Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A pharmacology research team investigates a medicinal plant
traditionally used to relieve severe pain. Chemical analysis identifies
morphine as the active constituent. Which discovery process best
describes the role of the plant in this example?
A. The plant served as a source of a bioactive compound that could be
isolated and characterized
,B. The plant directly confirmed the molecular target of morphine
C. The plant eliminated the need for pharmacological testing
D. The plant established the optimal therapeutic dose in humans
Correct Answer:
A. The plant served as a source of a bioactive compound that could be
isolated and characterized
Rationale:
Natural products have historically provided important starting points for
drug discovery. In this approach, a biologically active substance is
identified within a natural source, isolated, characterized, and
subsequently investigated for therapeutic potential. B is incorrect
because identifying a natural product does not by itself establish its
molecular target. C is incorrect because isolation of a compound does
not eliminate the need for preclinical and clinical evaluation. D is
incorrect because therapeutic dosing requires pharmacological and
clinical investigation.
Question 2
A researcher identifies a plant extract that produces a reproducible
biological effect in an experimental assay. What is the most appropriate
next step in a traditional natural-product drug discovery program?
A. Administer the entire extract to patients
B. Identify and characterize the active chemical constituents
C. Assume that the most abundant compound is responsible for the
effect
D. Begin phase III clinical trials
, Correct Answer:
B. Identify and characterize the active chemical constituents
Rationale:
When a natural extract demonstrates biological activity, investigators
generally seek to isolate and characterize the constituent or
constituents responsible for that activity. This converts a complex
mixture into defined chemical entities that can be studied
systematically. A is premature because the extract has not yet been
adequately characterized or evaluated for safety. C is incorrect because
abundance does not necessarily correlate with biological activity. D is
incorrect because extensive preclinical and clinical development must
precede phase III studies.
Question 3
Which characteristic makes a newly discovered compound particularly
valuable as a drug-discovery lead?
A. It produces any measurable biological effect regardless of toxicity
B. It has useful biological activity that can be optimized through
chemical modification
C. It is always structurally simple
D. It has already demonstrated long-term safety in humans
Correct Answer:
B. It has useful biological activity that can be optimized through
chemical modification
Rationale:
A lead compound is a molecule with promising biological activity and