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21 Cards in this Set

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Which amino acid residues located in the active site of acetylcholinesterase create the anionic site and how do they accomplish this?
Trp 86 and Phe 338; the pi-stacking interactions create a negative environment (anionic site)
What type of esterase is acetylcholinesterase?
It's a serine esterase with a similar mechanism to chymotrypsin.
How does atropine work in nerve gas treatment?
It blocks muscarinic ACh receptors from the excess ACh present after AChE inhibition by nerve gases.
How does pralidoxime chloride work in nerve gas treatment?
The potent alpha group nucleophile mimics ACh and can reactivate nicotinic ACh receptors.
What is the most common treatment for nerve gas poisoning?
Duo-dote of atropine and pralidoxine chloride.
What is an alpha group?
Two heteroatoms right next to each other.
What is theory behind using AChE inhibitors in Alzheimer's Disease?
It will increase the concentration of ACh in the synapse to make up for a loss of ACh receptors.
Which amino acid residue located in the active site of acetylcholinesterase acts as a nucleophile?
Serine 203
Do carbamates bind covalently to acetylcholinesterase?
Yes.
What type of acetylcholinesterase inhibitor can be used prior to nerve gas exposure to prevent binding?
Carbamates.
True or False: Carbamates cannot compete with irreversible acetylcholinesterase inhibitors.
False.
Why is the oxygen of a carbamate group always conjugated in acetylcholinesterase inhibitors?
It makes the carbamate more electrophilic and thus a better substrate for the serine nucelophile of AchE.
What type of acetylcholinesterase inhibitors bind reversibly to the anionic site?
Amino groups, or ammonium groups.
What functional groups on organophosphate drugs make them resistant to detoxification?
The ester groups.
What is the main role of acetylcholinesterase?
To regulate the concentration of Ach in the synapse.
What is an "aged enzyme"?
This occurs when an organophosphate drug (such as a nerve agent) bound to acetylcholinesterase deteriorates and become completely irreversible.
What does the DuoDote consist of?
Atropine and pralidoxime chloride
What are some examples of nerve agents?
Sarin, VX, Soman and Tabun
What is the functional group in pralidoxime chloride that undergoes the alpha effect?
Oxime
How is toxicity of insecticides achieved?
The sulfur is oxidized to O, creating a toxic organophosphate in insects.
Are carbamates considered reversible?
Yes, they are slowly reversible.