cholinesterase (che)

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).

Coumaran (2,3-Dihydrobenzofuran), an acetylcholinesterase (AChE) inhibitor isolated from the leaves of L. camara, can be used as a biopesticide and belongs to the class of 1-benzofurans as the 2,3-dihydro derivative of benzofuran with a role as a metabolite.

Galanthamine hydrobromide (Galantamine hydrobromide), a long-acting and centrally active AChE inhibitor (IC50:410 nM), is an allosteric potentiator at neuronal nicotinic ACh receptors.

Drofenine hydrochloride (Hexahydroadiphenine hydrochloride) is an effective competitive inhibitor of BChE (Ki value: 3 uM).

Pyridostigmine bromide (Mestinon) is a cholinesterase inhibitor with a slightly longer duration of action than NEOSTIGMINE. It is used in the treatment of myasthenia gravis and to reverse the actions of muscle relaxants.

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).

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

Neostigmine methyl sulfate (Syntostigmin) is a reversible inhibitor of acetylcholinesterase, can not cross the blood-brain barrier, used in the treatment of myasthenia gravis.

Neostigmine bromide is a cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike PHYSOSTIGMINE, does not cross the blood-brain barrier.

Rivastigmine tartrate (SDZ-ENA 713) is a carbamate-derived reversible CHOLINESTERASE INHIBITOR that is selective for the CENTRAL NERVOUS SYSTEM and is used for the treatment of DEMENTIA in ALZHEIMER DISEASE and PARKINSON DISEASE.

Azamethiphos, an organothiophosphate insecticide, is used in Atlantic salmon fish farming to control parasites.

Tacrine (CS 12602) is an indirect cholinergic agonist and centrally acting anticholinesterase. It is approved for the treatment of Alzheimer's disease.

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

Acotiamide monohydrochloride trihydrate (Z-338 HCl) is the hydrochloride salt form of acotiamide, a prokinetic agent with gastrointestinal (GI) motility-enhancing activity. Although the exact mechanism by which acotiamide exerts its effect has yet to be fully elucidated, this agent appears to inhibit acetylcholinesterase (AchE), an enzyme responsible for the breakdown of acetylcholine (Ach). Increased Ach concentrations lead to an improvement of gastric emptying and GI motility and eventually to a reduction of dyspepsia symptoms.

Benactyzine hydrochloride (Neuroleptone) is a centrally acting muscarinic antagonist. Benactyzine has been used in the treatment of depression and is used in research to investigate the role of cholinergic systems on behavior.

Imperatorin (8-Isopentenyloxypsoralene) is a modulator of p38, ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density/volume and mineralization in vivo.

Scopoletin (Esculetin 6-methyl ether) is a plant growth factor derived from the root of Scopolia carniolica, inhibits of acetylcholinesterase (AChE).

1. Isoeugenol acetate (Acetylisoeugenol) shows good antifungal activities against R. solani and F. oxysporum. 2. Isoeugenol acetate is a mild sensitizer in vivo.

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].

Donepezil HCl(Aricept) is a selective and effective AChE inhibitor for bAChE and hAChE (IC50: 8.12/11.6 nM).

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

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.

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

Methyl tridecanoate is a natural product.