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 is investigating a medicinal plant used traditionally for
pain relief. They isolate several compounds from the plant and
determine that one purified constituent produces the analgesic effect in
an experimental model. What is the most appropriate next step in a
drug-discovery strategy?
,A. Discard the compound because its origin is a natural product
B. Characterize the compound and investigate its pharmacological
activity and mechanism
C. Immediately begin large-scale human trials
D. Modify the compound without first determining whether it has
useful activity
Correct Answer:
B. Characterize the compound and investigate its pharmacological
activity and mechanism
Rationale:
B is correct because isolation of an active constituent provides an
opportunity to characterize its chemical properties, biological activity,
potential molecular target, and therapeutic potential. Natural products
have historically served as important starting points for drug discovery.
A is incorrect because natural origin does not make a compound
unsuitable for drug development.
C is incorrect because promising activity must be characterized and
evaluated through appropriate preclinical development before human
testing.
D is incorrect because chemical modification is most rational after the
parent compound's activity and structure-activity relationships are
understood.
Question 2
A compound isolated from a plant produces a reproducible biological
effect in experimental systems. Researchers subsequently synthesize
, several structurally related analogs and compare their biological
activities. What is the primary purpose of this approach?
A. To eliminate the need for biological testing
B. To determine how structural changes influence biological activity
C. To establish that all analogs will have identical pharmacokinetics
D. To determine whether the original plant remains suitable for
cultivation
Correct Answer:
B. To determine how structural changes influence biological activity
Rationale:
B is correct because comparing related compounds helps establish
structure-activity relationships (SAR), allowing researchers to identify
structural features associated with greater potency, selectivity, or other
desirable properties.
A is incorrect because analogs still require biological testing to
determine their activity.
C is incorrect because structural similarity does not guarantee identical
absorption, distribution, metabolism, or elimination.
D is incorrect because cultivation of the source plant is a supply issue
rather than the principal purpose of analog synthesis.
Question 3
A drug-discovery group wants to identify molecules that produce a
desired cellular response but does not yet know which molecular target
is responsible. Which screening strategy is most appropriate?