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WorksheetsMed Chem in Adrenergic System
Total questions: 10
Worksheet time: 8mins
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
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
