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Acetylcholinesterase (1). Sites of location Cholinergic neurons Cholinergic synapses Neuromuscular junction Red blood cells Substrates Acetylcholine is the best substrate Methacholine is a substrate

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Acetylcholinesterase (1)

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Acetylcholinesterase (1)

Sites of location

Cholinergic neurons

Cholinergic synapses

Neuromuscular junction

Red blood cells

Substrates

Acetylcholine is the best substrate

Methacholine is a substrate

Hydrolyzes ACh at greater velocity than choline esters with acyl groups larger than acetate or proprionate


Acetylcholinesterase (2)

Esters that are not substrates

Bethanechol

Carbachol

Succinylcholine

Its inhibition produces synergistic interaction with methacholine and additive actions with bethanechol and carbachol

Drugs that block its hydrolysis of esters are called cholinesterase inhibitors


Drug Interactions of Choline Esters and Inhibitors of Acetylcholinesterase - SynergismversusAdditivity

Methacholine

Carbachol

Bethanechol


Butyrylcholinesterase

(Plasma esterase, pseudocholinesterase, serum esterase, BuChE, PseudoChE)


Butyrylcholinesterase (1)

Sites of location

Plasma, liver, glial cells, other tissues

Substrates

Butyrylcholine is the best

Acetylcholine

Succinylcholine

Procaine


Butyrylcholinesterase (2)

Esters that are not substrates

Methacholine, bethanechol, and carbachol

Is inhibited by carbamyl and organophosphate inhibitors of acetylcholinesterase


Active Site of Acetylcholinesterase


Interaction of AChE and Acetylcholine


Acetylation of AChE and Release of Choline


Hydroxyl Group of Water Attacks the Carbonyl Group of Acetylated-AChE to Liberate AChE


Carbamyl Inhibitors of AChE


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