Flucindole

Flucindole is an orally active dopamine receptor inhibitor (IC₅₀ = 240 nM) that also exhibits affinity for S₂ receptors. Flucindole inhibits amphetamine-induced stereotyped behaviors in rats, and increases the levels of dopamine metabolites in the striatum of rats and mice. Flucindole can be used in the research of psychosis^[1][2]. In Vitro:Flucindole binds to dopamine, α₁, S₁, and S₂ receptors in rat brain membrane preparations, with the highest affinity for dopamine receptors (IC₅₀ = 240 nM) and no appreciable binding to α₂, β, muscarinic, or tryptamine receptors^[2]. In Vivo:Flucindole (1.4-50 mg/kg; p.o., i.p.; single dose) exhibits antipsychotic activity in rats with an ED₅₀ of 1.4 mg/kg p.o., and lacks antidepressant-like activity in mice at doses up to 50 mg/kg i.p^[1].
Flucindole (0.1-40 mg/kg; i.p.; single dose) dose-dependently elevates mouse striatal DA metabolites DOPAC, HVA, and 3-MT, with a significant decrease in DA observed only at the highest tested dose of 40.0 mg/kg^[2].
Flucindole (0.1-5 mg/kg; i.p.; single dose) dose-dependently elevates rat striatal DOPAC and HVA levels, with a significant decrease in DA observed only at the 5.0 mg/kg dose^[2].