Measuring selectivity and affinity Flashcards
What are the two ways of obtaining selectivity?
- Modification of drug structure
2. Selective delivery
What happens to selectivity of drugs as concentration increases?
Decreases
What is a ligand?
Substance that can bind to and form a complex with a biomolecule
What are drugs designed to mimic?
The physio-chemical properties of the endogenous ligand for a receptor of other type of target.
What sort of bonds for a irreversible interaction with the receptor?
Covalent
What are the reversible bonds which form?
Hydrogen, van der Waal and ionic.
What is another name for a ionic bond?
Salt bridge
What is affinity?
the concentration of drug which will occupy half of the receptors
What is Kd?
The concentration of the drug D which is required to occupy 50% of the receptors, D+R DR
If Kd is low what happens to the affinity?
High
What is a radioligand?
A radiolabelled ligand which can be used to find the concentration of the drug that is required to occupy 50% of the receptors.
what is specific binding?
Binding to the receptor
What is non-specific binding?
binding to random sites on the filters
What is saturation?
When all of the target sites are occupied
How is the saturation curve for specific binding obtained?
Subtracting the NSB from the T binding
