Podcast
Questions and Answers
Which enzyme hydrolyzes acetylcholine?
Which enzyme hydrolyzes acetylcholine?
- Gq
- Gi
- Butyrylcholinesterase
- AChE (correct)
Where are cholinergic terminals found?
Where are cholinergic terminals found?
- Muscle Skeletal
- Autonomic System
- Central Nervous System
- All of the above (correct)
Which receptor subtype is responsible for bronchoconstriction?
Which receptor subtype is responsible for bronchoconstriction?
- M3 (correct)
- M1
- M4
- M2
What is the effect of M2 receptors on the cardiovascular system?
What is the effect of M2 receptors on the cardiovascular system?
Which receptor subtype is responsible for vasodilation?
Which receptor subtype is responsible for vasodilation?
Which type of receptors do cholinergic neurons have?
Which type of receptors do cholinergic neurons have?
What are the subunits of mAChRs?
What are the subunits of mAChRs?
What are the subunits of nAChRs?
What are the subunits of nAChRs?
Which muscarinic agonist is used for the treatment of glaucoma and ocular surgery?
Which muscarinic agonist is used for the treatment of glaucoma and ocular surgery?
Which muscarinic agonist is used for bronchial challenge test?
Which muscarinic agonist is used for bronchial challenge test?
Which receptor does Methacholine primarily act on?
Which receptor does Methacholine primarily act on?
What is the main therapeutic application of Methacholine?
What is the main therapeutic application of Methacholine?
Which of the following is a contraindication for Methacholine use?
Which of the following is a contraindication for Methacholine use?
What is the effect of Methacholine on the cardiovascular system?
What is the effect of Methacholine on the cardiovascular system?
What is the primary diagnostic use of Methacholine?
What is the primary diagnostic use of Methacholine?
Which isomer of ACh hydrolyzes slower than acetylcholine by AChE?
Which isomer of ACh hydrolyzes slower than acetylcholine by AChE?
What is the SAR of Urecholine (bethanechol chloride)?
What is the SAR of Urecholine (bethanechol chloride)?
Which amine in pilocarpene reacts to form HCl salt?
Which amine in pilocarpene reacts to form HCl salt?
What metabolic/physicochemical vulnerabilities do you expect pilocarpene to have?
What metabolic/physicochemical vulnerabilities do you expect pilocarpene to have?
What kind of relationship do the highlighted functional groups in Arecoline and Xanomeline have?
What kind of relationship do the highlighted functional groups in Arecoline and Xanomeline have?
Which enzyme is responsible for breaking down Acetylcholine (ACh)?
Which enzyme is responsible for breaking down Acetylcholine (ACh)?
What is the role of autoreceptors in the cholinergic system?
What is the role of autoreceptors in the cholinergic system?
Which neurotransmitter is released by the sympathetic system to decrease the release of ACh?
Which neurotransmitter is released by the sympathetic system to decrease the release of ACh?
What is the role of M4 receptors in the cholinergic system?
What is the role of M4 receptors in the cholinergic system?
What happens when there is an excess of ACh in the synapse?
What happens when there is an excess of ACh in the synapse?
Which of the following is a reversible acetylcholinesterase inhibitor that forms a more stable inactive site of AChE or has a higher affinity for the active site than ACh but does not react as a substrate?
Which of the following is a reversible acetylcholinesterase inhibitor that forms a more stable inactive site of AChE or has a higher affinity for the active site than ACh but does not react as a substrate?
Which of the following drugs is a synthetic compound that resembles physostigmine and is used for prophylaxis of abdominal distension and urinary retention, myasthenia gravis, and reversal of neuromuscular blockade?
Which of the following drugs is a synthetic compound that resembles physostigmine and is used for prophylaxis of abdominal distension and urinary retention, myasthenia gravis, and reversal of neuromuscular blockade?
Which of the following drugs is a synthetic compound closely related to neostigmine, has a longer duration of action, and a lower incidence of side effects?
