What are System Independent Parameters? - Affinity
Efficacy
What are the parts of a system that are identified as System Dependent Parameters? -
... [Show More] Number of receptors
Cellular machinery
Presence of other drugs
- Competitive
- Noncompetitive
Affinity is - Thermokinetic propensity of drug to bind to receptor
Based largely on ΔG
Efficacy is - Magnitude of change of receptor shape/function upon drug binding
Based on atom/atom interactions
What is the 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
In terms of intrinsic activity, what is determined to be a full agonist? - α = 1
In terms of intrinsic activity, what is determined to me a partial agonist? - 0 < α < 1
In terms of intrinsic activity, what is determined to be an antagonist? - α = 0
What is the formula for the estimation 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 where the electrons in the metal surface layer are excited by photons of incident light with a certain angle of incidence, and then propagate parallel to the metal surface [Show Less]