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 group is investigating a traditional medicinal plant that has
been used for generations to treat inflammatory symptoms. Extracts
from the plant consistently reduce an inflammatory biomarker in
laboratory studies. What is the most appropriate next step in the
discovery process?
,A. Assume the entire plant extract is the therapeutic agent and begin
clinical use
B. Identify and characterize the chemical constituents responsible for
the observed activity
C. Replace the plant extract with a completely unrelated synthetic
compound
D. Determine the drug's elimination half-life before identifying the
active compound
Correct Answer: B
Rationale:
B is correct because a reproducible biological effect from a natural
source can provide a starting point for identifying active chemical
constituents. Isolation and characterization can reveal a lead compound
whose mechanism, potency, selectivity, and developability can then be
investigated.
A is incorrect because a complex extract may contain multiple
constituents with different activities, toxicities, and pharmacokinetic
properties. The active principle should be characterized rather than
assumed.
C is incorrect because there is no scientific reason to discard a
potentially useful natural-product lead before determining what causes
the activity.
D is incorrect because pharmacokinetic characterization becomes more
meaningful after a defined candidate or active compound has been
identified.
Question 2
, A medicinal chemist describes a compound as a lead compound. Which
characteristic best explains this designation?
A. It has already demonstrated clinical efficacy in humans
B. It has sufficient biological activity to justify further optimization
C. It has received regulatory approval for therapeutic use
D. It has the highest possible affinity for its biological target
Correct Answer: B
Rationale:
B is correct because a lead is a promising starting point for optimization
based on measurable biological activity and other potentially useful
properties. A lead is not necessarily ready for clinical use.
A is incorrect because clinical efficacy requires human clinical
investigation; a lead generally precedes that stage.
C is incorrect because regulatory approval occurs much later in drug
development.
D is incorrect because maximum affinity alone does not define a useful
lead; selectivity, physicochemical properties, pharmacokinetics, safety,
and developability also matter.
Question 3
A discovery team wants to identify compounds that alter a cellular
phenotype without first assuming which molecular target is
responsible. Which approach is most appropriate?
A. Phenotypic screening
B. Structure-based drug design
Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A research group is investigating a traditional medicinal plant that has
been used for generations to treat inflammatory symptoms. Extracts
from the plant consistently reduce an inflammatory biomarker in
laboratory studies. What is the most appropriate next step in the
discovery process?
,A. Assume the entire plant extract is the therapeutic agent and begin
clinical use
B. Identify and characterize the chemical constituents responsible for
the observed activity
C. Replace the plant extract with a completely unrelated synthetic
compound
D. Determine the drug's elimination half-life before identifying the
active compound
Correct Answer: B
Rationale:
B is correct because a reproducible biological effect from a natural
source can provide a starting point for identifying active chemical
constituents. Isolation and characterization can reveal a lead compound
whose mechanism, potency, selectivity, and developability can then be
investigated.
A is incorrect because a complex extract may contain multiple
constituents with different activities, toxicities, and pharmacokinetic
properties. The active principle should be characterized rather than
assumed.
C is incorrect because there is no scientific reason to discard a
potentially useful natural-product lead before determining what causes
the activity.
D is incorrect because pharmacokinetic characterization becomes more
meaningful after a defined candidate or active compound has been
identified.
Question 2
, A medicinal chemist describes a compound as a lead compound. Which
characteristic best explains this designation?
A. It has already demonstrated clinical efficacy in humans
B. It has sufficient biological activity to justify further optimization
C. It has received regulatory approval for therapeutic use
D. It has the highest possible affinity for its biological target
Correct Answer: B
Rationale:
B is correct because a lead is a promising starting point for optimization
based on measurable biological activity and other potentially useful
properties. A lead is not necessarily ready for clinical use.
A is incorrect because clinical efficacy requires human clinical
investigation; a lead generally precedes that stage.
C is incorrect because regulatory approval occurs much later in drug
development.
D is incorrect because maximum affinity alone does not define a useful
lead; selectivity, physicochemical properties, pharmacokinetics, safety,
and developability also matter.
Question 3
A discovery team wants to identify compounds that alter a cellular
phenotype without first assuming which molecular target is
responsible. Which approach is most appropriate?
A. Phenotypic screening
B. Structure-based drug design
