Engels - AL- Some questions - Block 1
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Questions and Answers

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?

  • Muscarinic Antagonist
  • Nicotinic Agonist
  • Cholinergic Inhibitors
  • Muscarinic Agonist (correct)

    • 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?

    <p>Make it necessary for the drug to travel from the target to the liver, where harsh phase 1 or 2 drug rxns will occur</p> Signup and view all the answers

    What should happen to further increase the half-life of a drug which already requires hepatic metabolism?

    <p>Add an EWG (like F) to protect the drug from hepatic metabolism</p> Signup and view all the answers

    Which of the following is NOT something that the nature of the amine determines?

    <p>Localized - protected or unprotected</p> Signup and view all the answers

    What does an alkyl linker provide?

    <p>A defined distance between the amine and ester required for binding to a receptor</p> Signup and view all the answers

    What is a difference between Muscarinic Agonist vs. Antagonist structures?

    <p>Muscarinic Antagonists all have an aromatic ring</p> Signup and view all the answers

    What change can occur to ACh so the resulting compound exhibits agonistic activity?

    <p>The area between the amine and ester can be bulkier than in ACh</p> Signup and view all the answers

    What change can NOT occur to ACh so the resulting compound exhibits antagonist activity?

    <p>Cleave the ester by esterases, which will allow for more things to attach to the structure</p> Signup and view all the answers

    What kind of biological effect will acetylcholinesterase inhibitors have?

    <p>The same as cholinergic agonists</p> Signup and view all the answers

    What is the makeup of the anionic site of mAChR?

    <p>It contains an Asp, which enables an ionic bond to form between negatively charged Asp and positively charged quaternary amine of ACh</p> Signup and view all the answers

    What is the makeup of the 'anionic' site of AChE?

    <p>Contains Trp, which enables a pi-cation interaction between resonating pi-electrons of the aromatic ring of Trp and positively charged quaternary amine of ACh</p> Signup and view all the answers

    Why is echothiopate suitable for application in humans?

    <p>It is the only irreversible AChEI which contains a quaternary amine, preventing it to reach the CNS</p> Signup and view all the answers

    Match the following regarding measures in the metabolism of malathion that are exploited.

    <p>True = The insect specific P=O bond required to activate drug (only in insects) False = The insects are not able to metabolize any kind of drug, making it useless True = Metabolism by esterases, which prevent drug from reaching CNS False = Metabolism by liver, which helps the drug to have better bioavailability</p> Signup and view all the answers

    Why can ProPam pass the BBB in contrast to 2-PAM?

    <p>ProPam does not contain permanent positive charge of the aromatic quaternary nitrogen in 2-PAM</p> Signup and view all the answers

    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?

    <p>True</p> Signup and view all the answers

    Which CYP enzyme is responsible for N-dealkylation and aromatic hydroxylation?

    <p>CYP3A4</p> Signup and view all the answers

    Which enzyme is responsible for converting a tertiary amine to an N-oxide?

    <p>FMO</p> Signup and view all the answers

    Which CYP enzyme is responsible for demethylation of methoxy group to phenol?

    <p>CYP2D6</p> Signup and view all the answers

    What slows down the AChE reaction time?

    <p>A tertiary carbamate</p> Signup and view all the answers

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