Podcast
Questions and Answers
Why is protection needed for muscarinic agonists, but not the natural ligand acetylcholine?
Why is protection needed for muscarinic agonists, but not the natural ligand acetylcholine?
- The muscarinic agonists exhibit inhibitory features that attract ubiquitous esterases, thus making them need protection. Whereas ACh has its own protection.
- The muscarinic agonists enter the body from outside. This makes them vulnerable to ubiquitous esterases. Therefore, the drug must be protected. ACh is localized in the synapse and will not contact any esterases - therefore no protection needed. (correct)
- The muscarinic agonists are able to be inhibited by amides and carbamates. This makes them need protection, which comes from esterases. ACh is able to be destroyed by esterases, which allows them to be rebuilt, stronger.
- Muscarinic agonists have certain structures that are easily engulfed by degrading enzymes. Thus, they will need to be protected. ACh is already localized in the cardiovascular region.
Which drug mimics ACh and binds to the cholinergic receptor?
Which drug mimics ACh and binds to the cholinergic receptor?
- Muscarinic Antagonist
- Nicotinic Agonist
- Cholinergic Inhibitors
- Muscarinic Agonist (correct)
Which drug binds to the cholinergic receptor, but produces no signal transduction?
Which drug binds to the cholinergic receptor, but produces no signal transduction?
- Muscarinic Antagonist (correct)
- Muscarinic Agonist
- Nicotinic Agonist
- Cholinergic Inhibitor
What should happen in order to increase a drug's half-life?
What should happen in order to increase a drug's half-life?
What should happen to further increase the half-life of a drug which already requires hepatic metabolism?
What should happen to further increase the half-life of a drug which already requires hepatic metabolism?
Which of the following is NOT something that the nature of the amine determines?
Which of the following is NOT something that the nature of the amine determines?
What does an alkyl linker provide?
What does an alkyl linker provide?
What is a difference between Muscarinic Agonist vs. Antagonist structures?
What is a difference between Muscarinic Agonist vs. Antagonist structures?
What change can occur to ACh so the resulting compound exhibits agonistic activity?
What change can occur to ACh so the resulting compound exhibits agonistic activity?
What change can NOT occur to ACh so the resulting compound exhibits antagonist activity?
What change can NOT occur to ACh so the resulting compound exhibits antagonist activity?
What kind of biological effect will acetylcholinesterase inhibitors have?
What kind of biological effect will acetylcholinesterase inhibitors have?
What is the makeup of the anionic site of mAChR?
What is the makeup of the anionic site of mAChR?
What is the makeup of the 'anionic' site of AChE?
What is the makeup of the 'anionic' site of AChE?
Why is echothiopate suitable for application in humans?
Why is echothiopate suitable for application in humans?
Match the following regarding measures in the metabolism of malathion that are exploited.
Match the following regarding measures in the metabolism of malathion that are exploited.
Why can ProPam pass the BBB in contrast to 2-PAM?
Why can ProPam pass the BBB in contrast to 2-PAM?
The electrophilicity of the phosphorous prevents the hydrolysis of the phosphorylated serine, which stops the regeneration of the enzyme - is the reaction why organophosphate AChEIs into quasi-irreversible inhibitors?
The electrophilicity of the phosphorous prevents the hydrolysis of the phosphorylated serine, which stops the regeneration of the enzyme - is the reaction why organophosphate AChEIs into quasi-irreversible inhibitors?
Which CYP enzyme is responsible for N-dealkylation and aromatic hydroxylation?
Which CYP enzyme is responsible for N-dealkylation and aromatic hydroxylation?
Which enzyme is responsible for converting a tertiary amine to an N-oxide?
Which enzyme is responsible for converting a tertiary amine to an N-oxide?
Which CYP enzyme is responsible for demethylation of methoxy group to phenol?
Which CYP enzyme is responsible for demethylation of methoxy group to phenol?
What slows down the AChE reaction time?
What slows down the AChE reaction time?
