TABLE 1.
Compound | CB1 Kia | [35S]GTPγ Turnover |
CB2 Kia | [35S]GTPγ Turnover |
||
---|---|---|---|---|---|---|
CB1 EC50b | CB1 Emaxc | CB2 EC50b | CB2 Emaxc | |||
CP55,940 | 0.59 | 23.3 | 124 | 0.30 | 2.1 | 63 |
(0.06) | (4.7) | (9) | (0.04) | (0.8) | (4) | |
7 | 12 | 12 | 6 | 10 | 10 | |
AB-CHMINACA | 0.78 | 7.4 | 205 | 0.45 | 232.4 | 35 |
(0.11) | (1.5) | (14) | (0.03) | (231.2) | (2) | |
3 | 6 | 6 | 3 | 4 | 4 | |
AB-PINACA | 2.87 | 71 | 192 | 0.88 | 14.9 | 41 |
(0.69) | (20.9) | (25) | (0.00) | (8.4) | (1) | |
3 | 6 | 6 | 3 | 4 | 4 | |
FUBIMINA | 296.1 | 2466.3 | 122 | 23.45 | 1269.3 | 56 |
(33.5) | (1037.2) | (7) | (3.21) | (557.1) | (9) | |
4 | 6 | 6 | 3 | 6 | 6 |
Values represent Ki (±S.E.M.) in nM for [3H]CP55,940 displacement at specified (hCB1 or hCB2) receptor.
Values represent EC50 (±S.E.M.) in nM for [35S]GTPγS binding at specified (hCB1 or hCB2) receptor.
Values represent percentage of maximal increase (±S.E.M.) for [35S]GTPγS binding over basal at specified (hCB1 or hCB2) receptor.