Compound | R | Receptor Affinitiesa | Effects in Miceb | |||||
---|---|---|---|---|---|---|---|---|
[3H]CP55,940 | [3H]SR144528 | CB2 | SA | %MPE | RT | RI | ||
O-4424 | 169 | 45 | >10,000 | N.T. | N.T. | N.T. | N.T. | |
(0.4) | (3) | |||||||
O-6211 | 138 | 52 | >10,000 | 2 | 6 | 4 | 12 | |
(3) | (3) | (1–4) | (4–10) | (2–4) | (8–16) | |||
O-6212 | 86 | 41 | >10,000 | 81 | 100 | −3.7 | Ataxia | |
(6) | (1) | (59) | (59) | (59) | (59) | |||
O-6617 | 85 | 43 | >10,000 | 12 | 8 | 19 | Ataxia | |
(3) | (1) | (6–17) | (6–12) | (13–25) | (58) | |||
O-6618 | 89 | 44 | >10,000 | 9 | 13 | 13 | 36 | |
(10) | (2) | (4–15) | (9–17) | (9–15) | (22–52) | |||
O-6213 | 182 | 91 | >10,000 | <17 | 9 | 10 | 10 | |
(18) | (6) | (5–14) | (7–14) | (7–15) | ||||
O-6215 | 332 | 221 | >10,000 | 9 | 13 | 7 | Ataxia | |
(52) | (12) | (5–13) | (9–18) | (5–11) | (54) | |||
O-6214 | 88 | 56 | >10,000 | 42 | 100 | −2.7 | Ataxia | |
(4) | (2) | (59) | (59) | (59) | (59) | |||
O-6629 | 24 | 20 | >10,000 | <2 | 1.5 | 1.3 | 4 | |
(5) | (1) | (0.6–4) | (0.6–2) | (2–6) | ||||
O-6658 | 57 | 46 | >10,000 | 1 | 2 | 2 | 12 | |
(11) | (2) | (0.4–2) | (0.9–4) | (1–4) | (6–24) | |||
O-6659 | 109 | 128 | >10,000 | 6 | 16 | 12 | ∼59 | |
(7) | (6) | (4–12) | (10–26) | (6–18) |
N.T., not tested.
↵a Ki values are nanomolar S.E.M. values for receptor affinities are shown in parentheses.
↵b Values shown are ED50 (95% confidence intervals in parentheses). Single dose tests are indicated by magnitude of effect, with dose that was tested in parentheses. All doses are expressed as micromoles per kilogram.