盐酸尼索西汀

Kd: 0.76 nM (NET)

Nisoxetine inhibits [ ³ H]Nisoxetine binding to rat frontal cortical membranes with a K _i of 1.4±0.1 nM.
Nisoxetine inhibits [ ³ H]Noradrenaline uptake into rat frontal cortical synaptosomes with a K _i of 2.1±0.3 nM.
Nisoxetine inhibits Na ⁺ currents with IC ₅₀ s of 1.6 and 28.6 µM at the membrane potential of -70 and -100 mV, respectively.

Nisoxetine (0.6-2.2 µM; a single intrathecal injection) displays dose-dependent effects on spinal anesthesia in rats.
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.