Table 3
In vitro and in vivo cannabinoid effects of bicyclic resorcinols with methylated cyclohexane
| ID | R | R1 | Ki(nM) | CB1/CB2 | ED50 | ||||
|---|---|---|---|---|---|---|---|---|---|
| CB1 | CB2 | SA | TF | RT | |||||
| 13 | O-1658 |
| DMH | 16 ± 2 | 1 ± 0.3 | 16 | 0.2 (0.1–0.3) | 0.3 (0.2–0.3) | 0.3 (0.27–0.5) |
| 14 | O-1659 | DMH | 45 ± 1 | 5 ± 0.9 | 9 | 4.8 (3–9) | 3.9 (3–6) | 3.3 (2–5) | |
| 15 | O-1663 | DMH | 144 ± 22 | 9 ± 2 | 16 | 32% (30) | 7% (30) | −2.2 (30) | |
| 16 | O-1657 | DMH | 14 ± 0.5 | 0.8 ± 0.04 | 17 | 0.3 (0.3–0.5) | 0.6 (0.5–1) | 0.9 (0.7–1.1) | |
| 17 | O-1797A | DMH | 5 ± 0.6 | 0.4 ± 0.03 | 12 | 0.5 (0.4–0.6) | 1.1 (0.8–1.5) | 0.7 (0.6–1.0) | |
| 18 | O-1798B |
| DMH | 4 ± 0.6 | 0.5 ± 0.07 | 8 | 0.2 (0.03–1.2) | 1.0 (0.7–1.6) | 0.6 (0.5–0.7) |
| 19 | O-1826 | DMH | 40 ± 11 | 0.8 ± 0.05 | 50 | 2.7 (2.1–3.9) | 2.4 (1.8–3.3) | 3.6 (2.7–4.5) | |
| 20 | O-1890 | Dimethylbutyl | 96 ± 4 | 13 ± 1 | 7 | 69 (55–90) | 48 (31–69) | 72 (45–114) | |
| 21 | O-1871 | DMH | 2 ± 0.3 | 0.3 ± 0.01 | 7 | <1.03-a | 2.3 (2.0–2.6) | 1.3 (0.3–4.3) | |
The Ki values are presented as means ± S.E.M. All ED50 values are expressed as micromole per kilogram (with 95% confidence limits in parentheses). For compounds that failed to produce either maximal or dose-related effects, the percent effect at the highest dose (mg/kg; in parentheses) is provided.
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SA, suppression of spontaneous activity; RT, rectal temperature; TF, tail flick.
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↵3-a This dose (μmol/kg) produced >50% inhibition and was the lowest dose tested.