TEST BANK
Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A research team begins a drug-discovery program by investigating a
plant traditionally used to relieve inflammatory symptoms. Which step
most directly converts the traditional observation into a
pharmacologically useful lead?
A. Administering the whole plant preparation to a large patient
population
,B. Isolating and characterizing bioactive constituents from the plant
extract
C. Marketing the plant preparation as a standardized medicine
D. Selecting a synthetic compound with a similar molecular weight
Correct Answer:
B. Isolating and characterizing bioactive constituents from the plant
extract
Rationale:
B is correct because natural-product drug discovery commonly begins
by fractionating an active extract, identifying the constituent
responsible for activity, and characterizing its chemical structure. This
converts an empirically observed biological effect into a defined
molecular lead.
A is incorrect because expanding human use does not identify the
active chemical entity or establish its mechanism.
C is incorrect because standardization and marketing occur after
characterization, development, and evaluation rather than serving as
the primary discovery step.
D is incorrect because molecular weight alone provides little
information about biological activity or target interaction.
Question 2
During early drug discovery, investigators identify a chemical compound
that produces a reproducible biological effect but has not yet been
optimized for potency, selectivity, or pharmacokinetic properties. How
is this compound best described?
, A. Lead compound
B. Approved drug
C. Active metabolite
D. Therapeutic index
Correct Answer:
A. Lead compound
Rationale:
A is correct because a lead compound is a molecule with sufficient
biological activity to justify further optimization. Medicinal chemistry
can then modify its structure to improve potency, selectivity,
pharmacokinetics, and safety.
B is incorrect because a compound is not an approved drug merely
because it demonstrates biological activity.
C is incorrect because an active metabolite is a pharmacologically active
product formed from metabolism of another compound.
D is incorrect because therapeutic index is a measure of relative drug
safety, not a chemical entity.
Question 3
A medicinal chemist systematically changes a functional group on a lead
compound and observes corresponding changes in biological activity.
Which concept is being investigated?
A. Structure-activity relationship
B. First-pass elimination
C. Therapeutic drug monitoring
D. Receptor desensitization
Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A research team begins a drug-discovery program by investigating a
plant traditionally used to relieve inflammatory symptoms. Which step
most directly converts the traditional observation into a
pharmacologically useful lead?
A. Administering the whole plant preparation to a large patient
population
,B. Isolating and characterizing bioactive constituents from the plant
extract
C. Marketing the plant preparation as a standardized medicine
D. Selecting a synthetic compound with a similar molecular weight
Correct Answer:
B. Isolating and characterizing bioactive constituents from the plant
extract
Rationale:
B is correct because natural-product drug discovery commonly begins
by fractionating an active extract, identifying the constituent
responsible for activity, and characterizing its chemical structure. This
converts an empirically observed biological effect into a defined
molecular lead.
A is incorrect because expanding human use does not identify the
active chemical entity or establish its mechanism.
C is incorrect because standardization and marketing occur after
characterization, development, and evaluation rather than serving as
the primary discovery step.
D is incorrect because molecular weight alone provides little
information about biological activity or target interaction.
Question 2
During early drug discovery, investigators identify a chemical compound
that produces a reproducible biological effect but has not yet been
optimized for potency, selectivity, or pharmacokinetic properties. How
is this compound best described?
, A. Lead compound
B. Approved drug
C. Active metabolite
D. Therapeutic index
Correct Answer:
A. Lead compound
Rationale:
A is correct because a lead compound is a molecule with sufficient
biological activity to justify further optimization. Medicinal chemistry
can then modify its structure to improve potency, selectivity,
pharmacokinetics, and safety.
B is incorrect because a compound is not an approved drug merely
because it demonstrates biological activity.
C is incorrect because an active metabolite is a pharmacologically active
product formed from metabolism of another compound.
D is incorrect because therapeutic index is a measure of relative drug
safety, not a chemical entity.
Question 3
A medicinal chemist systematically changes a functional group on a lead
compound and observes corresponding changes in biological activity.
Which concept is being investigated?
A. Structure-activity relationship
B. First-pass elimination
C. Therapeutic drug monitoring
D. Receptor desensitization
