Table 3 Potency (pEC50) and maximal response (Emax) of GRK2 recruitment to phosphorylation-deficient MOR mutants.
MORBRETβ-Gal
pEC50Emax
(% of WT DAMGO)
pEC50Emax
(% of WT DAMGO)
WTDAMGO6.22 ± 0.141006.39 ± 0.12100
Morphine6.37 ± 0.2037.88 ± 7.226.57 ± 0.36 (0.27)56.13 ± 9.64
TSST-4ADAMGO6.50 ± 0.1399.02 ± 9.385.72 ± 0.1145.35 ± 1.58^
Morphine6.47 ± 0.0842.72 ± 11.93
S375ADAMGO6.08 ± 0.0586.02 ± 3.795.80 ± 0.0940.15 ± 7.32^
Morphine5.92 ± 0.2730.36 ± 7.33
STANT-3A/
TREHPSTANT-4A
DAMGO5.77 ± 0.1558.33 ± 6.62^6.15 ± 0.3836.73 ± 4.27^
Morphine5.63 ± 0.5126.77 ± 5.45
11S/T-ADAMGO5.77 ± 0.0853.33 ± 2.48^6.13 ± 1.4633.86 ± 3.64^
Morphine5.57 ± 0.0523.20 ± 3.11

^Significance compared to WT (P < 0.01) by two-way ANOVA with Dunnett’s multiple comparison test.