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Advanced Med Pharm, GMS6504 Exam 2, GMS 6504, GMS 6504 Exam 1, GMS 6504 REVIEW EXAM 1 New Update With All GMS Questions And Accurate Answers$24.99
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Advanced Med Pharm, GMS6504 Exam 2, GMS 6504, GMS 6504 Exam 1,
GMS 6504 REVIEW EXAM 1 New Update 2024-2025 With All GMS
Questions And Accurate Answers
What is Occupancy Theory?
Response is proportional to fraction of receptors that are occupied
100% response is obtained when all receptors have ligand
What formula do we use to predict occupancy?
Langmuir equation
DR/Rt = r = D/D+Kd
How do we define response effect?
A+R --> (AR)
Intrinsic activity is depicted as what letter?
How is it defined?
Alpha
Multiplication factor describing ability of agonist to produce a stimulus
For intrinsic activity, what is considered to be a full agonist?
α=1
For intrinsic activity, what is considered to be a partial agonist?
0<α<1
For intrinsic activity what is considered to be an antagonist?
α=0
What is the equation for the determination of relative efficacy?
R = f ( α x r x Rt )
,f = stimulus response
Rt = receptor number
What is the Two State Theory?
Binding of a ligand to a receptor causes a conformational change
A + R --> <-- AR closed --> <-- AR open
Receptors can spontaneously open
The ligand can bind to either open or closed receptor
What is the Ternary Complex Model?
Developed to describe interactions between ligand/receptor/G protein
Receptor activates G protein binds, becomes activated, leaves
A+R --> <-- AR + G --> <--ARG
What is the Extended Ternary Complex Model?
G protein receptors spontaneously activate
What is an Inverse Agonist?
Shift equilibrium towards inactive state
What is the Cubic Ternary Complex?
G proteins bind to inactive receptor
Amplification is _______ ______ and _______________________
System Dependent
a Function of Distance
,MOD 2
What are the 4 types of binding assays?
Radioactive Assay
Fluorescence Assay
Polarization Assay
FRET Assay
What is Scintillation proximity?
a radio-isotopic technology format used to measure a wide range of biological
interactions, including drug-target binding affinity studies
What is Surface Plasmon Resonance?
a phenomenon in which electrons in the metal surface layer are excited by photons of
incident light with a specific angle of incidence and propagate parallel to the metal
surface
What are the three types of binding experiments?
Saturation binding
Displacement binding
Kinetics
What are the two types of binding that occur with binding experiments?
, plots the total amount of bound ligand divided by its free concentration (B/[L]) against the
total bound ligand, B.
What are the three types of displacement binding? (3) What is there impact on IC50?
Competitive- As the concentration of radioligand increases, IC50 increases.
Noncompetitive- IC50 does not increase with increasing radioligand
Allosteric- IC50 increases with increasing radioligand Complete inhibition is not possible
at high concentrations of radioligand (saturable)
What are the first 4 criteria for Binding Experiments?
1. The binding is saturable
2. The binding is reversible and able to be displaced by other ligands
3. A ligand with which to determine nonspecific binding
4. Sufficient biological binding material to result in an adequate signal to noise ratio yet
not so much that it depletes the tracer ligand.
What are the 2nd 4 conditions of Binding Experiments?
5. Optimal Binding Experiments possess the following features: There is a high % of
specific binding along with a low degree of nonspecific binding.
6. Agonist and antagonist tracer ligands are available
7. The kinetics of binding are rapid
8. The ligand used for determination of non-specific binding has a different molecular
structure from the tracer ligand.
What are the assay groups?
1, 2, 3
What is Assay group 1?
What is an example pf how it is tested?
- Measure cell/tissue function
- Highly amplified
---Most sensitive
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