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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.
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.
Fenitrothion-d6 is a deuterium-labeled analog of Fenitrothion, a broad-spectrum insecticide and acaricide that functions primarily by inhibiting cholinesterase, AMPKα, and the IRS1/PI3K/AKT signaling pathway. This compound exhibits apoptosis-inducing properties and reduces superoxide dismutase (SOD) activity, contributing to its biological efficacy. Fenitrothion is effective against pests such as Rhyzopertha dominica and Tribolium castaneum, making it valuable for agricultural applications in crops like cotton, vegetables, and rice. Additionally, it serves as a useful tool for toxicological studies in brain and spleen tissues.
Fenitrothion is an organophosphorus pesticide that primarily targets cholinesterase, along with AMPKα and IRS1/PI3K/AKT pathways. It exhibits significant insecticidal and acaricidal activity, effectively controlling pests such as Rhyzopertha dominica and Tribolium castaneum adults. This compound is widely utilized in agriculture for cotton, vegetable, fruit, and field crops, particularly rice. Additionally, Fenitrothion serves as a valuable tool for toxicological studies related to brain and spleen function.
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.
Synonyms: Buddleoside; Linarine
Linarin is a selective inhibitor of acetylcholinesterase (AChE), demonstrating oral bioavailability. This compound exhibits a range of biological activities, including anti-inflammatory, antioxidant, sedative, and antibacterial properties. Linarin is valuable for research in neurological disorders, osteoporosis, and cancer, providing insights into potential therapeutic applications across these areas.
BChE/HDAC6-IN-2 is a potent dual inhibitor targeting both butyrylcholinesterase (BChE) and histone deacetylase 6 (HDAC6), demonstrating IC50 values of 1.8 nM and 71.0 nM, respectively. This compound exhibits significant neuroprotective properties and scavenges reactive oxygen species (ROS), alongside effectively chelating metal ions such as Fe2+ and Cu2+. Furthermore, BChE/HDAC6-IN-2 inhibits tau phosphorylation and presents moderate immunomodulatory effects, making it a valuable reagent for research into neurodegenerative diseases and related pathways.
AChE/HDAC-IN-1 is a potent dual inhibitor of acetylcholinesterase (AChE) and histone deacetylases (HDAC) with IC50 values of 0.12 nM and 0.23 nM, respectively. This compound also demonstrates antioxidant activity and metal chelating properties, making it a valuable tool in understanding neurodegenerative processes. AChE/HDAC-IN-1 is suitable for research applications related to Alzheimer's disease and other conditions associated with cholinergic dysfunction and epigenetic modifications.
HDAC6-IN-5 is a potent inhibitor of histone deacetylase 6 (HDAC6), demonstrating an IC50 of 0.025 μM. This compound effectively inhibits the self-aggregation of amyloid-beta 1-42 and acetylcholinesterase (AChE), with IC50 values of 3.0 μM and 0.72 μM, respectively. HDAC6-IN-5 has been shown to promote neurite outgrowth while exhibiting minimal neurotoxicity, making it a valuable tool for research in neurodegenerative disease and neuronal regeneration studies.
HDAC6-IN-6 is a potent inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 of 0.025 μM. This compound is capable of crossing the blood-brain barrier and demonstrates strong inhibitory activity against amyloid-beta peptide (Aβ1-42) self-aggregation and acetylcholinesterase (AChE) with IC50 values of 3.0 μM and 0.72 μM, respectively. Additionally, HDAC6-IN-6 enhances neurite outgrowth while maintaining a favorable safety profile, making it a valuable tool for research in neurodegenerative diseases and related fields.
BChE/HDAC6-IN-1 is a selective dual inhibitor targeting both butyrylcholinesterase (BChE) and histone deacetylase 6 (HDAC6), with IC50 values of 4 nM and 8.9 nM, respectively. This compound demonstrates significant potential in ameliorating cognitive impairment in an Aβ1–42-induced mouse model, making it a valuable tool in Alzheimer's disease research. Its ability to modulate both cholinergic and epigenetic pathways positions BChE/HDAC6-IN-1 as a promising candidate for studies focused on neurodegenerative disorders.
