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 investigates a traditional medicinal plant and finds that
an extract consistently reduces inflammation in laboratory assays. What
is the most appropriate next step in a modern natural-product drug-
discovery program?
A. Administer the crude extract directly to patients as a standardized
drug
,B. Isolate and characterize the active constituent(s) responsible for the
observed activity
C. Discard the plant because its active components are chemically
complex
D. Begin large-scale clinical trials using the unprocessed extract
Correct Answer: B. Isolate and characterize the active constituent(s)
responsible for the observed activity
Rationale:
B is correct because natural-product discovery commonly proceeds by
identifying the biologically active constituent(s) within a complex
extract. Isolation and structural characterization allow investigators to
determine which molecule or molecules are responsible for the
pharmacological effect and provide a defined starting point for
optimization.
A is incorrect because a crude extract contains multiple constituents
whose concentrations and effects may vary, making it unsuitable as a
well-characterized drug without further development.
C is incorrect because chemical complexity is not a reason to abandon a
potentially useful source of drug leads; many important drugs
originated from natural products.
D is incorrect because clinical trials require adequate characterization
of the candidate, including evidence of pharmacological activity and
safety.
Question 2
Which finding most strongly supports the classification of a compound
discovered from a natural source as a lead compound?
, A. It produces the desired biological effect but has no measurable
potency
B. It has biological activity that can be optimized to improve therapeutic
properties
C. It is the most abundant molecule in the plant extract
D. It has already demonstrated complete safety in humans
Correct Answer: B. It has biological activity that can be optimized to
improve therapeutic properties
Rationale:
B is correct because a lead compound is a biologically active molecule
suitable for further chemical and pharmacological optimization. The
goal is often to modify the lead to improve potency, selectivity,
pharmacokinetics, efficacy, or safety.
A is incorrect because a compound without measurable activity would
not generally provide a useful pharmacological starting point.
C is incorrect because abundance does not establish pharmacological
usefulness; a highly abundant compound may have little or no desired
activity.
D is incorrect because a lead does not need to have established
complete human safety before optimization and development.
Question 3
A medicinal chemist modifies one functional group on a lead compound
and observes a large change in biological activity. This finding is most
directly useful for determining the compound's:
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 investigates a traditional medicinal plant and finds that
an extract consistently reduces inflammation in laboratory assays. What
is the most appropriate next step in a modern natural-product drug-
discovery program?
A. Administer the crude extract directly to patients as a standardized
drug
,B. Isolate and characterize the active constituent(s) responsible for the
observed activity
C. Discard the plant because its active components are chemically
complex
D. Begin large-scale clinical trials using the unprocessed extract
Correct Answer: B. Isolate and characterize the active constituent(s)
responsible for the observed activity
Rationale:
B is correct because natural-product discovery commonly proceeds by
identifying the biologically active constituent(s) within a complex
extract. Isolation and structural characterization allow investigators to
determine which molecule or molecules are responsible for the
pharmacological effect and provide a defined starting point for
optimization.
A is incorrect because a crude extract contains multiple constituents
whose concentrations and effects may vary, making it unsuitable as a
well-characterized drug without further development.
C is incorrect because chemical complexity is not a reason to abandon a
potentially useful source of drug leads; many important drugs
originated from natural products.
D is incorrect because clinical trials require adequate characterization
of the candidate, including evidence of pharmacological activity and
safety.
Question 2
Which finding most strongly supports the classification of a compound
discovered from a natural source as a lead compound?
, A. It produces the desired biological effect but has no measurable
potency
B. It has biological activity that can be optimized to improve therapeutic
properties
C. It is the most abundant molecule in the plant extract
D. It has already demonstrated complete safety in humans
Correct Answer: B. It has biological activity that can be optimized to
improve therapeutic properties
Rationale:
B is correct because a lead compound is a biologically active molecule
suitable for further chemical and pharmacological optimization. The
goal is often to modify the lead to improve potency, selectivity,
pharmacokinetics, efficacy, or safety.
A is incorrect because a compound without measurable activity would
not generally provide a useful pharmacological starting point.
C is incorrect because abundance does not establish pharmacological
usefulness; a highly abundant compound may have little or no desired
activity.
D is incorrect because a lead does not need to have established
complete human safety before optimization and development.
Question 3
A medicinal chemist modifies one functional group on a lead compound
and observes a large change in biological activity. This finding is most
directly useful for determining the compound's:
