TRV130 | cAMP | β-Arrestin-2 | [3H]Diprenorphine | |||||||
---|---|---|---|---|---|---|---|---|---|---|
pEC50 | S.D. | EC50 | Efficacy (%) | pEC50 | S.D. | EC50 | Efficacy (%) | Ki high | Ki low | |
nM | nM | nM | nM | |||||||
hMOR | 8.1 | 0.04 | 7.9 | 83 | 7.4 | 0.22 | 40.0 | 14 | 6 ± 1.7 | 551 ± 263 |
mMOR | 9.4 | 0.06 | 0.4 | 104 | 7.9 | 0.06 | 12.6 | 74 | 1 ± 0.3 | 39 ± 21 |
rMOR | 8.4 | 0.03 | 4.0 | 90 | N.Q. | 18 ± 3.7 | 203 ± 26 | |||
dMOR | 8.3 | 0.01 | 5.0 | 92 | 8.0 | 0.02 | 9.4 | 24 | N.D. | |
hNOP | 6.4 | 0.09 | 398 | 58 | N.Q. | N.D. | ||||
hKOR | 5.8 | 0.03 | 1585 | 58 | N.Q. | >10,000 | ||||
hDOR | 5.5 | 0.04 | 3162 | 46 | N.Q. | N.D. |
d, dog; h, human; m, mouse; N.D., not determined; N.Q., not quantifiable; r, rat.