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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.
2-Hydroxyalbrassitriol is a potent inhibitor of acetylcholinesterase (AChE) with an IC50 of 35.97 μM. This compound is utilized in research focused on neurodegenerative diseases and cognitive function by modulating cholinergic signaling. Its inhibition of AChE makes it a valuable reagent for studies investigating potential therapeutic strategies for conditions such as Alzheimer's disease.
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Insecticidal Agent 5 (compound 8) is a potent acetylcholinesterase (AChE) inhibitor designed for use as an insecticide. It exhibits significant biological activity with an LD50 of 27.65 ppm against the cotton leafworm, Spodoptera littoralis. This compound serves as an essential tool in research focused on pest control and insect physiology.
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BChE-IN-5 is a selective inhibitor of butyrylcholinesterase (BChE) with an IC50 of 2.8 nM, demonstrating greater potency against human BChE compared to human acetylcholinesterase (hAChE). This compound is valuable for research focused on neurodegenerative disorders, particularly Alzheimer's disease, by modulating cholinergic signaling pathways. Its specificity and efficacy make BChE-IN-5 a significant tool in elucidating the role of BChE in cognitive decline and related pathologies.
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6,9-Dichloro-1,2,3,4-tetrahydroacridine serves as an important intermediate in the synthesis of acetylcholinesterase (AChE) inhibitors. These inhibitors are relevant in the investigation of Alzheimer's disease, facilitating research on therapeutic strategies aimed at enhancing cholinergic transmission. This compound is essential for studying AChE's role in neurodegeneration and cognitive decline.
Synonyms: S 9977 free base; S 9977-2 free base
Stacofylline is a potent inhibitor of acetylcholinesterase (AChE), exhibiting an IC50 range of 5-50 nM. This xanthine derivative demonstrates significant anti-amnesic and promnesic properties, making it a valuable compound for research involving cognitive enhancement and memory-related studies. Its ability to modulate cholinergic neurotransmission highlights its potential applications in neuropharmacology and the investigation of Alzheimer's disease and other memory disorders.
8-Hydroxydihydrochelerythrine is a selective and competitive inhibitor of acetylcholinesterase (AChE) with an IC50 of 0.61 μM. Derived from the roots of Zanthoxylum nitidum, this benzophenanthridine alkaloid enhances acetylcholine levels in cholinergic synapses, thereby facilitating improved cholinergic neurotransmission. Its unique mechanism makes 8-Hydroxydihydrochelerythrine valuable for research into neurodegenerative disorders, particularly Alzheimer's disease and related dementias.
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AChE/BChE-IN-2 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 0.96 ± 0.14 µM for AChE and 1.23 ± 0.23 µM for BChE. This compound is valuable for research into Alzheimer's disease and other neurodegenerative disorders, facilitating studies on cholinergic signaling and enzyme activity modulation. Its efficacy in inhibiting cholinesterases makes it a significant tool for understanding the biochemical pathways involved in cognitive decline.
AChE/BChE-IN-6 is a potent dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 0.809 µM for AChE and 2.248 µM for BChE, with limited activity against hMAO-B. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for research focused on Alzheimer's disease. Its ability to inhibit cholinesterases suggests potential applications in studies aiming to understand and develop treatments for neurodegenerative conditions characterized by cholinergic dysfunction.
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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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Synonyms: EN101; ODN 7040; BL 7040
Monarsen is a synthetic 20-base antisense oligodeoxynucleotide targeting the human acetylcholinesterase (AChE) gene. This compound is utilized in research related to autoimmune myasthenia gravis (MG), a neuromuscular disorder characterized by autoantibodies against the acetylcholine receptor (AChR). Monarsen's mechanism of action allows for the inhibition of AChE expression, making it a valuable tool for studying disease mechanisms and potential therapeutic interventions in MG.
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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.
