Adrenergic Receptor

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

• Dopamine

• Tyrosine

• Norepinephrine

• Acetylcholine

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

• β₁-adrenoceptor

• β₂-adrenoceptor

• β₃-adrenoceptor

• β₄-adrenoceptor

To which class of compounds do this compound belong?

• Phenethylamines

• Adrenergics

• Catecholamine

• Aryloxypropanolamine

Which of the following is the strategies used to obtain β-adrenoceptor selectivity for adrenergic agonists?

• Introduction of a naphthalene ring

• Introduction of a bulky N-alkyl substituent

• Introduction of hydroxymethylene at one of the catechol OH groups

• Addition of an α-methyl group at the alpha carbon

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

• Poor activity

• Slow metabolism

• Poor selectivity

• Poor absorption

How does the amine group in propranolol interacts with the binding site of beta adrenoceptor?

• It interacts as a hydrogen bond donor

• It interacts as a hydrogen bond acceptor

• It is protonated and binds by ionic interactions

• It has no interactions with the binding site

How does the isopropyl group in propranolol interacts with the binding site of beta adrenoceptor?

• By ionic interactions

• By hydrogen bonding

• By van der Waals interactions

• It has no interactions

Tags

NGSS.HS-PS1-3

Shown below is the structure of sabutamol. What role does the t-butyl group play in this agent?

• It increases efficacy of the agent towards adrenergic receptor

• It increases hydrophobicity such that the agent can cross cell membranes

• It acts as steric shield to reduce metabolism

• It introduces selectivity for β-adrenoceptors

Shown below is the structure of sabutamol. What role does the hydroxymethylene group play in this agent?

• To extend the OH group so that it is closer to its binding region in the binding site

• To reposition the phenol OH such that it was not recognised by metabolic enzymes

• To increase the area of conformational space available to the OH group

• To reduce the electronic influence of the OH group on the aromatic ring

Which of the following is the strategy to convert this agonist to a partial antagonist?

• Introduction of a naphthalene ring

• Replacement of catechol meta OH group with a methoxy group

• Introduction of indole ring

• Replacement of catechol OH groups with fluoro groups