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Bifemelane is an antidepressant and cerebral activator that was primarily used in Japan for the treatment of depressive symptoms in patients with cerebral infarction and for dementia. It has also been investigated for use in glaucoma. Bifemelane acts as a non-selective monoamine oxidase inhibitor (MAOI), functioning as a reversible inhibitor of monoamine oxidase A (RIMA) and an irreversible inhibitor of monoamine oxidase B. Additionally, it exhibits weak norepinephrine reuptake inhibition. The drug demonstrates nootropic, neuroprotective, and antidepressant-like effects in animal models and appears to enhance the cholinergic system in the brain. Its mechanism may also involve modulation of muscarinic acetylcholine receptors and intracellular calcium signaling pathways[1][3][5][6][8]. Bifemelane was discontinued from the Japanese market in 1998 due to lack of effectiveness[1].
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