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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.
Synonyms: Cycloadiphenine hydrochloride; NSC 42559; Profenene hydrochloride; Trasentin H; Trasentine A
Drofenine hydrochloride is a potent competitive inhibitor of BChE, and the ki values of Drofenine is calculated to be 3 uM.
Synonyms: Tensilon; Tensilon chloride; Antirex; Enlon; Reversol
Edrophonium Chloride, also known as Tensilon, is an acetylcholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. Edrophonium Chloride has also been used as an antidote to curare principles.
Synonyms: Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene
Imidazole acts as an inhibitor of acetylcholinesterase (AChEI), xanthine oxidase (XO), and thromboxane. This heterocyclic aromatic compound exhibits significant biological activities, including antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic properties. By inhibiting the conversion of endoperoxides (PGG2 and PGH2) to thromboxane A2, Imidazole plays a role in cardiovascular research. Additionally, its derivatives have shown potential in inhibiting the SARS-CoV-2 3CLPro enzyme, making it a valuable candidate for studies related to Alzheimer's disease, gout, COVID-19, and thrombo-embolic conditions.
Synonyms: BC-48
Demecarium Bromide is a potent cholinesterase (ChE) inhibitor, exhibiting an apparent affinity (Kiapp) of 0.15 μM. It primarily functions by inhibiting the enzyme cholinesterase, thereby increasing acetylcholine levels. This compound is widely utilized in research related to glaucoma treatment and the study of acetylcholine metabolism, providing valuable insights into neurodegenerative diseases and neurotransmission pathways.
Synonyms: Carbophos; Mercaptothion; Carbofos; Karbofos; Maldison; Cythion; Prioderm; Sadophos
Malathion is an organophosphorous compound that inhibits cholinesterase enzyme activity. Malathion is an organophosphate insecticide of relatively low human toxicity.
Neostigmine methyl sulfate is a reversible inhibitor of acetylcholinesterase, primarily targeting the peripheral nervous system. This compound enhances cholinergic transmission by preventing the breakdown of acetylcholine, resulting in increased neurotransmitter levels at the neuromuscular junction. It is widely used in research applications related to neuromuscular disorders and pharmacological studies of cholinergic function.
Minaprine dihydrochloride is a selective monoamine oxidase inhibitor that penetrates the blood-brain barrier. It exhibits biological activity by reducing intraneuronal dopamine metabolism, lowering levels of striatal homovanillic acid and dihydroxyphenylacetic acid, while increasing levels of 3-methoxytyramine and 5-hydroxytryptamine in the striatum. Additionally, Minaprine dihydrochloride weakly inhibits acetylcholinesterase activity and displays both convulsant and antidepressant properties, making it a valuable reagent for research in neuropharmacology and mood disorder studies.
BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC50 of 8.9 nM.
Acetyllovastatin, a acetate of Lovastatin, presentes a moderate inhibitory effect against the enzyme acetylcholinesterase with an IC50 of 79 μg/mL. Lovastatin has been found to display antifungal activity, and suppresses proliferation of a number of transformed cell lines.
MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
(+)-Phenserine is a novel selective cholinesterase noncompetitive inhibitor with an IC50 of 45.3 μM.
(±)-Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).
Aldicarb sulfone(Temik sulfone) is a carbamate insecticide; is a cholinesterase inhibitor which prevents the breakdown of acetylcholine in the synapse.
TAE-1 is an inhibitor of amyloid-β fibril formation and aggregation. TAE-1 inhibits cholinesterases AChE and BuChE with IC50 of 0.3 μM and 3.9 μM, respectively.
Timosaponin AIII is a potent Inhibitor of U46619-induced Rat Platelet Aggregation, Selectively Inhibiting TxA2-induced Platelet Activation, Preferably Suppressing TP-mediated Activation of Gq, not G12/13, Signaling Pathways.
Distigmine Bromide, also known as Ubretid and BC-51, is an acetylcholinesterase inhibitor used for the treatment of underactive neurogenic bladder and myasthenia gravis.
MAPK-IN-1 (Compound 2) is an inhibitor of the MAPK signaling pathway with demonstrated neuroprotective and anti-neuroinflammatory properties. It also exhibits acetylcholinesterase (AChE) inhibitory activity, with an IC₅₀ of 23.84 μM, contributing to enhanced cholinergic signaling. These combined actions make MAPK-IN-1 a promising candidate for research in Alzheimer's disease and other neurodegenerative disorders, where modulation of MAPK signaling and cholinergic function are of therapeutic interest.
