TABLE 1

The effects of haloperidol on BRET² (Gα_i-Rluc + CB₁-GFP²), Gα_i-dependent ERK phosphorylation, BRET² (Gα_s-Rluc + CB₁-GFP²), Gα_s-dependent CREB phosphorylation, and BRET² (β-arrestin1-Rluc + CB₁-GFP²)

Determined using nonlinear regression with variable slope (four parameter) in GraphPad (version 6.0). Data shown are 95% CI, from four independent experiments.

Agonist	HALO (μM)	EC₅₀μM (95% CI)	E_Max (95% CI)	Hill Coefficient  (95% CI)
BRET² (Gα_i-Rluc + CB₁-GFP²)	0	0.22 (0.19 –0.28)	0.45 (0.41-0.48)	1.15 (0.91–1.40)
ACEA	0.01	0.25 (0.21–0.32)	0.36 (0.33-0.38)^*	0.90 (0.86–0.94)
	0.1	0.38 (0.32–0.43)^*	0.33 (0.26-0.39)^*	0.82 (0.76–0.89)^*
	1	0.68 (0.33–0.92)^*	0.23 (0.21-0.25)^*	0.71 (0.67–0.75)^*
	10	0.98 (0.94–1.41)^*	0.17 (0.14-0.20)^*	0.57 (0.60–0.54)^*
Gα_i-dependent ERK phosphorylation	0	0.27 (0.25–0.29)	0.76 (0.71–0.80)	1.11 (0.89–1.23)
ACEA	0.01	0.31 (0.26–0.36)	0.69 (0.64–0.75)	0.93 (0.84–1.03)
	0.1	0.41 (0.37–0.45)^*	0.52 (0.48–0.57)^*	0.84 (0.78–0.89)
	1	0.72 (0.67–0.78)^*	0.39 (0.37–0.42)^*	0.79 (0.69–0.79)^*
	10	1.01 (0.82–1.21)^*	0.32 (0.29–0.34)^*	0.74 (0.67–0.81)^*
BRET² (Gα_s-Rluc + CB₁-GFP²)	0	N.C.	N.C.	N.C.
ACEA	0.01	0.49 (0.36–0.62)^*	0.18 (0.16–0.19)^*	1.12 (0.92–1.32)^*
	0.1	0.35 (0.29–0.42)^*	0.26 (0.24–0.27)^*	1.28 (1.21–1.36)^*
	1	0.29 (0.24–0.35)^*	0.31 (0.28–0.33)^*	1.43 (1.36–1.51)^*
	10	0.23 (0.18–0.31)^*	0.36 (0.32–0.40)^*	1.53 (1.43–1.63)^*
Gα_s-dependent CREB phosphorylation	0	0.35 (0.31–0.40)	0.26 (0.23–0.28)	1.02 (0.90–1.14)
ACEA	0.01	0.31 (0.29–0.35)	0.42 (0.40–0.45)^*	1.11 (0.98–1.31)
	0.1	0.29 (0.23–0.48)^*	0.56 (0.53–0.59)^*	1.26 (1.10–1.42)^*
	1	0.23 (0.19–0.27)^*	0.65 (0.62–0.68)^*	1.56 (1.17–1.86)^*
	10	0.21 (0.17–0.25)^*	0.70 (0.67–0.74)^*	1.67 (1.42–1.91)^*
BRET² (β-arrestin1-Rluc + CB₁-GFP²)	0	0.25 (0.19–0.35)	0.56 (0.52–0.60)	1.21 (0.11–1.23)
ACEA	0.01	0.27 (0.21–0.37)	0.53 (0.49–0.56)	1.12 (0.98–1.10)
	0.1	0.33 (0.28–0.51)^*	0.48 (0.45–0.52)	1.01 (0.95–1.21)
	1	0.36 (0.29–0.44)^*	0.38 (0.36–0.41)^*	1.12 (0.90–1.12)
	10	0.45 (0.34–0.57)^*	0.32 (0.29–0.34)^*	1.04 (0.85–1.11)

Cl, confidence interval; N.C. not converged.
↵* P < 0.01, compared with ACEA-treated cells; one-way ANOVA with Tukey’s posthoc test.