TABLE 3

ED50 values (milligram/kilogram, subcutaneously; 95% confidence limits are in parentheses) of JNJ-37822681 and seven reference compounds for D2 receptor occupancy and inhibition of stimulant-induced behavior 1 h after subcutaneous administration

Test CompoundED50
D2 Occupancy In VivoInhibition of Apomorphine-Induced StereotypyBlockade of Apomorphine-Induced StereotypyInhibition of d-Amphetamine HyperlocomotionInhibition of Phencyclidine Hyperlocomotion
JNJ-378226810.39 (0.31–0.49)0.19 (0.14–0.26)8.1 (6.0–11)1.0 (0.68–1.5)4.7 (3.3–6.6)
Aripiprazole0.58 (0.44–0.76)0.59 (0.43–0.80)5.4 (4.0–7.3)0.26 (0.16–0.41)3.6 (2.0–6.5)
Clozapine8.5 (6.2–12)16 (12–22)>1602.0 (1.5–2.8)3.6 (2.4–5.3)
Haloperidol0.018 (0.014–0.022)0.028 (0.023–0.035)0.26 (0.19–0.35)0.064 (0.048–0.087)0.112 (0.075–0.17)
Olanzapine0.15 (0.13–0.17)0.22 (0.15–0.33)7.1 (5.2–9.6)1.0 (0.75–1.4)1.0 (0.68–1.5)
Quetiapine13 (9.6–17)12 (8.3–18)>1604.7 (3.1–7.0)14 (12–18)
Risperidone0.11 (0.09–0.14)0.26 (0.16–0.40)2.7 (2.0–3.6)0.44 (0.36–0.55)0.51 (0.32–0.83)
Ziprasidone0.24 (0.18–0.36)0.28 (0.20–0.38)4.7 (3.4–6.3)0.29 (0.19–0.35)1.2 (0.78–1.8)