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 medicinal plant traditionally used for
pain and isolates a chemically defined compound responsible for much
of the biological activity. What is the major advantage of isolating the
active compound for drug discovery?
A. It eliminates the need for pharmacological testing
B. It provides a defined chemical entity that can be characterized and
,optimized
C. It guarantees the compound will be safe in humans
D. It ensures the compound will have high oral bioavailability
Correct Answer: B
Rationale:
B is correct because isolation of a defined active compound allows
researchers to characterize its molecular structure, biological activity,
pharmacologic properties, and potential for chemical optimization.
Natural products can serve as starting points for discovering bioactive
molecules.
A is incorrect because isolation does not eliminate the need for
pharmacological and toxicological evaluation.
C is incorrect because activity in a plant or experimental system does
not establish human safety.
D is incorrect because oral bioavailability depends on properties such as
absorption, metabolism, and formulation and cannot be assumed from
natural origin.
Question 2
Which historical discovery pathway best illustrates how a medicinal
plant can provide the starting point for a modern drug?
A. Isolation of a bioactive constituent followed by structural
characterization and optimization
B. Selection of a plant solely because it grows rapidly
C. Random administration of an entire plant without identifying active
constituents
D. Selection of a compound based only on its color and physical
appearance
, Correct Answer: A
Rationale:
A is correct because natural-product drug discovery can proceed from
observation of biological activity to isolation of active molecules,
followed by characterization and development of analogs or optimized
candidates.
B is incorrect because growth rate does not establish pharmacological
activity.
C is incorrect because crude botanical material contains multiple
constituents and makes mechanistic and dose-response assessment
more difficult.
D is incorrect because appearance provides little evidence of
therapeutic molecular activity.
Question 3
During early drug discovery, researchers identify a protein that appears
to play a critical role in a disease process. In this context, the protein is
best described as a:
A. Formulation excipient
B. Therapeutic target
C. Drug metabolite
D. Placebo component
Correct Answer: B
Rationale:
B is correct because a therapeutic target is a biological molecule or
process whose modulation is intended to produce a beneficial
therapeutic effect. Target identification is an important component of