Drug receptor theory

Question 1

Explain the relationship between Kd and EC50

Answer 1

EC50 is the measure of response and is shifted more to the left in comparison to Kd due to the receptor reserve theory= More receptors than needed to produce a sufficient response- the more spare receptors= the more shifted to the left it is

Question 2

What are concentration response curves determined by?

Answer 2

They depend on the tissue machinery and how that effects efficacy e.g. secondary messengers can amplify the signal which means there are different max responses

Question 3

What determines a partial agonist?

Answer 3

Can’t produce a max response unless all the receptors are occupied. For a PA the EC50 is equal to the Kd

Question 4

How is response measured? (the equation)

Answer 4

(max response x agonist conc^slope factor)/(agonist con ^slope factor x Ec50^slope factor)