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 begins investigating a plant traditionally used for fever
and extracts several chemical constituents for laboratory testing. What
is the primary purpose of this early stage of drug discovery?
A. To determine the drug's final commercial price
B. To identify chemical entities that may have useful biological activity
,C. To establish the drug's therapeutic index in humans
D. To determine the most effective marketing strategy
Correct Answer:
B. To identify chemical entities that may have useful biological activity
Rationale:
B is correct because early discovery efforts often involve identifying
biologically active molecules that can become leads for further
development. Testing natural products can reveal compounds with
pharmacological activity that warrant isolation and characterization.
A is incorrect because pricing is a commercial consideration that occurs
much later and is not the purpose of initial discovery.
C is incorrect because therapeutic index assessment requires
substantially more pharmacological and toxicological information than
is available during initial screening.
D is incorrect because marketing strategy is unrelated to identifying
biologically active chemical compounds.
Question 2
Which finding most strongly supports designation of a newly identified
compound as a lead compound?
A. It has already received regulatory approval
B. It produces reproducible activity against a biologically relevant target
and can be chemically modified
C. It has the highest molecular weight among screened compounds
D. It is the most abundant compound in a medicinal plant
, Correct Answer:
B. It produces reproducible activity against a biologically relevant target
and can be chemically modified
Rationale:
B is correct because a lead compound is a chemical entity with
promising biological activity that can undergo structural optimization to
improve potency, selectivity, pharmacokinetic properties, or safety.
A is incorrect because regulatory approval occurs after extensive
preclinical and clinical development.
C is incorrect because molecular weight alone does not establish
biological usefulness or developability.
D is incorrect because abundance in a natural source does not
necessarily correlate with pharmacological activity or suitability for
development.
Question 3
A scientist compares a series of structurally related molecules and finds
that adding a small hydrophobic group increases activity, whereas
adding a bulky polar group substantially reduces activity. What concept
is being evaluated?
A. Structure-activity relationship
B. First-pass metabolism
C. Renal clearance
D. Therapeutic drug monitoring
Correct Answer:
A. Structure-activity relationship