AChE

Polygalacic acid (Virgaureagenin G)(PA) significantly improves cholinergic system reactivity, as indicated by decreased acetylcholinesterase (AChE) activity, increases choline acetyltransferase (ChAT) activity, and elevates levels of acetylcholine (ACh) in the hippocampus and frontal cortex, PA also significantly ameliorates neuroinflammation and oxidative stress in mice; suggest that PA might exert a significant neuroprotective effect on cognitive impairment, driven in part by the modulation of cholinergic activity and neuroinflammation. Polygalacic acid shows significant postingestive effects on Spodoptera littoralis larvae.

Nodakenin ((+)-Marmesinin) is a compound with anti-allergic and anti-inflammatory activities.

DL-Menthol ((±)-Menthol) is a racemic mixture of the monoterpene alcohols (–)-menthol and (+)-menthod, which have been found in Cannabis. (–)-Menthol is more common than (+)-menthol in nature and exhibits analgesic, antibacterial, and anticancer properties, as well as inhibits cholinesterase.2 (+)-Menthol inhibits the growth of F. verticillioides (MIC: 1.5 mM) but, unlike (–)-menthol, does not exhibit analgesic, antibacterial, anticancer, or cholinesterase inhibitory activities.

Diethyltoluamide (DEET) is the most general active composition in insect repellents.

Methyl tridecanoate is a natural product.

AChE/BChE/MAO-B-IN-1 is a reversible, non-time-dependent inhibitor of AChE, BChE and MAO-B that crosses the blood-brain barrier and exhibits inhibitory effects on hAChE, hBChE and hMAO-B with IC50s of 7.31, 0.56 and 26.1 μM, respectively. 1 had a neuroprotective effect and was not significantly cytotoxic.

SEW06622 is a potent inhibitor of acetylcholinesterase (AChE) and beta-secretase-1 (BACE-1) and is a potential candidate for the treatment of Alzheimer's disease.

Histone acetyltransferase p300 Inhibitor 4c is a 2-aminothiazole derivative. Histone acetyltransferase p300 Inhibitor 4c inhibited hCA I, hCA II, AChE and BChE with Ki values of 0.008 ± 0.001, 0.124 ± 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 µM. 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 μM.

1-[10-(pyridin-1-ium-1-yl)decyl]pyridin-1-ium dibromide is the inhibitor of human erythrocyte AChE.

Y13g dihydrochloride is a potent inhibitor of interleukin 6 (IL-6) and acetylcholinesterase (AChE) (both targets of Alzheimer's disease (AD) progression are related). Y13g dihydrochloride reverses STZ-induced memory deficits and exhibits histopathology similar to normal animals.

Desoxypeganine (Deoxypeganine) is an inhibitor of cholinesterase. It acting preferentially on butyrylcholinesterase, and as a selective inhibitor of monoamine oxidase A but not monoamine oxidase B.Desoxypeganine is being developed for its potential utility in the pharmacological treatment of alcohol abuse to reduce craving and depression in alcohol abusers, and might also be useful as a smoking cessation aid.

Rovatirelin (S-0373) is a newly synthesized thyrotropin-releasing hormone (TRH) analog that ameliorates cytosine arabinoside-induced motor dysfunction in a rat model of spinal cerebellar degeneration via acetylcholine and dopamine neurotransmission.

Corysamine chloride (CORYSAMINE CHLORIDE(RG)) was identified to inhibit the activity of ACHE.

(S)-Vamicamide is a novel anticholinergic compound.Vamicamide increases spontaneous locomotor activity in mice at 32 mg/kg or higher (p.o.) and inhibits tonic convulsions in mice at 100 mg/kg.CAS 번호13483-86-1

TA-03 (7-Meota) is a potent inhibitor of AChE in treatment of cognitive manifestation of AD.

Ladostigil (Ladostigil free base) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO) with inhibitory effects on MAO-B and AChE, with IC50 values of 37.1 and 31.8 μM, respectively.Ladostigil possesses anti-inflammatory, antioxidant, and neuroprotective activities, and may be used in studies of depression and Alzheimer's disease.

