Nomifensine maleate

Nomifensine is an inhibitor of norepinephrine (NE) and dopamine (DA) reuptake.¹ It inhibits uptake of NE, DA, and serotonin (5-HT) in rat brain synaptosomes with IC₅₀ values of 6.6, 48, and 830 nM, respectively. It is selective for DA, NE, and 5-HT uptake inhibition over binding to dopamine D₂, α₁- adrenergic-, 5-HT₂, and muscarinic receptors (IC₅₀s = 43,000, 1,200, 3,800, and >13,000 nM, respectively, in rat brain membranes). Nomifensine is selective for inhibition of NE over DA uptake in vivo with minimal inhibitory doses of 28 and less than 57 ?mol/kg, respectively. It decreases the time Wistar Kyoto, but not Sprague-Dawley, rats spend immobile in the forced swim test but also increases locomotor activity in the open field test in Wistar Kyoto and Sprague-Dawley rats when administered at a chronic dose of 10 mg/kg.²

1.Hyttel, J., and Larsen, J.J.Neurochemical profile of Lu 19-005, a potent inhibitor of uptake of dopamine, noradrenaline, and serotoninJ. Neurochem.44(5)1615-1622(1985) 2.Tejani-Butt, S., Kluczynski, J., and Paré, W.P.Strain-dependent modification of behavior following antidepressant treatmentProg. Neuropsychopharmacol. Biol. Psychiatry27(1)7-14(2003)