Table 1.
Binding affinity and Tetrad Tests of 1-Fluoro-1-deoxy-THCs
| Compound | structure | CB1 (nM) | CB2 (nM) | Tetrad Tests (ED50, mg/kg) | TF (i.t.) | ||
|---|---|---|---|---|---|---|---|
| SA | TF | RT | μg/mouse | ||||
| Δ9-THC | 40.7 ± 1.7 a | 36.4 ± 10 b | 1.0 | 1.4 | 1.4 | 29 (24–36) c | |
| 4 | >10,000 | >4550 | 8% @ 30 mg | 4% @ 30 mg | −2.2°@ 30 mg | 156.9 (114.1–216) | |
| (O-964) |
|
36 ± 0.8 | - | 3.68 | 3.24 | 2.96 | - |
| 5 | 285 ± 34 | 40 ± 8 | 0.51 | 5.8 | 4.1 | 99.5 (62.5–158) | |
| (O-1317) |
|
0.86 ± 0.09 | - | 0.09 | 0.09 | 0.13 | - |
| 6 | 1557 ± 203 | 1508 | 31.1 | 21.5 | 6.9 | 36% @ 100μ g | |
*
Behavioral Evaluation (tetrad tests); SA (spontaneous activity), TF (tail-flick), RT (rectal temperature), RI (ring immobility) were carried out in mice. The ED50 data is given in mg/kg. For details see references 17 and 8. RI test was not carried out f or any of the compounds and is therefore not given.
a
see reference 9.
b
see reference 6.
c
The results are presented as ED50 (95% confidence limits in parenthesis); see reference 18.