NA, not available.
MOR | β-Arrestin1 | β-Arrestin2 | |||||||
BRET | β-Gal | BRET | β-Gal | ||||||
pEC50 | Emax (% of WT DAMGO) | pEC50 | Emax (% of WT DAMGO) | pEC50 | Emax (% of WT DAMGO) | pEC50 | Emax (% of WT DAMGO) | ||
WT | DAMGO | 6.05 ± 0.06 | 100 | 5.82 ± 0.07 | 100 | 6.28 ± 0.04 | 100 | 5.94 ± 0.03 | 100 |
Morphine | — | — | — | — | 6.12 ± 0.05 | 33.57 ± 2.18 | — | — | |
TSST-4A | DAMGO | 6.10 ± 0.06 | 91.59 ± 1.56 | 5.86 ± 0.05 | 36.33 ± 6.79^ | 6.36 ± 0.02 | 94.08 ± 3.76 | 5.58 ± 0.05 | 56.73 ± 7.61^ |
Morphine | — | — | — | — | 5.85 ± 0.14 | 29.21 ± 4.11 | — | — | |
S375A | DAMGO | 5.89 ± 0.07 | 36.20 ± 6.27^ | 6.71 ± 0.13 | 32.20 ± 5.73^ | 6.30 ± 0.01 | 71.73 ± 6.47^ | 6.08 ± 0.18 | 49.36 ± 16.95^ |
Morphine | — | — | — | — | 6.37 ± 0.14 | 17.31 ± 0.90^ | — | — | |
STANT-3A | DAMGO | — | — | NA | NA | 6.20 ± 0.06 | 56.26 ± 1.81^ | NA | NA |
Morphine | — | — | NA | NA | 6.40 ± 0.08 | 14.76 ± 1.66^ | NA | NA | |
TREHPSTANT-4A | DAMGO | — | — | 5.95 ± 0.48 | 28.47 ± 7.18^ | NA | NA | 5.72 ± 0.05 | 42.55 ± 6.31^ |
Morphine | — | — | — | — | NA | NA | — | — | |
11S/T-A | DAMGO | — | — | 8.27 ± 1.74 | 23.46 ± 2.33^ | 6.16 ± 0.02 | 41.90 ± 5.48^ | 6.08 ± 0.17 | 43.73 ± 5.16^ |
Morphine | — | — | — | — | 6.29 ± 0.08 | 15.92 ± 1.67^ | — | — |
^Significance compared to WT (P < 0.01) by two-way ANOVA with Dunnett’s multiple comparison test.