Cholinesterase inhibitor

Cholinesterase inhibitors (ChEIs), also known as anti-cholinesterase, are chemicals that prevent the breakdown of the neurotransmitter acetylcholine or butyrylcholine by cholinesterase. This increases the amount of the acetylcholine or butyrylcholine in the synaptic cleft that can bind to muscarinic receptors, nicotinic receptors and others. This group of inhibitors is divided into two subgroups, acetylcholinesterase inhibitors (AChEIs) and butyrylcholinesterase inhibitors (BChEIs).

Medical use

While 4 ChEIs are approved in the US for the treatment of Alzheimer's Disease, only three of these are available commercially. Neostigmine is used in combination with a muscarinic antagonist to reverse the effects of non-depolarizing muscle relaxants e.g. rocuronium bromide ==Cholinesterase inhibitor toxicity==

Cholinesterase inhibitor toxicity

Common side effects of one ChEI include insomnia, nausea and vomiting, accidental injury, headache, dizziness, bradycardia, hypotension, ecchymosis, and sleep disturbance. ==Binding affinity==

Binding affinity

Acetylcholinesterase inhibitors Donepezil, phenserine, huperzine A, and BW284c51 are selective AChE inhibitors. Butyrylcholinesterase inhibitor Tetra (monoisopropyl) pyrophosphoramide (Iso-OMPA) and ethopropazine are selective BChE inhibitors. Acetylcholinesterase inhibitors and nicotinic receptor modulator Galantamine might be less well tolerated than donepezil and rivastigmine. == Chemical weapons ==

Chemical weapons

Assassination Attempt Cholinesterase inhibitors came to a public attention in 2020 when Russian opposition and dissent figure Alexei Navalny was treated in Berlin Charité hospital for poisoning by a Russian-made nerve agent which is known since 2019 as belonging to the Novichok agents subgroup of ChEI. ==See also==

Source: Wikipedia ↗

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