Table 3.
Effect | Parameter | MOR‐WT | MOR‐WT | MOR‐WT | MOR‐H297A |
---|---|---|---|---|---|
pH 7.4 | pH 6.5 | pH 6.0 | pH 7.4 | ||
Fentanyl‐induced cAMP reduction |
IC50 (nM) [95% CI] log (IC50) |
1.3 [0.7, 2.4] −8.90 ± 0.14 |
1.4 [0.5, 4.0] −8.71 ± 0.33 |
1.8 [0.4, 8.6] −8.74 ± 0.34 |
33.4 [5.6, 198.6] −7.48 ± 0.40* |
Bottom (%) | 28.8 ± 2.1 | 33.2 ± 2.9 | 39.5 ± 4.0 | 53.3 ± 4.7* | |
Naloxone antagonism of fentanyl‐induced cAMP reduction |
IC50 (μM) [95% CI] log (IC50) |
14.4 [5.8, 35.9] −4.84 ± 0.20 |
2.6 [0.9, 7.7] −5.58 ± 0.25* |
18.7 [7.6, 45.6] −4.73 ± 0.20 |
|
Top (%) | 93.1 ± 5.7 | 58.7 ± 3.4* | 106.3 ± 6.3 |
Note. Data are means ± SEM or means with 95% CI. Bottom: bottom of curve fit (maximum fentanyl effect); Top: top of curve fit (maximum reversal of fentanyl effect); log (IC50), Bottom and Top were each compared by one‐way ANOVA with Dunnett's Multiple Comparison post hoc test, control group = MOR‐WT pH 7.4.
P < 0.05, n = 6 per experiment.