Jatrorrhizine hydrochloride is a compound extracted from the roots of Berberis vulgaris with neuroprotective, antimicrobial, antiplasmodial, and antioxidant activities.Jatrorrhizine hydrochloride is an orally active and selective inhibitor of acetylcholinesterase (AChE), which inhibits norepinephrine (NE) uptake. It inhibits the uptake of norepinephrine (NE).

Chikusetsusaponin Ib (Chikusetsu saponin Ib) is an inhibitor of AChE and can be used in studies about anti-Alzheimer's diseases.

β-NETA (α-NETA) is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM and is a potent chemokine-like receptor-1 (CMKLR1) antagonist. β-NETA has anti-cancer activity[1][2]. β-NETA weakly inhibits cholinesterase (IC50=84 µM) and acetylcholinesterase (IC50=300 µM).

Vamicamide (FK 176) is a novel anticholinergic compound. Vamicamide increases spontaneous locomotor activity in mice at 32 mg/kg (p.o.) or higher and inhibits cataleptic convulsions in mice at 100 mg/kg.

Donepezil (Aricept) is a piperidine-based, potent, specific, and reversible inhibitor of acetylcholinesterase (AChE). It can be used for the treatment of mild to moderate dementia of the Alzheimer's type.

Pralidoxime Chloride (2-PAM chloride) is a useful agent in the treatment of organophosphate poisoning. Pralidoxime binds to organophosphate-inactivated acetylcholinesterase, used to combat poisoning by organophosphates or acetylcholinesterase inhibitors (nerve agents).

1. Linarin (Acacetin-7-O-rutinoside) (acacetin-7-O-β-d-rutinoside) shows selective dose dependent inhibitory effect on acetylcholinesterase. 2. Linarin alleviates GalN/LPS-induced liver injury by suppressing TNF-α-mediated apoptotic pathways. 3. Linarin prevents A beta-induced neurotoxicity through the activation of PI3K/Akt, which subsequently inhibits GSK-3b and up-regulates Bcl-2. 4. The piperine significantly enhanced the oral absorption of Linarin in rats by inhibiting P-glycoprotein mediated cellular efflux during the intestinal absorption and likely simultaneously by inhibiting the metabolism of Linarin.

Neoeriocitrin is a natural product isolated from Drynaria Rhizome, shows activity on proliferation and osteogenic differentiation in MC3T3-E1. Neoeriocitrin is a potent acetylcholinesterase (AChE) inhibitor.

Diazinon (Dimpylate) is a thiophosphoric acid ester, functioning as a nonsystemic organophosphate insecticide that effectively targets and controls a variety of pests including cockroaches, silverfish, ants, and fleas.

sn-Glycero-3-phosphocholine (Choline glycerophosphate) is a natural choline compound found in the brain and in milk. It is also a parasympathomimetic acetylcholine precursor which may have a potential for the treatment of Alzheimer's disease and dementia. sn-Glycero-3-phosphocholine 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 Glycerylphosphorylcholine 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].

Vincosamide is an alkaloid from Psychotria leiocarpa extract, inhibits the acetylcholinesterase (AChE) activity with anti-inflammatory activity. Vincosamide can effect relaxation of the supercoiled pBR322 plasmid DNA in the presence of Cu2+.

4-Methylbenzylidene camphor is an ultraviolet light blocker used in cosmetics and sunscreen preparations ,specifically UV B radiation, also has estrogenic activities.

Pitofenone hydrochloride (Pitophenone hydrochloride), a spasmolytic compound, inhibits the acetylcholinesterase (AChE) activity from bovine erythrocytes and from electric eel with Kis of 36 and 45 μM, respectively.

Acephate (Orthene) is an anticholinesterase insecticide with a weak inhibitory effect on AChE in rats, but it can effectively inhibit AChE in cockroaches.

