Table 1. Functional Activity of Δ9-THC, WIN 55,212-2, and 5–12 at Rat CB1 and Human CB2 Receptors.
| rCB1 |
hCB2 |
||||
|---|---|---|---|---|---|
| compd | pEC50 ± SEM (EC50, nM) | max ± SEM (% WIN 55,212-2) | pEC50 ± SEM (EC50, nM) | max ± SEM (% WIN 55,212-2) | CB1 selectivitya |
| 1 (Δ9-THC) | 7.24 ± 0.12 (58) | 78 ± 5 | n.d. | 13 (at 10 μM) | |
| 3 (WIN 55,212–2) | 7.57 ± 0.14 (27) | 6.93 ± 0.1 (117) | 4.3 | ||
| 5 (AB-001) | 7.46 ± 0.16 (35) | 105 ± 8 | 7.32 ± 0.12 (48) | 86 ± 6 | 1.4 |
| 6 (SDB-001) | 7.47 ± 0.12 (34) | 98 ± 6 | 7.54 ± 0.11 (29) | 91 ± 5 | 0.9 |
| 7 (AB-002) | 7.43 ± 0.13 (37) | 90 ± 6 | 7.05 ± 0.13 (89) | 82 ± 7 | 2.4 |
| 8 (SDB-002) | 7.37 ± 0.12 (43) | 84 ± 6 | 7.24 ± 0.26 (57) | 23 ± 4 | 1.3 |
| 9 (SDB-003) | 7.43 ± 0.16 (37) | 93 ± 7 | 6.99 ± 0.08 (102) | 95 ± 5 | 2.7 |
| 10 (SDB-004) | 7.79 ± 0.19 (16) | 94 ± 8 | 6.67 ± 0.09 (216) | 71 ± 5 | 13.1 |
| 11 (SDB-005) | 7.68 ± 0.11 (21) | 99 ± 6 | 6.86 ± 0.12 (140) | 74 ± 6 | 6.7 |
| 12 (SDB-006) | 7.73 ± 0.11 (19) | 85 ± 5 | 6.88 ± 0.22 (134) | 68 ± 9 | 7.2 |
a
CB1 selectivity expressed as the ratio of CB2 EC50 to CB1 EC50. n.d. = not determined.