anti-cholinesterase

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

Trihexyphenidyl hydrochloride (Benzhexol hydrochloride) is an antiparkinsonian agent of the antimuscarinic class.

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.

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).

1. Sinapine, an alkaloid from seeds of the cruciferous species, can be used as an effective natural compound for chemo-resistance. 2. Sinapine has antioxidant and radio-protective activities.

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+.

Pseudocoptisine chloride (Isocoptisine chloride) is isolated from Corydalis Tuber with anti-inflammatory and anti-amnestic properties. Pseudocoptisine chloride inhibits acetylcholinesterase (AChE) activity (IC50 = 12.8 μM).

Atherosperminine shows cholinesterase inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Atherosperminine shows strong anti-plasmodial activity against Plasmodium falciparum, with the IC50 value of 5.80 uM, it also s

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

α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. It is a potent ALDH1A1 (IC50 =0.04 μM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50 =84 μM) and acetylcholinesterase (AChE; IC50 =300 μM). α-NETA has anti-cancer activity [1] [2].

Ladostigil hemitartrate (TV-3326) is a dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50 values of 37.1 μM for MAO-B and 31.8 μM for AChE. Possessing neuroprotective, antioxidant, and anti-inflammatory properties, it is commonly used in research related to depression and Alzheimer's disease.

Garcinol also inhibits histone acetyltransferases (HATs, IC50= 7 μM) and p300 CPB-associated factor (PCAF, IC50 = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity. Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 0.66 μM and 7.39 μM, respectively.

Sinapine Thiocyanate, is a derivative of Sinapine (S486605), an alkaloidal amine found in black mustard seeds. It is the choline ester of Sinapic Acid (S486800). It is also a phenolic-chloine conjugates, acting as anti-oxidants and acetylcholinesterase inhibitors, that can be used for the treatment of Alzheimer's disease (AD).

Silatrane is a reversible cholinesterase inhibitor and anti-tumor agent.

Manghaslin (Quercetin 3-O-rutinoside-(1->2)-O-rhamnoside) has considerable α-glucosidase inhibitory activity, illustrating the anti-diabetic potential of phenolic-rich litchi pulp extracts. Manghaslin also shows inhibitory activity against AChE

(-)-Huperzine A (HupA) , an active Lycopodium alkaloid extracted from the 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).

Ladostigil hydrochloride (TV-3326), an orally active compound, acts as a dual inhibitor targeting both cholinesterase and brain-selective monoamine oxidase (MAO), demonstrating inhibition constants (IC50s) of 31.8 μM for acetylcholinesterase (AChE) and 37.1 μM for MAO-B. This compound exhibits neuroprotective, antioxidant, and anti-inflammatory properties, making it useful for research into depression and Alzheimer's disease.

2',4'-Dihydroxy-3',6'-dimethoxychalcone possesses cytotoxic, anti-inflammatory, and anti-cholinesterase activities, and demonstrates significant NO inhibitory activity.

Ovotransferrin (328-332), with an IC50 of 20 μM, exhibits protective activity against hypertension by inhibiting the Angiotensin-Converting Enzyme (ACE) and also displays anti-Cholinesterase (ChE) activity, suggesting a potential role in the treatment of Alzheimer's disease [1] [2].

(+)-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.