Nisoxetine hydrochloride is a potent and selective inhibitor ofnoradrenaline transporter (NET), with aK_dof 0.76 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gatedsodium channels^[1][2][3].

Kd: 0.76 nM (NET)^[1]

Nisoxetine inhibits [³H]Nisoxetine binding to rat frontal cortical membranes with a K_iof 1.4±0.1 nM^[2].
Nisoxetine inhibits [³H]Noradrenaline uptake into rat frontal cortical synaptosomes with a K_iof 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^[3].

Nisoxetine (0.6-2.2 μM; a single intrathecal injection) displays dose-dependent effects on spinal anesthesia in rats^[3].
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^[3].

307.82

Solid

C₁₇H₂₂ClNO₂

57754-86-6

盐酸尼索西汀

Room temperature in continental US; may vary elsewhere.

DMSO : 250 mg/mL(812.16 mM;Need ultrasonic)

H₂O : 8.33 mg/mL(27.06 mM;ultrasonic and warming and heat to 60℃)

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