Table 2.
Functional Potencies (EC50) of Selected (−)-Δ8-THC Ester Analogues for the rCB1 Cannabinoid Receptor
compd | rCB1 (EC50, nM)a
|
E(max) (%)d | |
---|---|---|---|
3-pointsb | 8-pointsc | ||
7a | 10–100 | ||
2b | <1 | 0.5 (0.1–1.2)e | 92e |
8b | 1–10 | ||
10a | <1 | 0.9 (0.3–1.5) | 89 |
10b | 1–10 | ||
7b | 1–10 | ||
18 | 1–10 | ||
2c | <1 | 0.4 (0.2–1.2)e | 90e |
7c | 1–10 |
Functional potencies at rCB1 receptor were determined by measuring the decrease in forskolin-stimulated cAMP levels, as described in Experimental Section.16,18
Three point data were obtained from one experiment (3 points) run in duplicate (less accurate EC50 values).
Data are average of two independent experiments (8 points) run in triplicate, and 95% confidence intervals for the EC50 values are given in parentheses. EC50 values were calculated using nonlinear regression analysis.
Forskolin stimulated cAMP levels were normalized to 100% and E(max) is the maximum inhibition of forskolin stimulated cAMP levels and is presented as the percentage of CP-55,940 response at 500 nM.
Reported previously.16