Agonists Flashcards
Define ligand.
A molecule that binds to a receptor
Define ligand.
A molecule that binds to a receptor
Define receptor.
Protein that detects a signal molecule and performs an action in response
How are receptors defined.
Possess structural and steric specificity, expressed in select tissues, saturable and finite, high affinity for endogenous ligand at [physiological], biochemical event occurs when ligand binds its receptor.
What is meant by a dose-response relationship.
Tissue responses are generally directly proportional to the fraction of receptors occupied with agonist
What is meant by Kd.
Dissociation constant. 1/Kd is affinity
Define Emax.
Maximal response that can be produced by the drug.
What is IC50?
Concentration of inhibitor required to reduce enzyme activity by 50%
Discuss the mechanism by which partial agonists work for the different receptor types.
Bind to receptor site up to point of saturation but do not elicit Emax.
Define agonist.
Drugs that produce a response
Define antagonist.
A drug that binds to the receptor to block or prevent an action or effect.
Define partial agonist.
Binds to a receptor but will not cause the maximal response
Define intrinsic activity.
AKA efficacy of a drug; the capacity of a drug to activate the receptor: ability to produce an effect.
Define efficacy
The ability to produce a desired or intended result.
Define potency.
Amount of drug needed for an effect of given intensity.