Which of the following drugs is a synthetic compound closely related to neostigmine, has a longer duration of action, and a lower incidence of side effects?
Which of the following drugs is a centrally-acting reversible and non-competitive inhibitor with a long elimination half-life of 70+ hours?
Which of the following drugs is a centrally-acting reversible and non-competitive inhibitor with a long elimination half-life of 70+ hours?
Which of the following drugs is a pseudo-irreversible inhibitor that inhibits plasma choline-E and crosses the blood-brain barrier?
Which of the following drugs is a pseudo-irreversible inhibitor that inhibits plasma choline-E and crosses the blood-brain barrier?
What is the primary diagnostic use of Methacholine?
What is the primary diagnostic use of Methacholine?
Which muscarinic agonist is used for the treatment of glaucoma and ocular surgery?
Which muscarinic agonist is used for the treatment of glaucoma and ocular surgery?
Which receptor does Methacholine primarily act on?
Which receptor does Methacholine primarily act on?
Which type of receptors are coupled to G-proteins and produce effectors in cholinergic neurons?
Which type of receptors are coupled to G-proteins and produce effectors in cholinergic neurons?
What is the main therapeutic application of Miostat (carbachol chloride)?
What is the main therapeutic application of Miostat (carbachol chloride)?
Which muscarinic agonist is preferentially selective for mAChRs over nAChRs?
Which muscarinic agonist is preferentially selective for mAChRs over nAChRs?
What is the main diagnostic use of Provocholine (methacholine chloride)?
What is the main diagnostic use of Provocholine (methacholine chloride)?
What makes carbachol chloride more stable to hydrolysis compared to ACh?
What makes carbachol chloride more stable to hydrolysis compared to ACh?
Which of the following drugs is a reversible acetylcholinesterase inhibitor that forms a more stable inactive site of AChE or has a higher affinity for the active site than ACh but does not react as a substrate?
Which of the following drugs is a reversible acetylcholinesterase inhibitor that forms a more stable inactive site of AChE or has a higher affinity for the active site than ACh but does not react as a substrate?
What is the elimination half-life of Cognex (tacrine HCl)?
What is the elimination half-life of Cognex (tacrine HCl)?
Which of the following drugs is a centrally-acting reversible and non-competitive inhibitor with a long elimination half-life of 70+ hours?
Which of the following drugs is a centrally-acting reversible and non-competitive inhibitor with a long elimination half-life of 70+ hours?
Which of the following drugs crosses the blood-brain barrier and is not associated with hepatotoxicity?
Which of the following drugs crosses the blood-brain barrier and is not associated with hepatotoxicity?
Which of the following is an irreversible acetylcholinesterase inhibitor that generates an extremely stable phosphorylated-Serine residue in AChE?
Which of the following is an irreversible acetylcholinesterase inhibitor that generates an extremely stable phosphorylated-Serine residue in AChE?
Which of the following statements about acetylcholine (ACh) is correct?
Which of the following statements about acetylcholine (ACh) is correct?
Which receptor subtype is responsible for bronchoconstriction?
Which receptor subtype is responsible for bronchoconstriction?
Which of the following is a therapeutic application of Bethanechol?
Which of the following is a therapeutic application of Bethanechol?
Which of the following statements about Muscarinic receptors is correct?
Which of the following statements about Muscarinic receptors is correct?
Which of the following drugs is used for the treatment of open-angle glaucoma and xerostomia (dry-mouth)?
Which of the following drugs is used for the treatment of open-angle glaucoma and xerostomia (dry-mouth)?
Which of the following drugs is a partial direct M1 agonist in the CNS and an M3 agonist in the epithelial tissue of lacrimal and salivary glands?
Which of the following drugs is a partial direct M1 agonist in the CNS and an M3 agonist in the epithelial tissue of lacrimal and salivary glands?
What is the main therapeutic application of Acetylcholinesterase (AChE) inhibitors?
