Drug/Receptor Theory Flashcards
Irreversible antagonist
A pharmacologic antagonist that cannot be overcome by increasing agonist concentration
Physiologic antagonist
A drug that counters the e!ects of another by binding to a di!erent receptor and causing opposing e!ects
Allosteric (noncompetitive) agonist, antagonist
A drug that binds to a receptor molecule without interfering with normal agonist binding but alters the response to the normal agonist
Partial agonist
A drug that binds to its receptor but produces a smaller e!ect (Emax) at full dosage than a full agonist
Inverse agonist
A drug that binds to the non-active state of receptor molecules and decreases constitutive activity/inverts Emax
Graded dose- response curve
A graph of the increasing response to increasing drug concentration or dose
Agonist
anything that binds to an effector and causes an effect
Quantal dose- response curve
A graph of the increasing fraction of a population that shows a specified response at progressively increasing doses
Spare receptor
Receptor that does not bind drug when the drug concentration is su!icient to produce maximal e!ect; present when Kd > EC50
Receptor site
Specific region of the receptor molecule to which the drug binds
How do spare receptors increase potency?
need lower drug concentrations to reach max effect
EC50
drug concentration at which you get 50% of the max response/potency
What is the relationship between EC50 and potency?
smaller EC50=greater potency
Antagonist
any drug/molecule that block the effect of an agonist