Table 2.
Cyclase and FLIPR functional assays
| Ligands |
Mean agonist EC50, nM (n), efficacy % relative to CP 55,940 (%) |
|||||
|---|---|---|---|---|---|---|
|
95% CI of EC50 values, nM |
||||||
|
Cyclase assays |
FLIPR assays |
|||||
| hCB1 | hCB2 | rCB1 | rCB2 | hCB2 | rCB2 | |
| A-796260 | 983 (7), 118 | 0.710 (6), 78 | 286 (8), 97 | 1.63 (7), 69 | 17.3 (8), 71 | 31.0 (4), 39 |
| 618–1560 | 0.315–1.60 | 206–397 | 0.505–5.28 | 10.64–28.2 | 7.87–125 | |
| WIN 55,212-2 | 47.2 (5), 113 | 0.650 (5), 98 | 16.5 (5), 114 | 1.16 (6), 46 | 119 (10), 74 | >10 000 (13) |
| 23.5–94.9 | 0.156–2.72 | 3.74–72.5 | 0.367–3.65 | 57.94–245 | ||
| CP 55,940 | 1.81 (12), 103 | 0.864 (41), 106 | 4.12 (17), 103 | 0.682 (42), 99 | 31.3 (212), 99 | 13.0 (29), 106 |
| 0.777–4.21 | 0.626–1.19 | 2.51–6.76 | 0.444–1.05 | 28.3–34.5 | 9.44–17.8 | |
| AM1241 | 2650 (5), 101 | >1000 (9) | 1970 (6), 81 | >1000 (8) | >10 000 (18) | >10 000 (9) |
| 1730–4050 | 842–4610 | |||||
| SR144528 | 9420 (4), 52 | 73.4 (20), −106 | 5960 (3), 39 | 34.3 (17), −75 | >10 000 (12) | >10 000 (6) |
| 4340–20 400 | 48.4–111 | 1780–20 000 | 24.9–47.3 | |||
| SR141716A | 21.3 (4), −67 | >3000 (4) | 31.6 (7), −61 | >3000 (2) | >10 000 (3) | >10 000 (6) |
| 5.73–79.1 | 16.2–61.8 | |||||
| GW-842166X | >25 000 (2) | 133 (4), 101 | 26 000 (4), 33 | 96.2 (6), 95 | 7780 (5), 84 | ND |
| 94–187 | 24 200–27 900 | 65.5–141 | 2700–22 400 | |||
| L-768,242 (GW405833) | ND | 44.4 (2), −30 | 916 (2), 70 | 3.26 (4), −39 | >10 000 (4) | ND |
| 22.4–88.1 | 839–1000 | 1.09–9.78 | ||||
Abbreviation: ND, not determined.