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Edrophonium (chloride) is an acetylcholinesterase (AChE) inhibitor that is known to prevent the breakdown of the neurotransmitter acetylcholine by binding specifically to its catalytic site.1 It has been shown to inhibit AChE activity in human red blood cells, purified calf forebrain, and purified octopus brain with Ki values of 0.2, 0.2, and 0.4 µM, respectively.2 Edrophonium is often used as part of a battery of pharmacological tests to confirm a diagnosis of the autoimmune neuromuscular junction disorder, myasthenia gravis.3
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1. Acetylcholinesterase: Specificity of the peripheral anionic site for cholinergic ligands. Mol. Pharmacol. 11(3), 352-360 (2011).
2. Synthesis and study of thiocarbonate derivatives of choline as potential inhibitors of acetylcholinesterase. J. Med. Chem. 40(19), 3009-3013 (1997).
3. Myasthenia gravis. Orphanet J. Rare Dis. 2, 44 (2007).