Pharmacodynamics Flashcards
1
Q
Define intrinsic efficacy
A
The ability of a ligand to cause a conformational change of the receptor
2
Q
Define ligand efficacy
A
The ability of a ligand to cause a measurable cell response
3
Q
How do we define agonist potency
A
The concentration of the drug that evokes EC50
EC50 = 50% of its maximal response (EMax)
4
Q
What is the measurement used to define affinity
A
Kd (Dissociation Constant)
Concentration of ligand at which 50% of all available receptors are bound
5
Q
Define affinity
A
The measure of strength to which a ligand binds to a receptor
6
Q
What is a partial agonists
A
A ligand that evokes a response that are lower than the maximal response of a full agonist
(I.e. have lower EMax Values)
7
Q
Compared to a full agonist, a partial agonist has …
A
It has a lower intrinsic efficacy
