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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
Acetylcholinesterase (1)

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Acetylcholinesterase 1 l.jpgSlide 1

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 l.jpgSlide 2

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

Slide3 l.jpgSlide 3

Drug Interactions of Choline Esters and Inhibitors of Acetylcholinesterase - SynergismversusAdditivity

Methacholine

Carbachol

Bethanechol

Butyrylcholinesterase l.jpgSlide 4

Butyrylcholinesterase

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

Butyrylcholinesterase 1 l.jpgSlide 5

Butyrylcholinesterase (1)

Sites of location

Plasma, liver, glial cells, other tissues

Substrates

Butyrylcholine is the best

Acetylcholine

Succinylcholine

Procaine

Butyrylcholinesterase 2 l.jpgSlide 6

Butyrylcholinesterase (2)

Esters that are not substrates

Methacholine, bethanechol, and carbachol

Is inhibited by carbamyl and organophosphate inhibitors of acetylcholinesterase

Active site of acetylcholinesterase l.jpgSlide 7

Active Site of Acetylcholinesterase

Interaction of ache and acetylcholine l.jpgSlide 8

Interaction of AChE and Acetylcholine

Acetylation of ache and release of choline l.jpgSlide 10

Acetylation of AChE and Release of Choline

Hydroxyl group of water attacks the carbonyl group of acetylated ache to liberate ache l.jpgSlide 11

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

Carbamyl inhibitors of ache l.jpgSlide 12

Carbamyl Inhibitors of AChE


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