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Question 1

Which of the following is a natural chemical messenger for the adrenergic receptor?

a) Acetylcholine

b) Dopamine

c) Serotonin

d) Noradrenaline

Question 2

What is the predominant adrenoceptor in heart muscle?

a) α₁-adrenoceptor

b) α₂-adrenoceptor

c) β₁-adrenoceptor

d) β₂-adrenoceptor

Question 3

What is the predominant β-adrenoceptor in bronchial smooth muscle?

a) β₁-adrenoceptor

b) β₂-adrenoceptor

c) β₃-adrenoceptor

d) β₄-adrenoceptor

Question 4

What is the main clinical use for agonists of the β₂-adrenoceptor?

a) Treatment of angina.

b) Treatment of hypertension.

c) Treatment of asthma.

d) Treatment of pain.

Question 5

What is the main clinical use for antagonists of the β₁-adrenoceptor?

a) Treatment of glaucoma.

b) Treatment of hypertension.

c) Treatment of asthma.

d) Treatment of pain.

Question 6

To which class of compounds do adrenaline, noradrenaline and dopamine belong?

a) Phenethylamines

b) Diphenolethylamines

c) Catecholamines

d) Adrenergics

Question 7

Identify the tactic which is used to obtain β-adrenoceptor selectivity for adrenergic agonists.

a) Introduction of a naphthalene ring.

b) Introduction of a bulky N-alkyl substituent.

c) Removal of one of the catechol OH groups.

d) Addition of an α-methyl group (alpha to the carbon bearing the amine).

Question 8

What disadvantage is there in using adrenaline as an adrenergic agonist?

a) Poor activity.

b) Rapid metabolism.

c) Poor selectivity.

d) All of the above.

Question 9

Salbutamol is an important clinical agent. The coloured groups are modifications that distinguish the molecule from adrenaline or noradrenaline.

What role does the t-butyl group play?

a) It acts as steric shield to reduce metabolism.

b) It increases hydrophobicity such that the molecule can cross cell membranes.

c) It introduces selectivity for β-adrenoceptors.

d) It introduces selectivity for α-adrenoceptors.

Question 10

Salbutamol is an important clinical agent. The coloured groups are modifications that distinguish the molecule from adrenaline or noradrenaline.

Why was the hydroxymethylene group introduced?

a) It was a chain extension to place the OH group closer to its binding region in the binding site.

b) It was introduced to increase the area of conformational space available to the OH group.

c) It was introduced to reposition the phenol OH such that it was not recognised by metabolic enzymes.

d) It was introduced to reduce the electronic influence of the OH group on the aromatic ring.

Question 11

The following diagram illustrates some of the compounds that were involved in the development of the important clinical agent - propranolol.

What effect does the naphthalene ring have?

a) It makes the agent an agonist.

b) It makes the agent an antagonist.

c) It makes the agent a partial agonist.

d) It makes the agent inactive.

Question 12

The diagram below indicates some of the groups present in propranolol.

How does the amine group interact with the binding site?

a) It interacts as a hydrogen bond donor.

b) It interacts as a hydrogen bond acceptor.

c) It is protonated and binds by ionic interactions.

d) It has no interactions with the binding site.

Question 13

The diagram below indicates some of the groups present in propranolol.

How does the alcohol group interact with the binding site?

a) By ionic interactions.

b) By hydrogen bonding.

c) By van der Waals interactions.

d) It remains solvated and has no interactions.

Question 14

The diagram below indicates some of the groups present in propranolol.

How does the ether group interact with the binding site?

a) It has no interactions and remains solvated.

b) By hydrogen bonding as a hydrogen bond donor.