Lecture 8 Flashcards
Receptor Theory II
The Hill Equation
Response=max.[Xa]^n/[Xa]^n + [EC50]^n
The slope factor
n in Hill equation
Related to how many molecules of agonist need to bind to a receptor in order to activate it
Potency depends on
Affinity
Efficacy
Receptor reserve
Low EC50…
Indicates a high potnecy
because a low conc. is required to elicit a response
Different agonists with different efficacies
Have different maximum responses
But still the same EC50 value
Partial agonist
Cannot produce the maximal response
Efficacy
The measure of a single agonist-receptor complexes ability to generate a response
Uses scale 1-0
Maximum response for a partial agonist
Can only be achieved with full occupation of receptors
In full agonists, EC50…
Does not = KD
Specificity
Interact with a structurally defined site/receptor
Chemical properties. molecular structure
Efficacy and drugs
major role in defining drug
Expression level of receptors will affect where the conc. response curve lies