Pharmacodynamics Flashcards
Describe using isolated tissue to measure efficacy
Place isolated tissue in an organ bath, suspended from a load transducer which measure the tension changes caused by different agonists/antagonists
Why do we use different types of tissues to measure responses?
Different tissues have different types of receptors on their surface
What is EC50?
The concentration of drug when 50% of the maximum response is given
What is alpha?
The maximum response of a isolated tissue
What is a partial agonist?
An agonist that will never give 100% of the maximum response
What is a surmountable antagonist?
An antagonist where the response can be regained by adding more of the agonist
What is an insurmountable antagonist?
An antagonist where the response can never be regained, regardless of the concentration of agonist added
What is pA2?
The concentration of antagonist that requires a 2-fold increase of agonist concentration to regain the response level
What is Kb?
The affinity of the antagonist
How does pA2 relate to Kb?
pA2 = -log Kb
How can we use recombinant DNA technology in drug discovery?
Manipulate the genes of a cell line to force expression of a receptor that we need to test drugs for