Session 8 - Drugs and Receptors Flashcards
How do drugs exert effects in the body?
By binding to target receptors
Name the three biggest targets for drugs
Enzymes
GPCRs
Ion channels
What are agonists?
Substances which mimick the actions of endogenous ligands and cause a response. Has both affinity and intrinsic efficacy.
What are anatgonists?
Substances which block endogenous ligands. Has affinity but NO intrinsic efficacy.
What is the concentration of drug molecules around receptors critical for?
The determination of drug action
What does MWt x Molarity equal?
g/L (mass)
What does g/L / MWt equal?
Molarity
What does g/l / M equal?
MWt
Why is it important to consider molarity?
Because drug molecules can be very different sizes, and so same mass can have vastly disproportional affects.
What is one of the most important factors in determining drug action?
The concentration of drug molecules around receptors is critical in determining drug action
Do drugs at equal molarity have proportional quantaties of drug molecules?
YES THEY DO SILLY
What is binding governed by?
By association and dissociation rates
What is the law of mass action related to?
It is related to the concentration of reactants and products.
How do we measure drug receptor interactions by binding?
By binding radioactively labelled ligands to cells OR membrans prepared from cells.
How many receptors is a large amount on a cell?
10,000 - 100,000
