Molindone (hydrochloride)

Molindone hydrochloride (EN-1733A) is an orally active and brain-penetrant dopamine D2/D5 receptor antagonist. Molindone hydrochloride shows antipsychotic and antidepressant-like activities. Molindone hydrochloride suppresses spontaneous locomotion, and antagonizes apomorphine-induced emesis. Molindone hydrochloride can be used for the research of neurological disease^[1][2]. In Vitro: Molindone hydrochloride scarcely affects rat brain MAO activity in vitro, with a IC₅₀ of 9.8 × 10^-3 M^[2]. In Vivo: Molindone hydrochloride (5-60 mg/kg-bw/day; i.g.,; daily; 13 weeks) induces dose-dependent CNS effects, body weight and food consumption reductions in males, serum chemistry alterations, organ weight changes, transient prolactin surges, and mild histopathological changes in reproductive and hepatic tissues in adult Wistar Han rats^[1].
Molindone hydrochloride (5-75 mg/kg-bw/day; i.g.; daily; 8 weeks) induces dose-dependent CNS effects, body weight and food consumption reductions in males, serum chemistry alterations, organ weight changes, and delays in sexual maturation (attributed to reduced body weights), with most effects resolving during a 6-week non-dosing recovery period; no significant adverse effects on reproductive function are observed when administered orally to juvenile CD Sprague-Dawley rats^[1].
Molindone hydrochloride (p.o.) exhibits neuroleptic and antidepressant activityin rats^[2].
Molindone hydrochloride (1-2 mg/kg; p.o.) blocks Apomorphine (HY-12723)-induced emesis in dogs^[2].
Molindone hydrochloride (0.5-1 mg/kg; p.o.) reduces aggressiveness for 2-3 hours, with higher doses producing gradual, sustained docility in Macaca mulatta^[2].