Bifemelane (hydrochloride)

Bifemelane hydrochloride (MCI-2016) is a potent, selective and competitive inhibitor of monoamine oxidase A (MAO-A), with a K_i of 4.20 μM. Bifemelane hydrochloride also inhibits MAO-B noncompetitively with a K_i of 46.0 μM. Bifemelane hydrochloride has a potent antidepressant activity and can be used for the research of cognitive and emotional disturbances related to cerebrovascular disease^[1][2]. In Vitro: Bifemelane inhibits MAO-A in a dose-dependent manner, with K_is of 4.2±0.2 and 14.1±0.7 μM in human brain synaptosomes and human liver mitochondria respectively^[1].
Bifemelane inhibits MAO-B activities in a dose-dependent manner, with K_is of 46.0±3.6 and 65.2±7.0 μM in human brain synaptosomes and human liver mitochondria respectively^[1]. In Vivo: Bifemelane (20-80 mg/kg; i.p.) dose-dependently decreases exploratory activity in the open field test^[3].
Bifemelane (20-80 mg/kg; i.p.) decreases immobility time in the forced swim test, although is not clearly dosedependent and has already reached ceiling at 20 mg/kg^[3].