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Acetylcholinesterase (1) Sites of location  Cholinergic neurons  Cholinergic synapses  Neuromuscular junction  Red blood cells Substrates  Acetylcholine.

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Presentation on theme: "Acetylcholinesterase (1) Sites of location  Cholinergic neurons  Cholinergic synapses  Neuromuscular junction  Red blood cells Substrates  Acetylcholine."— Presentation transcript:

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

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

3 Drug Interactions of Choline Esters and Inhibitors of Acetylcholinesterase - Synergism versus Additivity Methacholine Carbachol Bethanechol

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

5 Butyrylcholinesterase (1) Sites of location  Plasma, liver, glial cells, other tissues Substrates  Butyrylcholine is the best  Acetylcholine  Succinylcholine  Procaine

6 Butyrylcholinesterase (2) Esters that are not substrates  Methacholine, bethanechol, and carbachol Is inhibited by carbamyl and organophosphate inhibitors of acetylcholinesterase

7 Active Site of Acetylcholinesterase

8 Interaction of AChE and Acetylcholine

9

10 Acetylation of AChE and Release of Choline

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

12 Carbamyl Inhibitors of AChE


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