GMS6504 Exam 1&2 Advanced Med Pharm Verified Questions And Answers 2024/2025 Updates
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GMS6504
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GMS6504
GMS6504 Exam 1&2 Advanced Med Pharm Verified Questions And Answers 2024/2025 Updates
Which of the following would best be described as a system independent parameter determining pharmacological response?
Receptor affinity for the ligand
When taking a natural agonist and converting it to an antag...
GMS6504 Exam 1&2 Advanced Med Pharm Verified
Questions And Answers
Which of the following would best be described as a system independent parameter determining
pharmacological response?
Receptor affinity for the ligand
When taking a natural agonist and converting it to an antagonist using synthetic chemistry, what are
the desired effects on affinity and efficacy?
Affinity increases, efficacy decreases
In the Langmuir equation, which variable represents the proportion of receptors that are bound by
ligand?
r
If a ligand has an intrinsic activity, α, of 0.54, this ligand is best considered a ______.
partial agonist
If you do a cell culture experiment where you exogenously express a receptor in cells, which variable
in the equation R = f(α •r • Rt) are you most directly controlling?
Rt
With an efficacy-driven agonist, reducing the number of receptors present will shift the response
curve _____.
right
Applying the two-state theory of receptors to an ion channel, which state(s) would be active?
ARopen
In a two-state system that allows for spontaneously active receptors, increasing the expression levels
of receptor in the absence of agonist will have what effect on measured response?
Increase
In the extended ternary complex model of receptors, which state(s) will result in subsequent
downstream signaling?
ARaG, RaG
Addition of an inverse agonist to a system containing a receptor that does not spontaneously activate
will have what effect on the measured response in the absence of any other ligand?
Have no effect
,You use an agonist to treat two systems that are identical other than the number of receptors present.
System A required 1 mM of the ligand to reach 100% response while system B required 100 mM.
Which system has the larger receptor reserve?
System A
The cellular veil _______ the measured response
may increase or decrease
Assuming cellular amplification, measuring a response that is ______ the ligand binding event will
result in a larger measured response.
further from
When comparing two partial agonists, you are more likely to see a difference in response if you are
measuring a response that is ______ the ligand binding event. Assume that you are not limited in any
way by the instrumentation used to measure the response.
closer to
You treat a system with an agonist, wash out the agonist, and then add a second treatment of the same
agonist. Your measurements show that the receptors underwent desensitization due to the
pretreatment. The response you measured after the second treatment must have been _____ the
response measured after the first treatment.
lower than
Which binding assay technique does not require any additional steps after ligand addition in order to
eliminate non-specific binding from the measured signal?
FRET assay
If you double the agonist concentration, what will happen to the non-specific binding?
Double
At what point after addition of an agonist does the rate of occupancy increase the fastest?
Immediately after addition
On a Scatchard plot, 100% occupancy is reached when _______.
Y=0
You are carrying out a displacement binding assay. You find that, regardless of what concentration of
radioligand you start with, it always requires 50 mM of your cold ligand to displace 50% of the
radioligand and always requires 200 mM of your cold ligand to completely displace the radioligand.
Your cold ligand is which type of antagonist?
Noncompetitive
In a displacement binding experiment, a known allosteric antagonist will most likely produce which
effect?
,There is no concentration at which it will completely displace all of the radioligand.
Binding of a radioligand to a receptor is usually ______ when in the presence of a competitive
inhibitor.
slower
Which assumption must hold true for displacement binding experiments to be interpretable?
Binding of radioligand to the receptor does not substantially reduce the amount of free radioligand.
True or false? An agonist that has higher binding at a given concentration than a different agonist will
also always give a higher response in a functional assay.
False
Application of an agonist to Xenopus melanophores resulted in the cells becoming completely
transparent. Which G protein was activated?
Gi
After addition of an agonist, you measure an increase in mRNA from the whatchamacallit gene. This
is an example of a group ____ assay.
3
You have cells that express fluorescent β-arrestin. Upon addition of an agonist that binds to GPCRs,
would you expect fluorescence located at the cell membrane to increase or decrease after giving time
for the system to equilibrate (i.e. not immediately)?
Decrease
An antagonist that has a concentration where addition of more antagonist will have no additional
measurable effect is called ______.
Saturable
A more potent antagonist will have a _______ pA2.
lower
A Schild analysis reveals a graph that resembles a y = x2 graph. This antagonist is most likely
______.
noncompetitive
A reversible inverse agonist applied to a system that does not contain constitutive activity will appear
to behave most like a(n) _____ antagonist.
Competitive
True or false? It is possible for a competitive antagonist and an allosteric modulator to have
synergistic effects in blocking agonist binding. (This probably wasn't discussed in the lecture. You
have to think about it.)
, True
An allosteric modulator with α > 1, β = 1 is best classified as a _______.
PAM
An allosteric modulator that increases affinity while decreasing efficacy is best classified as a
_______.
PAM-antagonist
True or false? An allosteric modulator may be a NAM when applied with one agonist and a PAM
when applied with a different agonist. (This probably wasn't discussed in the lecture. You have to
think about it.)
True
In which model of allosterism does the ligand actively cause a conformational change in the
receptor?
Sequential model
True or false? An allosteric ligand that increases binding of an orthosteric ligand will also increase
efficacy of that orthosteric ligand.
False
Which of the following types of kinase inhibitors does NOT inhibit ATP binding to the kinase?
Indirect allosteric
An allosteric modulator that blocks the SH2 domain on a kinase is likely to serve as a _______.
Negative allosteric modulator
In terms of Lipinski's rules, which of the following functional groups serves as a hydrogen bond
donor?
-NH2
Will a hydrophobic molecule have a high or low logP?
high
Which is the best explanation as to why CNS drugs tend to have smaller polar surface areas than
drugs that target things outside of the CNS?
It helps the drug cross the blood brain barrier
Which functional group is most often utilized when making pro-drugs?
Esters
Which of the following protein domains would you expect to find in an "easily druggable" target but
NOT in an "undruggable" target?
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