Potency and maximal effect estimates for the stimulation of luciferase reporter gene activity by CP 55,940 in human CB1-expressing Chinese hamster ovary cells pEC50 is the negative logarithm of the agonist EC50 value and Emax is the maximal agonist effect, both determined using nonlinear regression analysis according to eq. 4 under Materials and Methods. Values shown in parentheses are 95% confidence limits.
| Modulator & Parameter | Modulator Concentration | ||||||
|---|---|---|---|---|---|---|---|
| 0 (Vehicle) | 3 nM | 10 nM | 30 nM | 100 nM | 300 nM | 1 μM | |
| Org 27569 | |||||||
| Emax | 123 (118–127) | 135 (132–138) | 93 (91–96) | 46 (45–48) | 3.81 (3.45–4.17) | ||
| pEC50 | 8.29 ± 0.07 | 8.67 ± 0.04** | 9.01 ± 0.05** | 9.30 ± 0.09** | |||
| Org 27759 | |||||||
| Emax | 103 (100–106) | 104 (102–106) | 93 (91–95) | 69 (68–71) | 26 (25–27) | ||
| pEC50 | 8.22 ± 0.06 | 8.45 ± 0.03* | 8.56 ± 0.04** | 8.80 ± 0.04** | 9.50 ± 0.08** | ||
| Org 29647 | |||||||
| Emax | 105 (101–109) | 105 (100–109) | 108 (104–111) | 90 (87–92) | 52 (50–54) | 25 (23–26) | 4.75 (4.16–5.33) |
| pEC50 | 8.59 ± 0.07 | 8.67 ± 0.08 | 8.56 ± 0.06 | 8.73 ± 0.06 | 9.17 ± 0.08** | 9.58 ± 0.12** | |
↵** P < 0.01, one-way analysis of variance followed by Dunnett's post test