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 identifies a plant extract that has been used
traditionally to relieve pain and fever. Which discovery strategy would
most directly help the team determine whether a specific chemical
constituent is responsible for the observed pharmacological activity?
A. Increase the concentration of the entire plant extract until toxicity
occurs
,B. Fractionate the extract and test individual constituents for biological
activity
C. Replace the extract immediately with a structurally unrelated
synthetic compound
D. Determine the drug's elimination half-life before identifying the
active constituent
Correct Answer: B. Fractionate the extract and test individual
constituents for biological activity
Rationale:
B is correct because bioassay-guided fractionation separates a complex
natural product mixture into fractions and evaluates each fraction for
activity, helping identify the constituent responsible for the effect.
A is incorrect because increasing the whole extract concentration does
not identify which constituent produces the activity and may increase
toxicity from unrelated compounds.
C is incorrect because a replacement compound does not establish
which constituent in the original preparation is pharmacologically
active.
D is incorrect because pharmacokinetic characterization is premature
when the active chemical entity has not yet been identified.
Question 2
Which statement best describes a lead compound in the drug-discovery
process?
A. A compound that has already demonstrated definitive clinical efficacy
B. A chemical compound with promising biological activity that can be
, optimized further
C. A drug that has completed regulatory approval
D. A compound selected solely because it is abundant in a medicinal
plant
Correct Answer: B. A chemical compound with promising biological
activity that can be optimized further
Rationale:
B is correct because a lead compound has sufficient biological activity
and chemical characteristics to justify further optimization for potency,
selectivity, pharmacokinetics, and safety.
A is incorrect because a lead is generally identified well before clinical
efficacy is definitively established.
C is incorrect because regulatory approval occurs much later than lead
identification.
D is incorrect because abundance in a natural source does not by itself
establish a compound as a useful lead.
Question 3
A chemist modifies the structure of a promising lead compound to
increase its ability to bind a desired molecular target while reducing
binding to an off-target receptor. What is the primary purpose of this
modification?
A. To improve selectivity
B. To eliminate all metabolism
C. To guarantee oral absorption
D. To convert the compound into a placebo
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 identifies a plant extract that has been used
traditionally to relieve pain and fever. Which discovery strategy would
most directly help the team determine whether a specific chemical
constituent is responsible for the observed pharmacological activity?
A. Increase the concentration of the entire plant extract until toxicity
occurs
,B. Fractionate the extract and test individual constituents for biological
activity
C. Replace the extract immediately with a structurally unrelated
synthetic compound
D. Determine the drug's elimination half-life before identifying the
active constituent
Correct Answer: B. Fractionate the extract and test individual
constituents for biological activity
Rationale:
B is correct because bioassay-guided fractionation separates a complex
natural product mixture into fractions and evaluates each fraction for
activity, helping identify the constituent responsible for the effect.
A is incorrect because increasing the whole extract concentration does
not identify which constituent produces the activity and may increase
toxicity from unrelated compounds.
C is incorrect because a replacement compound does not establish
which constituent in the original preparation is pharmacologically
active.
D is incorrect because pharmacokinetic characterization is premature
when the active chemical entity has not yet been identified.
Question 2
Which statement best describes a lead compound in the drug-discovery
process?
A. A compound that has already demonstrated definitive clinical efficacy
B. A chemical compound with promising biological activity that can be
, optimized further
C. A drug that has completed regulatory approval
D. A compound selected solely because it is abundant in a medicinal
plant
Correct Answer: B. A chemical compound with promising biological
activity that can be optimized further
Rationale:
B is correct because a lead compound has sufficient biological activity
and chemical characteristics to justify further optimization for potency,
selectivity, pharmacokinetics, and safety.
A is incorrect because a lead is generally identified well before clinical
efficacy is definitively established.
C is incorrect because regulatory approval occurs much later than lead
identification.
D is incorrect because abundance in a natural source does not by itself
establish a compound as a useful lead.
Question 3
A chemist modifies the structure of a promising lead compound to
increase its ability to bind a desired molecular target while reducing
binding to an off-target receptor. What is the primary purpose of this
modification?
A. To improve selectivity
B. To eliminate all metabolism
C. To guarantee oral absorption
D. To convert the compound into a placebo
