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. 2015 Oct 13;172(20):4790–4805. doi: 10.1111/bph.13250

Table 2.

Schild analysis of arrestin2, PLCβ3 and ERK modulation by CBD

Agonist Slopea R 2 pA2 (μM) ± SEMa IC50 (μM) (95% CI)a
HEK 293A
BRET2 (arrestin2‐Rluc and CB1‐GFP2)
THC, O‐2050 1.02 ± 0.11 0.89 0.84 ± 0.06 0.42 (0.22–0.64)
THC, CBD 0.54 ± 0.06* 0.62 – 0.31 (0.19–0.37)
2‐AG, O‐2050 1.06 ± 0.06 0.95 0.38 ± 0.04** 0.57 (0.29–0.67)
2‐AG, CBD 0.54 ± 0.07* 0.41 – 0.36 (0.21–0.47)
Gαq‐coupled phosphorylation of PLCβ3
THC, O‐2050 0.99 ± 0.05 0.90 1.04 ± 0.13 0.45 (0.35–0.58)
THC, CBD 0.59 ± 0.09* 0.68 – 0.39 (0.29–0.51)
2‐AG, O‐2050 1.03 ± 0.07 0.96 0.29 ± 0.03** 0.58 (0.31–0.73)
2‐AG, CBD 0.48 ± 0.07* 0.38 – 0.31 (0.17–0.46)
GαI/O‐coupled phosphorylation of ERK1/2
2‐AG, O‐2050 0.93 ± 0.15 0.88 0.26 ± 0.03 0.39 (0.09–0.46)
2‐AG, CBD 0.15 ± 0.02* 0.62 – 0.26 (0.19–0.59)
STHdh Q7/Q7
BRET2 (arrestin2‐Rluc and CB1‐GFP2)
THC, O‐2050 0.92 ± 0.09 0.95 0.83 ± 0.21 0.35 (0.27–0.46)
THC, CBD 0.34 ± 0.10* 0.78 – 0.23 (0.16–0.27)
2‐AG, O‐2050 0.97 ± 0.10 0.99 0.35 ± 0.13** 0.52 (0.45–0.59)
2‐AG, CBD 0.35 ± 0.13* 0.70 – 0.63 (0.57–0.89)††
Phosphorylation of PLCβ3
THC, O‐2050 1.05 ± 0.17 0.97 0.93 ± 0.15 0.79 (0.42–0.85)
THC, CBD 0.22 ± 0.08* 0.70 – 0.94 (0.62–1.19)
2‐AG, O‐2050 1.02 ± 0.05 0.99 0.36 ± 0.09** 0.83 (0.46–1.17)
2‐AG, CBD 0.29 ± 0.05* 0.71 – 0.96 (0.75–1.25)
Phosphorylation of ERK1/2
2‐AG, O‐2050 1.06 ± 0.11 0.97 0.36 ± 0.06 0.87 (0.57–0.99)
2‐AG, CBD 0.17 ± 0.08* 0.60 – 0.27 (0.18–0.36)†

Data shown are means ± SEM or with 95% CI, from six independent experiments. CI, confidence interval.

a

Determined using nonlinear regression analysis with a Gaddum/Schild EC50 shift for data presented in Figures 1, 2, 3. IC50 determined at 1 μM agonist. pA2 was not determined where Schild slope was different from 1.

††

Significantly different from the same modulator treatment; as determined by nonoverlapping CI.

†

Significantly different from the same agonist treatment,

**

P < 0.01 compared with the same modulator treatment; one‐way ANOVA with Dunnett's multiple comparison test.

*

P < 0.01 compared with the same agonist treatment,