Table 3.
Agonist | CBD (μM) | EC50 μM (95% CI)a | E max (95% CI)a, b | n (95% CI)a, c | RA ± SEMd |
---|---|---|---|---|---|
HEK 293A | |||||
THC | DMSO | 0.47 (0.27–0.69) | 1.01 (0.82–1.20) | 1.00 (0.76–1.26) | 1.00 ± 0.0 |
0.01 | 0.58 (0.34–0.81) | 0.98 (0.80–1.17) | 0.83 (0.70–1.13) | 0.79 ± 0.17 | |
0.10 | 0.76 (0.59–0.97) | 0.97 (0.81–1.13) | 0.73 (0.67–0.93) | 0.60 ± 0.08* | |
0.50 | 0.86 (0.70–1.07)† | 0.85 (0.70–1.00) | 0.54 (0.41–0.72)† | 0.46 ± 0.05* | |
1.00 | 1.23 (0.85–1.80)† | 0.71 (0.63–0.79)† | 0.36 (0.18–0.51)† | 0.27 ± 0.03* | |
5.00 | 1.26 (0.82–1.58)† | 0.51 (0.41–0.61)† | 0.16 (0.04–0.26)† | 0.19 ± 0.02* | |
2‐AG | DMSO | 0.48 (0.28–0.72) | 1.09 (0.90–1.29) | 1.00 (0.86–1.15) | 1.00 ± 0.0 |
0.01 | 0.63 (0.37–0.96) | 1.11 (0.91–1.30) | 0.92 (0.81–1.02) | 0.84 ± 0.07 | |
0.10 | 0.83 (0.58–1.03) | 1.03 (0.74–1.32) | 0.84 (0.74–1.00) | 0.60 ± 0.07* | |
0.50 | 1.11 (0.95–1.35)† | 0.95 (0.80–1.10) | 0.57 (0.46–0.79)† | 0.41 ± 0.08* | |
1.00 | 1.62 (1.23–1.51)† | 0.78 (0.67–0.88)† | 0.22 (0.07–0.36)† | 0.23 ± 0.01* | |
5.00 | 2.48 (1.72–3.22)† | 0.60 (0.54–0.66)† | 0.13 (0.04–0.24)† | 0.12 ± 0.06* | |
STHdh Q7/Q7 | |||||
THC | DMSO | 0.58 (0.42–0.79) | 0.77 (0.65–0.89) | 1.00 (0.71–1.25) | 1.00 ± 0.0 |
0.01 | 0.72 (0.61–0.85) | 0.73 (0.63–0.82) | 0.54 (0.44–0.82) | 0.77 ± 0.3 | |
0.10 | 0.99 (0.78–1.22) | 0.62 (0.54–0.69) | 0.51 (0.42–0.78) | 0.48 ± 0.1* | |
0.50 | 1.22 (0.85–1.57)† | 0.53 (0.48–0.58)† | 0.55 (0.23–0.64)† | 0.33 ± 0.1* | |
1.00 | 4.00 (2.76–4.32)† | 0.49 (0.37–0.52)† | 0.51 (0.17–0.62)† | 0.10 ± 0.0* | |
5.00 | >5.00 | – | <0.50 | 0.03 ± 0.0* | |
2‐AG | DMSO | 0.66 (0.40–0.85) | 0.73 (0.59–0.87) | 1.00 (0.70–1.18) | 1.00 ± 0.0 |
0.01 | 0.67 (0.48–0.86) | 0.65 (0.56–0.74) | 0.77 (0.55–0.89) | 0.88 ± 0.2 | |
0.10 | 0.78 (0.58–1.01) | 0.61 (0.52–0.70) | 0.57 (0.34–0.74) | 0.71 ± 0.2* | |
0.50 | 0.87 (0.63–0.92) | 0.52 (0.46–0.58)† | 0.39 (0.15–0.58)† | 0.60 ± 0.1* | |
1.00 | 1.04 (0.87–1.61)† | 0.51 (0.43–0.56)† | 0.39 (0.12–0.50)† | 0.45 ± 0.1* | |
5.00 | 1.78 (1.07–2.05)† | 0.42 (0.32–0.51)† | 0.36 (0.09–0.49)† | 0.21 ± 0.0* |
CI, confidence interval.
Data shown are means ± SEM or with 95% CI, from six independent experiments.
Determined using nonlinear regression with variable slope (four parameters) analysis.
Maximal agonist effect BRETEff.
Hill coefficient.
Relative activity, as determined in equation (2).
Significantly different from the DMSO vehicle as determined by non‐overlapping CI.
P < 0.01, compared with DMSO vehicle; one‐way ANOVA with Dunnett's multiple comparison test.