Befloxatone

Befloxatone (MD-370503) is an orally active, selective and reversible inhibitor of Monoamine Oxidase A (MAO-A) (IC₅₀=4 nM). Befloxatone increases the tissue level of monoamine, striatal dopamine and cortical norepinephrine. Befloxatone has antidepressant potential^[1]. In Vitro:Befloxatone (100 nM; 0-100 min) reversibly reduces MAO-A activity in rat brain homogenates, while completely lost 60 min later^[1]. In Vivo:Befloxatone (0.75 mg/kg; i.p.; single dose) increases tissue levels of monoamines and decreases levels of their deaminating metabolites in rats^[1].
Befloxatone (1 mg/kg; i.p.; single dose) induces elevated levels of dopamine and corticonorepinephrine in the extracellular striatum of rats, but not elevates levels of corticoserotonin^[1].
Befloxatone (0.03-0.3 mg/kg; p.o.; single dose) effectively inhibits the firing rate of serotonergic neurons and partially reduces the firing of norepinephric neurons, but had no effect on the firing of dopaminergic neurons in rats^[1].
Befloxatone (1.5 mg/kg; p.o.; single dose) does not enhance the pressor effect of the central active dose of oral tyramine and has a broad safety profile in rats^[1].