What is the main therapeutic application of Acetylcholinesterase (AChE) inhibitors?
What is the catalytic triad involved in the esteratic site of AChE?
What is the catalytic triad involved in the esteratic site of AChE?
If the AChE enzyme is acylated by an agent with a more stable functional group, what happens?
If the AChE enzyme is acylated by an agent with a more stable functional group, what happens?
What is the main diagnostic use of Methacholine?
What is the main diagnostic use of Methacholine?
Which of the following is true about Methacholine's effect on the cardiovascular system?
Which of the following is true about Methacholine's effect on the cardiovascular system?
Which of the following is a therapeutic application of Methacholine?
Which of the following is a therapeutic application of Methacholine?
Which receptor subtype is responsible for vasodilation?
Which receptor subtype is responsible for vasodilation?
What is the effect of M2 receptors on the cardiovascular system?
What is the effect of M2 receptors on the cardiovascular system?
What is the main therapeutic application of Acetylcholinesterase (AChE) inhibitors?
What is the main therapeutic application of Acetylcholinesterase (AChE) inhibitors?
True or false: Acetylcholine is a neurotransmitter for both the sympathetic and parasympathetic nervous systems.
True or false: Acetylcholine is a neurotransmitter for both the sympathetic and parasympathetic nervous systems.
True or false: Muscarinic cholinergic agents interact with nicotinic receptors.
True or false: Muscarinic cholinergic agents interact with nicotinic receptors.
True or false: Muscarinic acetylcholinergic receptors are metabotropic receptors.
True or false: Muscarinic acetylcholinergic receptors are metabotropic receptors.
True or false: Pirenzepine acts as a muscarinic agonist without blocking the effect of muscarinic antagonists?
True or false: Pirenzepine acts as a muscarinic agonist without blocking the effect of muscarinic antagonists?
True or false: Anticholinergic agents are used to treat glaucoma?
True or false: Anticholinergic agents are used to treat glaucoma?
True or false: Odd numbered mAChRs are coupled to Gq proteins?
True or false: Odd numbered mAChRs are coupled to Gq proteins?
True or false: Nicotinic receptors are found in the neuromuscular junctions, adrenal medulla, and autonomic ganglia?
True or false: Nicotinic receptors are found in the neuromuscular junctions, adrenal medulla, and autonomic ganglia?
True or false: ACh cannot be administered orally due to its physicochemical properties and inability to penetrate the Blood-Brain Barrier?
True or false: ACh cannot be administered orally due to its physicochemical properties and inability to penetrate the Blood-Brain Barrier?
True or false: Acetylcholine (ACh) is a poor therapeutic agent due to its promiscuity towards both muscarinic (mAChRs) and nicotinic (nAChRs) receptors?
True or false: Acetylcholine (ACh) is a poor therapeutic agent due to its promiscuity towards both muscarinic (mAChRs) and nicotinic (nAChRs) receptors?
Which of the following drugs is a non-specific muscarinic agonist that acts as an agonist to both mAChRs and nAChRs?
Which of the following drugs is a non-specific muscarinic agonist that acts as an agonist to both mAChRs and nAChRs?
True or false: Muscarinic agonists with a longer chain length between the ethylene group and the N atom have increased activity?
True or false: Muscarinic agonists with a longer chain length between the ethylene group and the N atom have increased activity?
True or false: Muscarinic agonists with quaternary ammonium groups substituted with heteroatoms like S, Se, Ar, Ph are more active than those with nitrogen?
True or false: Muscarinic agonists with quaternary ammonium groups substituted with heteroatoms like S, Se, Ar, Ph are more active than those with nitrogen?
Which of the following drugs is a specific muscarinic agonist that has a preference to act as an agonist to mAChRs over nAChRs?
Which of the following drugs is a specific muscarinic agonist that has a preference to act as an agonist to mAChRs over nAChRs?
Which of the following drugs is a synthetic compound closely related to neostigmine, has a longer duration of action, and a lower incidence of side effects?
