Nisoxetine is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine is an antidepressant and local anesthetic, it can block voltage-gated sodium channels[2].IC50 & Target:Kd: 0.76 nM (NET)In Vitro:Nisoxetine inhibits [3H]Nisoxetine binding to rat frontal cortical membranes with a Ki of 1.4±0.1 nM[2].
Nisoxetine inhibits [3H]Noradrenaline uptake into rat frontal cortical synaptosomes with a Ki of 2.1±0.3 nM[2].
Nisoxetine inhibits Na+ currents with IC50s of 1.6 and 28.6 μM at the membrane potential of -70 and -100 mV, respectively.In Vivo:Nisoxetine (2.2 μM; a single intrathecal injection) shows 100, 100, and 100% of blockades in motor function, proprioception, and with duration of action of about 61, 96, and 236 min, respectively.
Nisoxetine (3,10, 30 mg/kg, i.p.) inhibits refeeding response (intake of standard chow) in rats.