TABLE 1

Overview of effects in rat test models of positive psychotic symptoms of schizophrenia and CNS side effects

Results are expressed as ED50 values (milligram per kilogram) with 95% CI. Drug pretreatment times are shown in parentheses with exceptions in footnotes.

EffectNo. in GroupED50
Brexpiprazole (1 h)aAripiprazole (2 h)bRisperidone
(1 h)c
mg/kg p.o. (95% CI)
Efficacy tests
 CAR4–66.0 (4.3–9.7)23 (20–27)3.3 (2.0–7.6)
 APO hyperactivity (0.25 mg/kg)52.3 (1.2–3.1)3.2 (1.9–5.0)NT
 APO stereotypy (0.7 mg/kg)62.9 (2.2–3.8)6.1 (5.2–7.2)4.7 (2.9–6.9)
 AMPH hyperactivity (0.5 mg/kg)80.92 (0.6–1.5)3.9 (2.0–7.7)NT
CNS side effects
 Inhibition of spontaneous locomotor activity83.4 (2.4–5.0)6.1 (2.3–16)NT
 Catalepsy (at time of maximum effect)620 (12–40)42 (26–68)6.6 (2.9–16)
  • AMPH, amphetamine; APO, apomorphine; NT, not tested.

  • a Except for spontaneous locomotor activity, amphetamine-induced hyperactivity (2 hours) and catalepsy (maximum effect at 6 hours).

  • b Except for catalepsy (maximum effect at 8 hours).

  • c Except for catalepsy (2 hours).