Sophoflavescenol is a mixed inhibitor of PDE5 with a K(i) value of 0.005 microM. Sophoflavescenol has antioxidant, anti-inflammatory, and apoptotic effects , these effects might contribute to the antitumor activity without severe side effects. Sophoflaves

AChE-IN-3 had inhibitory effect on AChE and stronger inhibitory effect on NO, with EC50 of 0.57 μM.

(±)-Hexanoylcarnitine chloride is a fatty acid metabolite that breaks down fatty acids into small compounds that can be utilized by the body. (±)-Hexanoylcarnitine chloride can be used as a biomarker of skeletal muscle toxicity in rats through specificity. (±)-Hexanoylcarnitine chloride has cholinergic activity.

Hydroxytacrine maleate (Velnacrine maleate) is a cholinesterase (cholinesterase) inhibitor that enhances memory in rodents and may be used in the study of Alzheimer's dementia of the Alzheimer type (SDAT).

Clozapine N-oxide dihydrochloride is a derivative of Clozapine and an agonist of human muscarinic design receptors (DREADDs) that crosses the blood-brain barrier.Clozapine N-oxide dihydrochloride induces activation of DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride induces activation of DREADD receptors hM3Dq and hM4Di.

(-)-Corynoxidine is an AChE inhibitor derived from tubers of Stephania succifera. Corynoxidine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus strains in different degrees.

1. Picfeltarraenin IB and Picfeltarraenin IA displayes no cytotoxic activity in vitro human tumor cell line panel.

1-Naphthyl acetate is usually used in a rapid staining method for identification of macrophages. 1-Naphthyl acetate is a potent chromogenic substrate for the detection of erythrocyte acetylcholinesterase (AChE) activity. It has the potential to detect organophosphorus pesticide poisoning.

AChE/BuChE-IN-4 is a multi-target AChE/BuChE inhibitor with oral activity and blood-brain barrier permeability, with IC50 values of 2.08 and 7.41 μM for AChE and BuChE, respectively.

Leptomerine (IC50 = 2.5 mM) shows potent anticholinesterasic activity.

(+)-Balanophonin is a natural phenolic compound isolated from Passiflora edulis with antioxidant, anti-inflammatory, anticancer and anti-neurodegenerative activities, cholinesterase inhibition, and marginal inhibition of OPM2 and RPMI-8226 cell proliferation.

CV-6209 is a selective and potent platelet-activating factor (PAF) antagonist with antiproliferative effects, partial inhibition of acetylcholine-induced hypotension, and inhibition of Paf-induced PMN or platelet aggregation.CV-6209 has an antiplasmodial effect against Helicobacter pylori, and can inhibit PAF-induced hypotension in rats.

Simpinicline (OC-02) (OC-02) is a highly selective nicotinic acetylcholine receptor (nAChR) agonist that activates the trigeminal parasympathetic pathway and can be used to treat dry eye.

ML352 is a selective and potent inhibitor of the presynaptic choline transporter (CHT), inhibits non-competitive choline uptake.

Trimyristin (Tritetradecanoin) is primarily located in the membrane (predicted from logP) and adiposome. glyceryl trimyristate exists in all eukaryotes, ranging from yeast to humans. In humans, glyceryl trimyristate is involved in the metabolic disorder called de novo triacylglycerol biosynthesis glyceryl trimyristate pathway.

Itopride hydrochloride (Ganaton) is an AChE and D2DR inhibitor.

Isomerazin (Isomeranzin) has anti-inflammatory activity, it suppresses inflammation by inhibiting M1 macrophage polarization through the p65, NF-κB and ERK pathway.

O-Desmethyl Galanthamine (Sanguinine) is galanthamine-type alkaloid and it is an acetylcholinesterase (AChE) inhibitor, with an IC50 1.83 μM.

Ethyl (triphenylphosphoranylidene) acetate ((Carbethoxymethylene)triphenylphosphorane) may act as an cholinesterase inhibitor that inhibits AChE and BChE.

Fenchlorphos (Dermafos) is a cholinesterase inhibitor, used as an insecticide.