Receptor Binding Equations and Related Terminology

Question 1

The REVERSIBILITY of binding together with receptor saturation lead to the following fundamental equation ____

Answer 1

[RD] = [Rt] x [D]/Kd+[D]

Question 2

Rt, D, Rd, Kd stand for the following _____.

Answer 2

Rt - total number of receptors
D = greg drug concentration (NOT bound to receptor)
Rd = drug-receptor complex (drug BOUND to receptor)
Kd = “equilibrium dissociation constant” for the drug and its receptor

Question 3

Kd is the ______.

Answer 3

Equilibrium dissociation constant for the drug and its receptor.

Question 4

What parameters determine [RD] complex and what the response is going to be?

Answer 4

[Rt], [D], and Kd.

Question 5

Fraction of receptors occupied, or FRO is equivalent to what?

Answer 5

Drug bound to receptor divided by total # of receptors = ([RD]/[Rt])…. OR the Free Drug Concentration divided by the equilibrium dissociation constant plus free drug concentration = ([D]/Kd+[D])

Question 6

When drug concentration is equal to Kd (equilibrium dissociation constant) then ____.

Answer 6

the fraction of receptors occupied is 50%.