Table 2.

Selected dopamine receptor occupancy studies that report a relationship between ARI BL or dose and D₂ occupancy. EC₉₀ estimated from EC₅₀

Reference	Design and subjects	PET tracer	Mean ARI dose (range) [mg/day]	Mean ARI BL (range) [ng/ml]	Mean receptor occupancy (%)	EC50 [ng/ml]	EC90 [ng/ml]	Comment
Kim et al. 2012	RCT; N = 18; healthy volunteers; mean age 23; 100% males	[11C]raclopride	13 ± 12 (2–30)	Peak: 3.4 ± 0.9 per mg	D2/3: 62 ± 21 (s)	11.1 (s)	100 (s)	Values reported for PK model; PK/PD model estimates EC90 of 77 ng/ml (s).
Gründer et al. 2008	CS; N = 16/8 (medicated/ medication-free); SCZ or SAD (DSM-4); mean age 30; 94% males	[18F]fallypride	19 ± 7 (5–30)	245 ± 307	D2/3: 83 ± 1 (p), 84 ± 1 (c)	10 ± 4 (p) 9 ± 4 (c)	90 (p), 81 (c)	Complete occupancy with ARI BL > 100–150 ng/ml. EC90 for AM is 180 ng/ml.
Takahata et al. 2012	CS; N = 11; healthy volunteers; mean age 24 ± 4; 100% males	[11C]raclopride, [11C]FLB457	6	29 ± 5	D2/3: 74 ± 7 (c), 70.1 ± 6.3 (p)	9.9 (s), 12.2 (p)	89 (s), 110 (p)	Concentration reported for raclopride scans; lower in FLB457. No preferential extrastriatal binding of ARI.
Mamo et al. 2007 ; Mizrahi et al. 2009	RCT; N = 12; SCZ or SAD; mean age 31; 75% males	[11C]raclopride, [18F]setoperone, [11C]WAY100635	19 ± 8 (10–30)	221 ± 179	D2/3: 87 ± 4 (p), 92.9 ± 5.7 (c)	NA	NA	ARI and DARI BL correlated with D2 occup. (p and s). No corr. between occup. And clinical or well-being scores. EPS in 2 patients with occupancy > 90%.
Kegeles et al. 2008	CS; N = 19; SCZ or SAD (DSM-4); mean age 29; 79% males	[18F]fallypride	14 ± 11 (2–40)	NA	D2/3: NA 80 ± 15 (s) in 15 mg	ED80 5.6 ± 1.0 (s) ~ 100	NA	Dose correlated with ARI BL, PANSS positive scale correlated with D2 occup. (s). No EPS occured.

c = caudate, CS = cohort study, EPS = extrapyramidal side effects, NA =. Not available, p = putamen, RCT = randomized controlled trial, SCZ = schizophrenia, SAD = schizoaffective disorder, s = striatum