AChE
Acetylcholinesterase (AChE) is the principal cholinergic enzyme that rapidly hydrolyzes acetylcholine at cholinergic synapses and neuromuscular junctions, thereby terminating neurotransmission and maintaining synaptic signaling fidelity[1]. Mechanistically, AChE regulates cholinergic pathway activity through efficient acetylcholine clearance, a process that is essential for normal neuronal communication and neuromuscular function[1]. Beyond its catalytic role, AChE displays multiple molecular forms and has been implicated in cellular interactions, neuronal activity modulation, and pathological states, supporting broader biological functions outside classical neurotransmission[1]. In neurodegenerative disease models, particularly Alzheimer’s disease (AD), altered cholinergic signaling is closely associated with cognitive impairment, and cholinesterase inhibition remains a major symptomatic therapeutic strategy[2][3]. Compared with the related isoform butyrylcholinesterase (BChE), AChE is the predominant cholinesterase in the brain and plays a primary role in synaptic acetylcholine hydrolysis, whereas BChE may compensate when AChE activity is reduced and exhibits distinct pathological changes during AD progression[3][4]. For experimental and translational applications, reversible and dual AChE/BChE inhibitors, including rivastigmine, are widely used to enhance cholinergic neurotransmission and investigate mechanisms underlying neurodegeneration and cognitive dysfunction[2][3].
References:
- [1]. Massoulié J, et al. Structure and functions of acetylcholinesterase and butyrylcholinesterase. Prog Brain Res. 1993;98:139-46. [Content Brief]
- [2]. Walczak-Nowicka ŁJ, et al. Acetylcholinesterase Inhibitors in the Treatment of Neurodegenerative Diseases and the Role of Acetylcholinesterase in their Pathogenesis. Int J Mol Sci. 2021 Aug 27;22(17):9290. [Content Brief]
- [3]. Nordberg A, et al. A review of butyrylcholinesterase as a therapeutic target in the treatment of Alzheimer's disease. Prim Care Companion CNS Disord. 2013;15(2):PCC.12r01412. [Content Brief]
- [4]. Geula C, et al. Butyrylcholinesterase, cholinergic neurotransmission and the pathology of Alzheimer's disease. Drugs of Today (Barcelona, Spain : 1998). 2004 Aug;40(8):711-721. [Content Brief]
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AChE Related Products (438)
Related Products (438)
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Physostigmine hemisulfate
0 ImagesPhysostigmine hemisulfate (Eserine hemisulfate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine hemisulfate is also an antidote for anticholinergic poisoning.
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Pralidoxime chloride
0 ImagesPralidoxime chloride is a potent reactivator of acetylcholinesterase (AChE). Pralidoxime chloride reactivates nerve agent-inhibited AChE via direct nucleophilic attack by the oxime moiety on the phosphorus center of the bound nerve agent. Pralidoxime chloride is an antidote for organophosphate poisoning.
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Skimmianine
0 ImagesSkimmianine is an orally active furoquiniline alkaloid present mainly in the Rutaceae family. Skimmianine has analgesic, antispastic, sedative, and anti-inflammatory properties. Skimmianine inhibits acetylcholinesterase (AChE) (IC50 = 8.6 μg/mL). Skimmianine exhibits cytotoxicity against a variety of cancer cell lines and genotoxicity. Skimmianine has antioxidant and anti-inflammatory effects on ischemia-reperfusion (IR) injury. Skimmianine exerts anti-inflammatory effects through activation of the phosphatidylinositol-3-kinase (PI3K)-protein kinase B (AKT) pathway. Skimmianine is neuroprotective by targeting the NF-κB activation pathway to prevent neuroinflammation. Skimmianine inhibits the release of histamine, intracellular Ca2+ signaling and protein kinase C signaling.
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Cornuside
0 ImagesCornuside is an iridoid glycoside with anti-allergic, anti-inflammatory, and neuroprotective activities. Cornuside exerts anti-allergic activity by downregulating the p38 MAPK, JNK, and NF-κB signaling pathways, and inhibits IgE-mediated histamine release from mast cells. Cornuside improves cognitive impairment in mice by inhibiting BACE1 activity (IC50 = 55.84 μg/mL) and enhancing ChAT activity. Cornuside inhibits LPS (HY-D1056)-induced inflammatory mediators, including iNOS, COX-2, PGE2, TNF-α, IL-6, and IL-1β, by suppressing NF-κB activation.
