and related neurological disorders.
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eeAChE/eqBuChE-IN-1 is a reversible dual inhibitor targeting both eeAChE and eqBuChE, with IC50 values of 1.3 μM and 0.81 μM, respectively. This compound demonstrates significant anti-inflammatory activity and offers neuroprotective effects, particularly in mitigating Aβ25-35-induced cytotoxicity in PC12 cells. It is suitable for research applications focused on neurodegenerative diseases and related pathways.
AChE-IN-31 is a non-competitive inhibitor of acetylcholinesterase (AChE). This compound demonstrates significant potential in the exploration of Alzheimer's disease pathology by modulating cholinergic signaling. AChE-IN-31 is suitable for use in research applications aimed at understanding the mechanisms of neurodegeneration and developing therapeutic strategies for cognitive disorders.
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AChE-IN-71 is an acetylcholinesterase (AChE) inhibitor that plays a significant role in the modulation of neurotransmitter levels. This compound is particularly relevant for research focused on neurodegenerative disorders, including Alzheimer’s disease. By inhibiting AChE activity, AChE-IN-71 can help elucidate the mechanisms underlying cholinergic dysfunction in Alzheimer's pathology, providing valuable insights for potential therapeutic strategies.
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Feralolide is a dihydroisocoumarin that functions as a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), exhibiting IC50 values of 55 μg/mL and 52 μg/mL, respectively. This compound also demonstrates antioxidant properties, effectively inhibiting 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS). Feralolide may serve as a valuable tool in research focused on cognitive disorders, such as Alzheimer's disease, aiming to restore and enhance memory functions.
Synonyms: Echothiophate chloride
Echothiopate chloride is a potent, irreversible inhibitor of cholinesterase (ChE). By forming a covalent bond with the serine residue at the active site of ChE, it permanently inactivates the enzyme, necessitating de novo enzyme synthesis for restoration of activity. This long-lasting inhibition makes echothiopate chloride effective in ocular applications, particularly as a miotic agent in the management of chronic glaucoma and accommodative esotropia, with effects that can persist for over a week.
Lycoramine is a dihydro-derivative of galanthamine that functions as a potent acetylcholinesterase (AChE) inhibitor. Isolated from the plant Lycoris radiata, it demonstrates significant potential in enhancing cholinergic signaling, making it a valuable reagent for research related to neurodegenerative diseases and cognitive disorders. Its inhibitory action on AChE may offer insights into therapeutic strategies for conditions such as Alzheimer's disease.
AChE/BChE-IN-31 is a cholinesterase inhibitor targeting human acetylcholinesterase (hAChE) and equine butyrylcholinesterase (eqBChE). It demonstrates significant inhibitory activity against these enzymes, making it relevant for research on neurodegenerative diseases such as Alzheimer’s disease. Additionally, AChE/BChE-IN-31 exhibits antioxidant properties, with an IC50 value of 105.04 μM against DPPH, indicating its potential utility in studies related to oxidative stress.
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3β-Hydroxy-lup-20(29)-en-16-one is a potent dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting a notable selectivity for BChE with an IC50 value of 28.9 μM. This lupane derivative serves as a valuable tool in the study of cholinergic signaling pathways and triterpenoid research. Its inhibitory properties position it as a potential candidate for neurodegenerative disease research applications, particularly in disorders characterized by cholinergic dysregulation.
AChE/BChE-IN-24 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 16.38 μM and 10.44 μM, respectively. This compound functions as a neuroprotective agent by preventing the breakdown of acetylcholine, thereby enhancing cholinergic neurotransmission. Its applications are particularly relevant in research related to neurodegenerative diseases and cognitive function disorders.
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Lakoochin C is a potent inhibitor of acetylcholinesterase (AChE) with an IC50 of 61.86 μM and butyrylcholinesterase (BChE) with an IC50 of 47.21 μM. This compound demonstrates significant biological activity in modulating cholinergic signaling, making it a valuable tool for research focused on neurodegenerative diseases such as Alzheimer's disease. Its application in studies of cholinergic dysfunction may provide insights into therapeutic strategies for memory-related disorders.
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AChE-IN-64 is a selective inhibitor of acetylcholinesterase (AChE) with an IC50 value of 36.9 µM. This compound is primarily utilized in research related to cognitive disorders, offering a valuable tool for the investigation of cholinergic dysfunction and its implications in conditions such as Alzheimer's disease and other neurodegenerative disorders.
