Relative agonist activity
as a function of changing receptor density.
Values of log(τ/KA), pEC50, and log(RA) for two agonists (one designated with a solid line
and the other with a dotted line) were calculated for a range of τ
values. (A) Because values of log(τ/KA) do not change with receptor density, the ratio Δlog(τ/KA) remains constant over all ranges of receptor
density. (B and C) The pEC50 values change with receptor
density for transducer slope coefficients of ≠1, leading to
variance and reversal of ΔpEC50 values with receptor
density (or changes in receptor coupling efficiency, KE). (D and E) Values of log(RA) change with τ values
for slope coefficients of ≠1, leading to differences in the
value of Δlog(RA) with varying receptor density as simulated
by changes in τ.