Receptor Theory Flashcards
What is affinity?
The ability of a ligand to bind to a target
What is efficacy?
The ability of a ligand to generate an effect at a target
What is Emax?
The maximal effect of a ligand
What is EC50?
The concentration of a ligand at which the effect is half maximal
What is potency?
The concentration of a drug needed to cause an effect
What is a partial agonist?
Produce a submaximal effect from a target
Which have lower efficacy, full or partial agonists?
Partial
Are partial agonists able to produce a maximal effect of concentration is increased?
No
What is an inverse agonist?
Induce the opposite effect at a target
What happens to Emax and EC50 when there is a reversible competitive antagonist and you increase the concentration of agonist?
Emax will not change
EC50 will increase
What effect do non-competitive antagonists have on Emax and EC50?
Decrease Emax
No change in EC50
What do irreversible antagonists do to Emax?
Reduce it
How do you overcome irreversible antagonists?
Express new receptors
What do allosteric modulators do?
Generate conformational changes to the receptor which either positively or negatively affects its ability
What is the therapeutic range?
Dose range between minimal effect and toxic effect
