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Question 1

Which of the following is a clinical use for a muscarinic agonist?

a) Treatment of myasthenia gravis.

b) 'Switching off' the gastrointestinal tract prior to surgery.

c) 'Switching on' the urinary tract after surgery.

d) Increasing heart muscle activity in certain heart defects.

Question 2

Atropine has been used to decrease gastrointestinal motility and to counteract anticholinesterase poisoning.

What function does this molecule have?

a) Muscarinic agonist

b) Muscarinic antagonist

c) Nicotinic agonist

d) Nicotinic antagonist

Question 3

Atropine has been used to decrease gastrointestinal motility and to counteract anticholinesterase poisoning.

Atropine
Structure I was developed from atropine.

Structure I
What drug design strategy has been used principally in this case?

a) Simplification

b) Rigidification

c) Extension

d) Substituent variation

Question 4

Tubocurarine is a lead compound for a class of medicinally useful compounds.

What clinical use was the agent put to?

a) A cardiovascular agent.

b) A neuromuscular blocker.

c) An anti-asthmatic drug.

d) An analgesic.

Question 5

What sort of receptor is the nicotinic receptor?

a) A G-protein coupled receptor.

b) A kinase linked receptor.

c) An intracellular receptor .

d) An ion channel.

Question 6

What sort of receptor is the muscarinic receptor?

a) A G-protein coupled receptor.

b) A kinase linked receptor.

c) An intracellular receptor.

d) An ion channel.

Question 7

The following diagram shows the first part of the mechanism by which acetylcholine is inactivated by acetylcholinesterase. One of the arrows in the mechanism is incorrect. Which one?

a) A

b) B

c) C

d) D

Question 8

The following diagram shows the second part of the mechanism by which acetylcholine is inactivated by acetylcholinesterase. One of the arrows in the mechanism is incorrect. Which one?

a) A

b) B

c) C

d) D

Question 9

Which feature of acetylcholine interacts with the binding site of cholinergic receptors by hydrogen bonding?

a) The acyl methyl group.

b) The ester.

c) The quaternary nitrogen.

d) All three N-methyl groups.

Question 10

Several aromatic amino acid residues present in the cholinergic binding site are thought to interact with acetylcholine by means of an induced dipole-dipole interaction. Which part of the acetylcholine is involved?

a) The acyl methyl group.

b) The ester.

c) The ethylene bridge.

d) The quaternary ammonium head group.

Question 11

The following structure (carbachol) is a cholinergic agonist.

What is the purpose of the amino group in red?

a) It acts as a metabolically susceptible group.

b) It interacts with a hydrophilic pocket in the binding site.

c) It acts as a steric shield to protect the ester group.

d) It protects the neighbouring ester group by means of an electronic effect.

Question 12

Tubocurarine is a lead compound for a class of medicinally useful compounds.

What feature of the above structure is crucial to its activity?

a) The phenol ring

b) The isoquinoline rings

c) The aromatic ring

d) The two positively charged nitrogen atoms

Question 13

Atracurium is used intravenously as a neuromuscular blocker.

The molecule undergoes a chemical degradation at slightly alkaline pH. What is the name of this reaction?

a) Hofmann rearrangement

b) Hofmann elimination

c) Cope rearrangement

d) McLafferty rearrangement

Question 14

The following structure is parathion.

What was it used for commercially?

a) A medicine in the treatment of glaucoma

b) An antidote to anticholinesterase poisoning

c) An insecticide

d) A medicine in the treatment of Alzheimer's disease

Question 15

The following drug (tacrine) has been used medicinally. In what area of medicine has it been used?

a) A medicine in the treatment of glaucoma.

b) An antidote to anticholinesterase poisoning.

c) An insecticide.

d) A medicine in the treatment of Alzheimer's disease.

Oxford University Press, Online Resource Centre, Chapter 22.

Chapter 22

Instructions