Picfeltarraenin IA is a triterpenoid compound isolated from *Picria fel-terrae* (*P. fel-terrae*) that functions as an acetylcholinesterase (AChE) inhibitor. It exhibits therapeutic potential for the treatment of herpes infections, cancer, and inflammatory conditions, making it a promising candidate for further pharmacological research.
Neuroprotective Agent 15 is a selective butyrylcholinesterase (BChE) inhibitor with IC50 values of 2.6 μM for BChE and 114.3 μM for acetylcholinesterase (AChE). This compound exhibits cannabinoid CB2 receptor agonistic activity, contributing to its neuroprotective properties. Neuroprotective Agent 15 has been shown to reduce cell death, alleviate LDH release, and inhibit Caspase-3/7 activity, thereby diminishing apoptosis. Additionally, it mitigates the formation of superoxide free radicals, preserves cell morphology, and lowers oxidative stress levels, making it a valuable tool for research into neurodegenerative diseases such as Alzheimer's and Parkinson's disease.
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NDs-IN-1 is a non-covalent multi-target inhibitor designed to inhibit the activities of key enzymes including human beta-secretase 1 (hBACE-1), human acetylcholinesterase (hAChE), and human monoamine oxidase B (hMAO-B). This compound is primarily utilized in research focused on neurodegenerative diseases, offering potential avenues for understanding disease mechanisms and developing therapeutic strategies.
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AChE-IN-105 is a potent mixed inhibitor of acetylcholinesterase (AChE) with an IC50 value of 5.02 μM. It exhibits significant antioxidant properties by scavenging reactive oxygen species (ROS) and mitigating hydrogen peroxide-induced activation of Caspase-3, while also downregulating the Nrf2-ARE pathway. In preclinical studies, AChE-IN-105 demonstrated the ability to prevent memory deficits in a zebrafish model of scopolamine-induced cognitive dysfunction. This compound is valuable for research focused on Alzheimer's disease and cognitive impairment mechanisms.
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SCR1693 is a selective, reversible, orally active noncompetitive inhibitor of acetylcholinesterase (AChE), with an IC50 value of 0.68 μM, and exhibits calcium channel blocking properties. This compound effectively reduces tau phosphorylation levels and inhibits the generation and release of amyloid-beta (Aβ). Additionally, SCR1693 has been shown to restore insulin signaling and improve cognitive deficits, making it a valuable tool for studying Alzheimer's disease, particularly in cases complicated by type 2 diabetes mellitus.
MR2938 is a potent acetylcholinesterase (AChE) inhibitor, exhibiting an IC50 of 5.04 μM. In addition to its enzymatic activity, MR2938 significantly reduces nitric oxide production, with an IC50 of 3.29 μM. This compound effectively mitigates neuroinflammation by inhibiting the MAPK/JNK and NF-κB signaling pathways. MR2938 is applicable for research focused on Alzheimer's disease and related neurodegenerative conditions.
AD-35 is a potent acetylcholinesterase (AChE) inhibitor and a metal ion chelating agent, designed for research in Alzheimer’s disease. It demonstrates AChE and butyrylcholinesterase (BuChE) inhibition with IC50 values of 793 nM and 31,428 nM, respectively. AD-35 effectively chelates copper (Cu²⁺) and iron (Fe³⁺) ions, while exhibiting limited interaction with zinc (Zn²⁺). Additionally, AD-35 can inhibit amyloid-beta (Aβ) aggregation, destabilize pre-formed Aβ aggregates, and inhibit Aβ-induced ERK phosphorylation. Its ability to reduce neuroinflammation in rat models of Alzheimer's and improve cognitive performance underscores its potential in therapeutic research.
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Synonyms: (S)-3,7-Dimethyloct-6-en-1-ol
L-Citronellol ((S)-3,7-Dimethyloct-6-en-1-ol) is an ERK/BACE1/PSEN1 inhibitor known for its anti-allergic and neuroprotective properties. This compound effectively inhibits mast cell activation and subsequent release of inflammatory mediators by targeting the ERK pathway. Additionally, L-Citronellol decreases the activity of BACE1, PSEN1, and acetylcholinesterase (AChE), while reducing TNF-α expression and lipid peroxidation, indicating its potential utility in multi-target approaches for Alzheimer's disease research.
