Nisoxetine (hydrochloride)

Nisoxetine is a norepinephrine transporter (NET) inhibitor (K_i = 5.1 nM).¹ It is selective for NET over the dopamine transporter (DAT) and the serotonin (5-HT) transporter (SERT; K_is = 477 and 383 nM, respectively). Nisoxetine inhibits norepinephrine uptake and inhibits amphetamine-induced increases in norepinephrine release in mouse brain (EC₅₀s = 2.97 and 0.08 µM, respectively).² It reduces increases in locomotor activity induced by d-N-ethylamphetamine, methylphenidate, and cocaine, but not morphine, in mice when administered at a dose of 32 mg/kg.³ Nisoxetine (0.5 mg/kg i.v.) also reduces cataplexy in narcoleptic dogs.⁴

WARNING This product is not for human or veterinary use.

1. Torres, G.E., Gainetdinov, R.R., and Caron, M.G. Plasma membrane monoamine transporters: Structure, regulation and function. Nat. Rev. Neurosci. 4(1), 13-25 (2003).

2. Tyler, T.D., and Tessel, R.E. Amphetamine’s locomotor-stimulant and noreprinephrine-releasing effects: Evidence for selective antagonism by nisoxetine. Psychopharmacology (Berl) 64(3), 291-296 (1979).

3. Tyler, T.D., and Tessel, R.E. Norepinephrine uptake inhibitors as biochemically and behaviorally selective antagonists of the locomotor stimulation induced by indirectly acting sympathomimetic aminetic amines in mice. Psychopharmacology (Berl) 69(1), 27-34 (1980).

4. Foutz, A.S., Delashaw, J.B., Jr., Guilleminault, C., et al. Monoaminergic mechanisms and experimental cataplexy. Ann. Neurol. 10(4), 369-376 (1981).