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Explain Why Edrophonium Is A Competitive Inhibitor Of Acetylcholinesterase
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Recommended: Aids and other immunodeficiency
Edrophonium (chloride)
Edrophonium is a competitive inhibitor of acetylcholinesterase (AChE) [1]. AChE is an extrinsic membrane-hound enzyme that functions in the central and peripheral nervous systems. AChE rapidly terminates the ACh receptor-mediated signal transmission by hydrolyzing Ach. Inhibition of AChE results in accumulation of ACh in the synaptic cleft and leads to impeded neurotransmission [2].
In vitro: Edrophonium inhibited 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. The IC50s were 0.2, 0.05, and 0.5 µM, respectively [1].
In vivo: In symptomatic patients without coronary artery disease, edrophonium (80 µg/kg, intravenous bolus)
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