Monoamine oxidases (MAOs) are a family of enzymes that catalyze the oxidation of monoamines. Additionally, they including MAO-A and MAO-B. MAOs plays important role in the inactivation of neurotransmitter. Therefore, their dysfunction is related with many psychiatric and neurological disorders. MAO-A can catabolize monoamines ingested in food, breaking down serotonin, melatonin, norepinephrine and epinephrine. According to many researches, MAO inhibitors are highly effective anti-depressants.

Brofaromine (CGP 11305A) is a reversible and selective MAO-A inhibitor and 5-hydroxytryptamine (5-HT) reuptake inhibitor, primarily being researched in depression and anxiety disorders. Compared with standard MAO inhibitors, Brofaromine exhibits less possible side effects such as cardiovascular complications, liver toxicity or hyperthermia, and producing less severe anticholinergic side effects.

In cell experiments, Brofaromine inhibits MAO-A activity in cortical cells with an IC₅₀ of 0.19 μM. Besides, it exhibits no toxicity even at high concentrations (up to 200 μM). Following the evidence in vivo experiments, Brofaromine (10 and 30 mg/kg; s.c., single dosage) can significantly increase the 5-HT production to about 200% of basal values after administration for 4 hours in rat brain. Besides, Brofaromine (10 mg/kg; i.p., single dosage) does not affect the duration of immobility in the mouse tail suspension test.

In conclusion, Brofaromine is a potent, reversible and selective MAO-A inhibitor which can be used for researching depression and anxiety disorders.

Reference:

[1] Boland A, et al. Br J Pharmacol. 2002;135(3):713-720.

[2] Prakhie IV, et al. Int J Neuropsychopharmacol. 1998;1(1):35-40.