TABLE 2.
Estimation of Kb, Kobs, and relative efficacy using equations 57, 58, and 59, respectively
The parameters were estimated from the Tsat and EC50 values of the concentration-response curves shown in Fig. 4. For the calculations, it was assumed that the Tsat of agonist A was a good estimate of Msys. The estimate of the basal response was 20.6%.
Agonist | Tsat | Log EC50 | Log Kb | Log Kobs | Log Relative Efficacya |
---|---|---|---|---|---|
% Msys | |||||
A | 100 | −7.32 | 8.00 | N.D. | N.D. |
B | 96.6 | −6.33 | 7.00 | 4.97 | 0.00 |
C | 73.4 | −5.46 | 6.02 | 4.99 | −1.01 |
D | 34.0 | −5.08 | 5.37 | 5.07 | −1.74 |
E | 13.5 | −6.96 | 6.72 | 6.95 | −2.26 |
F | 5.05 | −6.92 | 6.32 | 7.01 | −2.72 |
G | 0.28 | −6.90 | 5.03 | 6.99 | −4.00 |
N.D., not determined.
Expressed relative to that of agonist B.