Synonyms: Nymphaeol A; Propolin C
Diplacone is a geranylated flavanone derived from the unripe fruits of Paulownia tomentosa. It exhibits significant anti-inflammatory, antiradical, cytoprotective, antibacterial, and anticancer properties. Diplacone induces ferroptosis-mediated cell death through mechanisms involving increased mitochondrial Ca2+ influx, reactive oxygen species (ROS) production, and mitochondrial permeability transition. Additionally, it effectively inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activity, making it valuable for research into chronic inflammatory diseases, cancers, and neurological disorders such as Alzheimer's disease.
Penconazole-d7 is a deuterium-labeled derivative of Penconazole, a triazole fungicide primarily utilized for the management of powdery mildew in crops such as apples, grapes, and vegetables. This compound exerts its biological activity by inhibiting sterol biosynthesis in fungi, thereby disrupting cell membrane integrity. Additionally, Penconazole has been shown to decrease acetylcholinesterase (AChE) activity in the cerebrum and cerebellum of rat models, making it relevant for neurobiological research applications.
Iprobenfos is an organophosphorus fungicide primarily targeting the rice blast fungus. Its mechanism involves the phosphorylation of the -OH group on serine residues located within the active site of cholinesterases, leading to the inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities. This compound is significant in agricultural research for its role in managing fungal diseases in crops and understanding the interaction of organophosphorus compounds with cholinergic systems.
Synonyms: β-Amyron
β-Amyrone is a triterpene compound recognized for its anti-inflammatory properties, primarily through the inhibition of cyclooxygenase-2 (COX-2) expression. It demonstrates significant antifungal activity and exhibits antiviral effects against the Chikungunya virus. Additionally, β-Amyrone inhibits α-glucosidase and acetylcholinesterase (AChE) activities, making it a valuable compound for research in inflammation, infectious diseases, and obesity-related studies.
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Penconazole is a triazole fungicide that targets sterol biosynthesis in fungi, effectively inhibiting their growth. It is primarily utilized in the agricultural sector for the control of powdery mildew on crops such as apples, grapes, and various vegetables. Additionally, studies indicate that Penconazole may reduce acetylcholinesterase (AChE) activity in the cerebrum and cerebellum of rats, suggesting potential implications for neurobiological research.
T 82 is a potent 5-HT3 receptor antagonist that also functions as an acetylcholinesterase (AChE) inhibitor. This compound exhibits significant biological activity relevant for modulating neurotransmitter signaling in the central nervous system. T 82 is primarily utilized in research related to neurodegenerative diseases, including Alzheimer's Disease, making it a valuable tool in understanding the pathophysiology and treatment approaches for related conditions.
Synonyms: RS-1259
BGC-201259 is a potent and orally active inhibitor of acetylcholinesterase (AChE) and serotonin transporter (SERT), with IC50 values of 101 nM and 42 nM, respectively. Additionally, it inhibits the 5-HT receptor with an IC50 of 90 nM. BGC-201259 exhibits varying activity against several targets, including the norepinephrine transporter (IC50 = 7.7 μM), L-type calcium channel (IC50 = 3.6 μM), σ receptor (IC50 = 2 μM), and sodium channel (IC50 = 5.1 μM). This compound shows promise in research related to Alzheimer's disease by potentially enhancing cognitive and emotional functions through its dual-targeting mechanism.
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Flucopride is an AChE inhibitor with an IC50 of 24 nM, demonstrating significant potency in acetylcholinesterase modulation. Additionally, it acts as a partial agonist at the 5-HT4 receptor with a binding affinity (Ki) of 9.6 nM. Flucopride facilitates non-amyloidogenic processing of amyloid precursor protein (APP) in COS-7 cells expressing the human 5-HT4 receptor, with an EC50 of 23.0 nM. Its properties suggest effective gastrointestinal tract penetration and the capability to cross the blood-brain barrier, as indicated by PAMPA assay results, making it relevant for neuropharmacology research.
α-NETA is a potent noncompetitive inhibitor of choline acetyltransferase (ChA), exhibiting an IC50 value of 9 μM. Additionally, it displays strong antagonistic activity against aldehyde dehydrogenase 1A1 (ALDH1A1) with an IC50 of 0.04 µM and also targets chemokine-like receptor-1 (CMKLR1). While it shows some inhibitory effects on cholinesterase (ChE) and acetylcholinesterase (AChE) with higher IC50 values, α-NETA is notable for its anti-cancer properties, making it a valuable tool for research in cancer biology and neuropharmacology.