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Itopride hydrochloride
0 ImagesSynonyms: HSR803Itopride (HSR803) hydrochloride is a potent dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride hydrochloride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD).
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Asoxime dichloride
0 ImagesSynonyms: HI-6Asoxime dichloride (HI-6) is an orally active thiosemicarbazone-based antidote. Asoxime dichloride is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dichloride significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dichloride is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dichloride can serve as an effective immunomodulator, improving the immune effect of the nervous system.
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Trimethylammonium chloride-d9
0 ImagesTrimethylammonium chloride-d9 is the d9-labeled Trimethylammonium chloride (HY-Y0504). Trimethylammonium chloride (Hegzadesil) is a non-competitive Acetylcholinesterase inhibitor. Trimethylammonium chloride reversibly blocks the deacetylation of acetylcholinesterase.
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Schisanhenol
0 ImagesSynonyms: Schizanhenol; Gomisin-K3Schisanhenol (Schizanhenol), a lignan, is an orally active antioxidant. Schisanhenol reduces AChE activity, increases SIRT1 and PGC-1α expression, and decreases phosphorylated Tau (Ser 396) levels. Schisanhenol increases SOD and glutathione peroxidase activity, decreases malondialdehyde (MDA) content, and inhibits UGT2B7 activitY. Schisanhenol attenuates ox-LDL-induced apoptosis, intracellular reactive oxygen species generation, and cytotoxicity in endothelial cells. Schisanhenol inhibits LDL oxidation, brain mitochondrial and membrane peroxidative damage, and brain mitochondrial swelling and disintegration. Schisanhenol can be used for the research of Alzheimer’s disease, atherosclerosis, brain ischemia, and age-related brain deterioration.
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Acephate
0 ImagesAcephate is a broad-spectrum anticholinesterase insecticide. Acephate acts via inhibiting AChE activity of insects. Acephate is used for control of several species of insects in agriculture and in horticulture.
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Profenofos
0 ImagesCat. No.: HY-B0832CAS No.: 41198-08-7Profenofos is an insecticida used on field crops, vegetables, and fruit crops. Profenofos is an acetylcholinesterase (AChE) inhibitor, with neurotoxicity.
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Aaptamine
0 ImagesAaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the α-adrenergic receptor, as well as an inhibitor of the proteasome and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects.
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Rhodionin
0 ImagesRhodionin is an orally active, multifunctional antivirulence and cytoprotective agent that targets and inhibits Lipase, sortase A (SrtA), CYP2D6 (IC50=0.761 μM), AChE (IC50=2.43-57.5 μM), and DPPH free radicals (IC50=19.49 μM). Rhodionin is isolable from the roots of Rhodiola crenulata. Rhodionin reduces postprandial serum triglyceride levels in mice by inhibiting lipase activity. Rhodionin also binds directly to SrtA to inhibit its transpeptidase activity, thereby reducing the fibrinogen adhesion and surface protein A levels of MRSA, effectively inhibiting biofilm formation and protecting against MRSA-induced cell damage. Rhodionin improves the survival rate of infected mice without affecting MRSA growth, and finds wide application in studies related to hyperlipidemia, exogenous obesity, and pneumonia induced by methicillin-resistant Staphylococcus aureus (MRSA).
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Tenuifolin
0 ImagesTenuifolin is effective and has a protective action. Tenuifolin inhibits β-secretase decreases Aβ protein secretion, suppresses Aβ25-35 secretion, and subsequently caspase-3 and caspase-9 become active. Tenuifolin's ability to lower AChE activity, increase at the same time, increase the ability of the upper glands, and improve the ability to read and remember. Research on tenuifolin's potential for use in urinary disease (AD).
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Violanthin
0 ImagesViolanthin is isolated from the stems of Dendrobium officinale, has potent antioxidant and antibacterial activities. Violanthin inhibits acetylcholinesterase (AChE) with an IC50 value of 79.80 μM.
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ACG548B
0 ImagesACG548B (compound 24) is a potent inhibitor of acetyl- and butyrylcholinesterase (AChE and BChE) with IC50s of 1.78 and 0.496 μM, respectively. ACG548B has higher AChE affinity and selectivity over BChE and ChoK (choline kinase). ACG548B can be uesd for the study of myasthenia gravis and neuromuscular blockade.
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RPR121056
0 ImagesSynonyms: APCRPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE.
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Phenserine
0 ImagesSynonyms: (-)-Eseroline phenylcarbamate; (-)-PhenserinePhenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine (HY-N6608) and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease.
