ACETYLCHOLINESTERASE (EC 3.1.1.7, AChE), also known as RBC cholinesterase, is found primarily in the blood and neural synapses. AChE catalyzes the hydrolysis of the neurotransmitter acetylcholine into choline and acetic acid, a reaction necessary to allow a cholinergic neuron to return to its resting state after activation. Inhibition of the enzyme leads to acetylcholine accumulation, hyperstimulation of nicotinic and muscarinic receptors, and disrupted neurotransmission. AChE inhibition is an important target for the management of Alzheimer's disease and AChE inhibitors are the most common drugs used for its management. In addition to Alzheimer's disease, AChE inhibitors have been useful in the diagnosis or treatment of diseases such as glaucoma, myasthenia gravis, bladder distention, and more. BioAssay Systems' QuantiChromTM Acetylcholinesterase Inhibitor Screening kit is based on an improved Ellman method, in which thiocholine produced by the action of acetylcholinesterase forms a yellow color with 5,5'-dithiobis(2-nitrobenzoic acid). The intensity of the product color, measured at 412 nm, is proportionate to the enzyme activity in the sample.
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Applications
HTS for inhibitor screening and evaluation of acetylcholinesterase inhibitors by a colorimetric (412nm) method.