Piperilate (Pipethanate) is one of the mixtures of hetrazepine derivative PAF antagonists with anticholinergics, can be used for bronchial asthma research. Piperilate also causes hypotension and rescues mice poisoned by the organophosphates[1][2][3].
A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 0.12 uM, >400-fold selectivity over ChoKβ; demonstrates in vitro antiproliferative activity against HT29 cells with IC50 of 2.08 uM.
Fmoc-L-Val-OH-13C5,15N is a 15N-labeled and 13C-labled Pirimicarb. Pirimicarb is a fast-acting selective carbamate insecticide on a wide range of crops including cereals, sugar beet, potatoes, fruits and vegetables. Pirimicarb is an AChE inhibitor and an
Hemicholinium 3 is a competitive inhibitor of the high affinity choline transporter (HACU) with a Ki value of 25 nM. Hemicholinium 3, a neuromuscular blocking agent which inhibits the synthesis and the release of acetylcholine (ACh)[1]. Hemicholinium 3 inhibits the Epibatidine-evoked contraction and [3H]acetylcholine release with IC50s of 897 nM and 693 nM, respectively[2].
sEH inhibitor-5 (compound D016) is a potent sEH (soluble epoxide hydrolase) inhibitor with an IC50 value of 0.1 nM[1].
Desoxypeganine (Deoxypeganine), an alkaloid, is a potent and orally active cholinesterase (BChE and AChE) and selective MAO-A inhibitor, with IC50 values of 2, 17, and 2 μM, respectively. Desoxypeganine can be used for alcohol abuse research[1].
Ladostigil (TV-3326) hydrochloride is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hydrochloride exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease[1][2].
L-Alpha glycerylphosphorylcholine (alpha-GPC, choline alfoscerate) is a natural choline compound found in the brain and in milk. It is also a parasympathomimetic acetylcholine precursor which may have potential for the treatment of Alzheimer's disease and dementia.IC50 value:Target: Anti-ADAlpha-GPC rapidly delivers choline to the brain across the blood–brain barrier and is a biosynthetic precursor of the acetylcholine neurotransmitter. It is a non-prescription drug in most countries due to its Generally Recognised As Safe (GRAS) status [1]. Studies have investigated its efficacy for cognitive disorders including stroke and Alzheimer’s disease. An Italian multicentre clinical trial on 2,044 patients suffering from recent stroke were supplied alpha-GPC in doses of 1,000 mg/day for 28 days and 400 mg three times per day for the five ensuing months. The trial confirmed the therapeutic role of alpha-GPC on the cognitive recovery of patients based on four measurement scales, three of which reached statistical significance [2].
Acotiamide hydrochloride is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide hydrochloride can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide hydrochloride has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory[1][2][3].
Lycoramine, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine is a potent acetylcholinesterase (AChE) inhibitor[1][2].
AChE/BuChE-IN-2 (Compound 5f) is an orally active AChE and BuChE inhibitor with IC50 values of 0.72 μM and 0.16 μM, respectively. AChE/BuChE-IN-2 shows a non-competitive inhibition with AChE and shows potent self-induced β-amyloid (Aβ) aggregation inhibition with an IC50 of 62.52 μM. AChE/BuChE-IN-2 can cross the BBB[1].
Malathion is an organophosphate parasympathomimetic which binds irreversibly to cholinesterase, is an insecticide of relatively low human toxicity.
Fosthiazate is a broad-spectrum nematicide against various plant parasitic nematodes, including Meloidogyne spp., Globodera spp., and Pratylenchus spp., through inhibiting the synthesis of acetylcholinesterase[1].
Dehydronuciferine is isolated from the leaves of Nelumbo nucifera Gaertn, a acetylcholinesterase (AChE) inhibitor with an IC50 of 25 μg/mL[1].
AChE/BChE-IN-3 (BMC-1) is a dual AChE and BChE inhibitor with IC50 values of 6.08 μM and 0.383 μM against electric eel AChE (elAChE) and equine serum BChE (eqBChE), respectively[1].
Dehydrogeijerin is an inhibitor of acetylcholinesterase with an IC50 of 9.7 μM. Dehydrogeijerin can be used in study Alzheimer’s disease[1].
HDAC6-IN-6 (compound 6a) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-6 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-6 can enhance neurite outgrowth without significant neurotoxicity[1].
Penconazole is a typical triazole fungicide, and mainly applied on apples, grapes, and vegetables to control powdery mildew. Penconazole inhibits sterol biosynthesis in fungi. Penconazole decrease AChE activity in the cerebrum and cerebellum of rats[1][2].
Pralidoxime iodide is a reactivator of acetylcholinesterase (AChE). Pralidoxime iodide reactivates nerve agent, which inhibits AChE via direct nucleophilic attack by the oxime moiety on the phosphorus center of the bound nerve agent. Pralidoxime iodide is an antidote for organophosphate poisoning[1][2].
Cyanidin-3-O-galactoside chloride (Ideain chloride) is a component from extract peel of hawthorn fruit (EPHF) with the value of 179.4 mg/g. EPHF exhibits strong AChE inhibitory activity[1].
AChE-IN-27 (compound 8c) is an AChE inhibitor (IC50=0.19 µM). AChE-IN-27 can be used in studies of neurological diseases such as alzheimer's disease, dementia, ataxia and myasthenia gravis[1].
AChE/BChE-IN-9 (Compound 7a) is a potent, orally active AChE and BChE inhibitor with IC50 values of 5.74 μM and 14.05 μM against hAChE and eqBChE, respectively. AChE/BChE-IN-9 is also an efficacious antioxidant with an IC50 of 57.35 μM. AChE/BChE-IN-9 is able to chelate iron and modulates aggregation of amyloid β1-42. AChE-IN-16 can cross the BBB[1].
COX-2-IN-22 (Compound 4h) is a COX-2 inhibitor with an IC50 of 8.6 µM. COX-2-IN-22 also inhibits AChE, BChE, β-Secretase, LOX-5 and DPPH with IC50 values of 2.8, 6.3, 15.3, 13.9 and 6.8 µM, respectively. COX-2-IN-22 can cross BBB[1].
1-Naphthyl acetate is an attractive chromogenic substrate for the detection of erythrocyte acetylcholinesterase (AChE) activity. 1-Naphthyl acetate has the potential to detect organophosphorus pesticide (OP) poisoning[1].
AChE-IN-14 is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease[1].
Coumaran (2,3-Dihydrobenzofuran) is an acetylcholinesterase (AChE) inhibitor isolated from leaves of L. camara. Coumaran can be used as a biopesticide[1].
Methyl tridecanoate moderately inhibits β-amyloid aggregation. Methyl tridecanoate weakly inhibits acetylcholinesterase (AChE)[1].
Z164597606 is a selective BChE inhibitor (IC50: 1.3 and 1.7 μM for eqBChE and hBChE). Z164597606 forms a π-π stacking interaction with the amino acid Trp82 of hBChE. Z164597606 can be used for the research of Alzheimer’s disease (AD)[1][2].
(R)-Rivastigmine D6 (tartrate) is the deuterium labeled (R)-Rivastigmine, which is an cholinesterase inhibitor.
(R)-Donepezil is a R-enantiomer of Donepezil (HY-14566). Donepezil is a specific and potent AChE inhibitor[1][2].