cholinesterase (che)

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.

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.

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.

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

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 (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.

Galanthaminone ((-)-Narwedine) is a cholinesterase (AChE) inhibitor, is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments.

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

Physostigmine, a parasympathomimetic alkaloid, is a reversible cholinesterase inhibitor. It extracts from the Calabar bean.

Protriptyline Hydrochloride is the hydrochloride salt form of protriptyline, a tricyclic secondary amine with an antidepressant property. Protriptyline hydrochloride (Protriptyline HCl) blocks the re-uptake of norepinephrine and serotonin by nerve terminals, thereby increasing available norepinephrine and serotonin. In addition, this agent exhibits anticholinergic activity.

Galanthamine N-Oxide, an alkaloid extracted from Zephyranthes concolor bulbs, effectively inhibits acetylcholinesterase (AChE) from electric eel with an EC50 of 26.2 μM. It acts as a significant inhibitor of substrate accommodation within the active sites of Torpedo californica AChE (TcAChE), human AChE (hAChE), and human BChE (hBChE) enzymes.

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.

Violanthin is a natural product isolated from the aerial parts of Piper bavinum and inhibits acetylcholinesterase (AChE) (IC50: 79.80 μM). It has potent antioxidant and antibacterial activities.

Epi-galantamine, a diastereomer of galantamine, is an alkaloid extracted from the bulbs and flowers of the Caucasian snowdrop (Galanthus woronowii). It acts as an AChE inhibitor, featuring an EC50 of 45.7 μM.