Name: Score:
67 Multiple choice questions
Definition 1 of 67
Depression of dose-response curves with no dextral displacement
Additional antagonist cannot be overcome by additional agonist
shift the original curve to the right and shifts the maximal down!
Noncompetitive antagonist/Unsurmountable!
What is Surface Plasmon Resonance?
Is a higher or lower pa2 more potent?
Amplification is _______ ______ and _______________________
Definition 2 of 67
- Measure cell/tissue function
- Highly amplified
---Most sensitive
---Partial agonists appear as full agonists
-----Can't compare agonists
Microphysiometry - in vitro measurement of the functions and activities of life or of living matter
and of the physical and chemical phenomena involved on a very small scale.
What is Assay group 2?
What is Assay group 3?
What is the Two State Theory?
What is Assay group 1?
What is an example pf how it is tested?
,Term 3 of 67
How do we define response effect?
Β-arrestin internalizes activated gpcrs (gdp exchanged for gtp)
[A]/[A] + Kd
A+R --> (AR)
An agonist that binds to a receptor, does not impact the maximum, but decreases the
response (shifts the curve to the right)
Term 4 of 67
What is Assay group 2?
a radio-isotopic technology format used to measure a wide range of biological
interactions, including drug-target binding affinity studies
- Measure second messengers
- G proteins activate adenylate cyclase
---Measure cAMP
- Calcium flux influences many cellular processes
---Measure calcium concentration
-----Transient
A tool for measuring the affinity of drugs to their receptors
A graph on a log scale that depicts the response of a reaction on a a line with an increased
or decreased amount of confidence
An agonist that prevents the binding of a full agonist.
At high receptor density - it disrupts lower values by increasing the initial response but will
lower the maximal response
With low receptor density - shifts the curve to the right and decreases the maximim
,Term 5 of 67
What is a Scatchard Plot?
plots the rate of ligand degradation over time
plots the total amount of bound ligand divided by its free concentration (B/[L]) against the
total bound ligand, B.
plots the total amount of unbound ligand against the concentration of receptors
plots the total concentration of free ligand against the time of binding
Term 6 of 67
Amplification is _______ ______ and _______________________
Variable and Unpredictable a Function of Pressure
System Dependent
a Function of Distance
Constant and Unchanging a Function of Time
Separate effects on potency and efficacy
Term 7 of 67
What is the Extended Ternary Complex Model?
G protein receptors only activate in the presence of calcium
G protein receptors are always inactive
G protein receptors spontaneously activate
G protein receptors require a ligand to activate
, Term 8 of 67
What does a Shild Analysis of Non-equilibrium binding look like?
A straight line that tapers off but doesn't quite reach a maximal value.
A vertical line indicating infinite binding
A random scatter of points
A fluctuating curve that rises and falls
Term 9 of 67
IC50 of an allosteric modulator depends not only on the affinity of the modulator, but also the
_________,_________ and _________ of the agonist
affinity, efficacy and concentration
stability, solubility and volume
activity, toxicity and clearance
potency, selectivity and duration
Term 10 of 67
What formula do we use to predict occupancy?
Langmuir equation
DR/Rt = r = D/D+Kd
[a]/[a] + kd
R = f ( α x r x rt )
f = stimulus response
rt = receptor number
K'/k = Ec50 with antagonist/ec50 without Antagonist
67 Multiple choice questions
Definition 1 of 67
Depression of dose-response curves with no dextral displacement
Additional antagonist cannot be overcome by additional agonist
shift the original curve to the right and shifts the maximal down!
Noncompetitive antagonist/Unsurmountable!
What is Surface Plasmon Resonance?
Is a higher or lower pa2 more potent?
Amplification is _______ ______ and _______________________
Definition 2 of 67
- Measure cell/tissue function
- Highly amplified
---Most sensitive
---Partial agonists appear as full agonists
-----Can't compare agonists
Microphysiometry - in vitro measurement of the functions and activities of life or of living matter
and of the physical and chemical phenomena involved on a very small scale.
What is Assay group 2?
What is Assay group 3?
What is the Two State Theory?
What is Assay group 1?
What is an example pf how it is tested?
,Term 3 of 67
How do we define response effect?
Β-arrestin internalizes activated gpcrs (gdp exchanged for gtp)
[A]/[A] + Kd
A+R --> (AR)
An agonist that binds to a receptor, does not impact the maximum, but decreases the
response (shifts the curve to the right)
Term 4 of 67
What is Assay group 2?
a radio-isotopic technology format used to measure a wide range of biological
interactions, including drug-target binding affinity studies
- Measure second messengers
- G proteins activate adenylate cyclase
---Measure cAMP
- Calcium flux influences many cellular processes
---Measure calcium concentration
-----Transient
A tool for measuring the affinity of drugs to their receptors
A graph on a log scale that depicts the response of a reaction on a a line with an increased
or decreased amount of confidence
An agonist that prevents the binding of a full agonist.
At high receptor density - it disrupts lower values by increasing the initial response but will
lower the maximal response
With low receptor density - shifts the curve to the right and decreases the maximim
,Term 5 of 67
What is a Scatchard Plot?
plots the rate of ligand degradation over time
plots the total amount of bound ligand divided by its free concentration (B/[L]) against the
total bound ligand, B.
plots the total amount of unbound ligand against the concentration of receptors
plots the total concentration of free ligand against the time of binding
Term 6 of 67
Amplification is _______ ______ and _______________________
Variable and Unpredictable a Function of Pressure
System Dependent
a Function of Distance
Constant and Unchanging a Function of Time
Separate effects on potency and efficacy
Term 7 of 67
What is the Extended Ternary Complex Model?
G protein receptors only activate in the presence of calcium
G protein receptors are always inactive
G protein receptors spontaneously activate
G protein receptors require a ligand to activate
, Term 8 of 67
What does a Shild Analysis of Non-equilibrium binding look like?
A straight line that tapers off but doesn't quite reach a maximal value.
A vertical line indicating infinite binding
A random scatter of points
A fluctuating curve that rises and falls
Term 9 of 67
IC50 of an allosteric modulator depends not only on the affinity of the modulator, but also the
_________,_________ and _________ of the agonist
affinity, efficacy and concentration
stability, solubility and volume
activity, toxicity and clearance
potency, selectivity and duration
Term 10 of 67
What formula do we use to predict occupancy?
Langmuir equation
DR/Rt = r = D/D+Kd
[a]/[a] + kd
R = f ( α x r x rt )
f = stimulus response
rt = receptor number
K'/k = Ec50 with antagonist/ec50 without Antagonist
