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Synthesis of choline
Hydrolysis of ACh
Acetylation of Choline
1-transmembrane protiens (enzyme associated)
G-protien coupled
Ion Channel
Transcriptional regulators
Hydrolysis of the acetylated enzyme
Diffusion of choline from the active site
Formation of the acetylated enzyme
Binding of ACh to the enzyme to form the transition state
Increase the ethylene bridge by one atom
Addition of beta methyl on ethylene bridge
Replacement of one N-mehtyl with N-ethyl
Replacement of the ester with carbamate
Addition of alpha methyl on ethylene bridge
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Replacement of one N-methyl with N-ethyl
Replacement of the esters with a carbamate
Addition of alpha methyl on ethylene bridge
Increase the ethylene bridge by one atom
Addition of beta methyl on ethylene bridge
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Choline
Serine
S-adenosyl methione
Acetyl-S-CoA
Hydrolysis of ACh
Synthesis of ACh
Synthesis of choline
Oxidation (replace S with O)
Hydrolysis with phosphatases
Hydrolysis of esters
Phosphatase (hydrolyze P-S bond)
Oxidation (replace S with O)
Carboxyesterase (hydrolyze ester)
Only one aging reaction occurs before AChE becomes completely refractory to reactivation.
AChE cannot be reactivated with pralidoxime
It is more lipophilic than other agents so more topical absorption occurs
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Donepezil
Galantamine
Memantine
Rivastigmine
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A
B
C
D
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The receptors in the NMJ have two binding sites of Ach
Thy are voltage regulated ion channels
They are contained on glycoprotiens imbedded in synaptic membranes
The SAR for ligands differs for the receptors in the NMJ and the ganglia
The receptors in the NMJ have a pentameric structure
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