Nomifensine (maleate)

Nomifensine ((±)-Nomifensine) maleate is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine maleate inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC₅₀ values of 6.6 nM, 48 nM and 830 nM, and K_i values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine maleate has antidepressant and analgesic effects. Nomifensine maleate is used in neurodegenerative diseases, compound addiction, and pain research^{[1][2][3][4][5][6][7]}. In Vivo:Nomifensine (10 mg/kg; i.p.; 12 days) maleate reduces response latency and increases activity in WKY rats, with no significant effect on Wistar rats^[3].
Nomifensine (5 mg/kg/day; s.c. using minipumps; 2-14 days) maleate potently and significantly inhibits dopamine neuronal firing in the ventral tegmental area of SD rats after 2 days, with recovery to normal after 14-day treatment due to D₂ autoreceptor desensitization^[4].
Nomifensine (0.625-5 mg/kg; s.c.; 30 min before testing) maleate produces analgesia (only in the formaldehyde test) and abolishs the nociceptive behavior induced by 2% formaldehyde in rats^[6].
Nomifensine (20 mg/kg; i.p.; once a day; 6 consecutive days) maleate can suppress the neurotoxicity of MPTP (HY-15608) in C57 black mice, inhibiting the long-term depletion of neostriatal DA concentration induced by MPTP^[7].