Quinolactacin A1 is a potent acetylcholinesterase (AChE) inhibitor derived from the solid-state fermentation of Penicillium citrinum 90648. It exhibits significant biological activity in inhibiting AChE, making it a valuable compound for studying neurodegenerative disorders, particularly Alzheimer's disease. Research applications include exploring therapeutic strategies and understanding the biochemical pathways associated with cholinergic dysfunction.
Cyanofenphos is an orally active organophosphate compound that acts as an acetylcholinesterase (AChE) inhibitor, exhibiting neurotoxic properties. This reagent is associated with delayed neurotoxic effects, including ataxia and paralysis, and may present additional symptoms such as somnolence, decreased feed intake, and weight loss in avian models. Cyanofenphos demonstrates a self-antagonistic effect, whereby repeated low-dose pre-treatment can mitigate acute toxicity but exacerbate long-term neurotoxicity and decrease enzyme inhibition, with protective effects peaking 24 hours post-treatment. This compound is widely utilized in research focused on neurotoxicity and AChE inhibition pathways.
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BChE-IN-9 (Azepano-11-deoxo-glycyrrhetol) is a mixed type inhibitor of butyrylcholinesterase (BChE) with a Ki value of 0.21 µM. This compound exhibits significant inhibitory activity, making it a valuable tool for studying cholinergic signaling pathways and neurodegenerative diseases where BChE is implicated. Its use in research can provide insights into therapeutic strategies for conditions such as Alzheimer's disease and other neurocognitive disorders.
AChE-IN-21 is a potent and selective inhibitor of acetylcholinesterase (AChE), exhibiting an IC50 value of 2.66 nM. This compound demonstrates significant blood-brain barrier permeability in vitro, making it suitable for central nervous system research applications. AChE-IN-21 may be utilized in studies related to neurodegenerative diseases, such as Alzheimer's disease, by modulating cholinergic signaling pathways.
Synonyms: HP-290; NXX-066
Quilostigmine is a potent acetylcholinesterase inhibitor with an IC50 of 148 nM in rat brain acetylcholinesterase. This orally active analogue of Physostigmine demonstrates prolonged efficacy in reducing tremors. Its mechanism of action makes it a valuable tool for research related to Alzheimer's disease and other cognitive disorders.
BChE-IN-4 is a potent butyrylcholinesterase (BChE) inhibitor that effectively crosses the blood-brain barrier. This compound has demonstrated the ability to attenuate learning and memory deficits associated with cholinergic deficits in mouse models. BChE-IN-4 shows promise for research applications related to Alzheimer's disease, making it a valuable tool for investigations into cognitive dysfunction and neurotransmitter modulation.
Bleformin A is a potent butyrylcholinesterase (BChE) inhibitor with an IC50 value of 5.2 μM. Isolated from the natural source Bletilla striata, this compound demonstrates significant biological activity that is relevant to neurodegenerative disorders. Bleformin A is primarily utilized in research related to Alzheimer's disease, providing insights into cholinergic system modulation.
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Melineurine is a reversible mixed-type inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 95.3 μM for AChE and 28.0 μM for BChE. This compound is instrumental in the study of neurodegenerative disorders, particularly Alzheimer's disease, due to its effects on cholinergic signaling. Melineurine serves as a valuable tool for investigating the role of cholinesterase inhibition in cognitive function and related therapeutic strategies.
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Synonyms: Fas-2
Fasciculin-II is a potent inhibitor of acetylcholinesterase (AChE), an enzyme critical for neurotransmitter regulation. By blocking AChE activity, Fasciculin-II enhances cholinergic transmission, making it a valuable tool for research in neurobiology and related fields. Its biological activity is particularly relevant in studies of synaptic function and neurodegenerative diseases.
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AChE/BChE/MAO-B-IN-1 is a reversible inhibitor targeting acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and monoamine oxidase B (MAO-B), exhibiting IC50 values of 7.31 μM, 0.56 μM, and 26.1 μM, respectively. This compound effectively crosses the blood-brain barrier and demonstrates neuroprotective properties while maintaining a lack of cytotoxicity. Its multifaceted inhibition profile makes it a valuable tool for research on neurodegenerative diseases and associated pathways.
