Bifemelane

2023-12-20: Drugs

• PGL cart: TAK 250mg, ABT spray 5 bottles, bifemelane, and 1 bottle of methylene blue

Bifemelane #

Antidepressant and ‘cerebral activator’ (which is used for cerebrovascular diseases; seems to be a Japanese class of drugs)

• Competitive (i.e. reversible) MAO-A inhibitor and non-competitive/irreversible inhibitor of MAO-B, and weak NRI.
  • The fact the MAO-A inhibition is reversible means tyramine isn’t a problem.
  • Norepinephrine→α1→serotonin release. NRI + MAOI prevents the tyramine reaction to serotonin release Reboxetine prevents the tranylcypromine-induced increase in tyramine levels in rat heart
• M1 enhancement (prevents loss of mRNA levels and receptor binding) and ChAT enhancement. Effects of Bifemelane on Muscarinic Receptors and Choline Acetyltransferase in the Brains of Aged Rats Following Chronic Cerebral Hypoperfusion Induced by Permanent Occlusion of Bilateral Carotid Arteries
  • Chronic administration of bifemelane or aniracetam also enhanced ChAT activity in the cortex, hippocampus and striatum. In particular, administration of bifemelane resulted in a significant increase in Vmax values of ChAT in all three brain regions, while no significant change in Km values for ChAT was observed
  • JC claims this ChAT enhancement (after 2 weeks, where a cholinergic depression started to kick in) undid his Piracetam tolerance back to honeymoon period level. Restoring choline reserves in the liver is just not enough. Thus, massive synergy and they were made for each other.
• Attenuates decrease in NMDAR density with aging
• Free radical scavenging by bifemelane hydrochloride and its major metabolites
• Bifemelane Hydrochloride Protects Against Cytotoxicity of Hydrogen Peroxide on Cultured Rat Neuroblastoma Cell Line

Dose #

• 75 mg twice daily or so. Ideally 3x50mg apparently. Which would be a good $2.25/day from PGLchem (10g = bit over a 2-month supply of 150mg/day for $150… brutal.)
• Brotherman: Bifemelane is one of my favorite noots, going to order again soon. Used back in spring 2022 and it amplified life, made me feel energized, potentiated my noot stack.
• MattNZ: Likes it more than 4Cl-modafinil. Better task initiation.
• 3-4x60mg https://discord.com/channels/962009752035008593/973028978212368384/1236994649860866150
• JC: insane morning wood and diamond hard erections. Together with piracetam it’s the best thing ever for verbal fluency. Too impulsive and horny though.
• Best cycled I think and not just used acutely. For the ChAT upregulation and the like