Which of the following drugs is a synthetic compound closely related to neostigmine, has a longer duration of action, and a lower incidence of side effects?
Which of the following drugs is used for the treatment of post-surgical and post-partum urinary retention?
Which of the following drugs is used for the treatment of post-surgical and post-partum urinary retention?
Which muscarinic agonist is used to treat open-angle glaucoma and xerostomia (dry-mouth)?
Which muscarinic agonist is used to treat open-angle glaucoma and xerostomia (dry-mouth)?
Which muscarinic agonist is a partial direct M1 agonist in the CNS and an M3 agonist in epithelial tissue of lacrimal and salivary glands?
Which muscarinic agonist is a partial direct M1 agonist in the CNS and an M3 agonist in epithelial tissue of lacrimal and salivary glands?
Which muscarinic agonist has affinity for M3 subtype and is used as an ocular and oral treatment for open-angle glaucoma and xerostomia (dry-mouth)?
Which muscarinic agonist has affinity for M3 subtype and is used as an ocular and oral treatment for open-angle glaucoma and xerostomia (dry-mouth)?
Which of the following drugs is an irreversible acetylcholinesterase inhibitor that generates an extremely stable phosphorylated-Serine residue in AChE?
Which of the following drugs is an irreversible acetylcholinesterase inhibitor that generates an extremely stable phosphorylated-Serine residue in AChE?
Which of the following drugs is a synthetic compound closely related to neostigmine, has a longer duration of action, and a lower incidence of side effects?
Which of the following drugs is a synthetic compound closely related to neostigmine, has a longer duration of action, and a lower incidence of side effects?
Which of the following drugs is a reversible acetylcholinesterase inhibitor that forms a more stable inactive site of AChE or has a higher affinity for the active site than ACh but does not react as a substrate?
Which of the following drugs is a reversible acetylcholinesterase inhibitor that forms a more stable inactive site of AChE or has a higher affinity for the active site than ACh but does not react as a substrate?
Which of the following drugs is an alkaloid isolated from the calabar bean (Physostigma venenosum), carbamylates AChE at a slow rate but has high affinity, and can diffuse across the blood-brain barrier?
Which of the following drugs is an alkaloid isolated from the calabar bean (Physostigma venenosum), carbamylates AChE at a slow rate but has high affinity, and can diffuse across the blood-brain barrier?
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Study Notes
Cholinergic System
- Acetylcholine (ACh) is broken down by the enzyme acetylcholinesterase (AChE)
- Cholinergic terminals are found in the neuromuscular junction, autonomic ganglia, and central nervous system
Receptors and Agonists
- Muscarinic receptors are responsible for various physiological responses, including bronchoconstriction and vasodilation
- M2 receptors are responsible for bronchoconstriction
- M3 receptors are responsible for vasodilation
- Methacholine is a muscarinic agonist used for bronchial challenge tests and has a primary diagnostic use for bronchial hyperreactivity
- Methacholine primarily acts on M3 receptors
- Pilocarpine is a muscarinic agonist used to treat glaucoma and ocular surgery
Enzymes and Inhibitors
- Acetylcholinesterase (AChE) is the enzyme responsible for breaking down acetylcholine (ACh)
- Reversible acetylcholinesterase inhibitors, such as Neostigmine, form a more stable inactive site of AChE or have a higher affinity for the active site than ACh
- Physostigmine is a reversible acetylcholinesterase inhibitor that crosses the blood-brain barrier
- Tacrine is a centrally-acting reversible and non-competitive inhibitor with a long elimination half-life of 70+ hours
Autoreceptors and Neurotransmitters
- Autoreceptors in the cholinergic system decrease the release of ACh
- The sympathetic system releases norepinephrine to decrease the release of ACh
- M4 receptors play a role in the cholinergic system
Other
- Excess ACh in the synapse leads to increased transmission
- Arecoline and Xanomeline have a synergistic relationship between their functional groups
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