Nisoxetine (hydrochloride)


CAS No. : 57754-86-6

57754-86-6
Price and Availability of CAS No. : 57754-86-6
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Cat. No. : HY-B1704A
M.Wt: 307.82
Formula: C17H22ClNO2
Purity: >98 %
Solubility: H2O : 8.33 mg/mL (ultrasonic;warming;heat to 60°C);DMSO : 250 mg/mL (ultrasonic)
Introduction of 57754-86-6 :

Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gated sodium channels[1][2][3]. IC50 & Target:Kd: 0.76 nM (NET)[1] In Vitro:Nisoxetine hydrochloride inhibits [3H]Nisoxetine binding to rat frontal cortical membranes with a Ki of 1.4±0.1 nM[2].
Nisoxetine hydrochloride inhibits [3H]Noradrenaline uptake into rat frontal cortical synaptosomes with a Ki of 2.1±0.3 nM[2].
Nisoxetine hydrochloride inhibits Na+ currents with IC50s of 1.6 and 28.6 µM at the membrane potential of -70 and -100 mV, respectively[3]. In Vivo:Nisoxetine (2.2 µM; a single intrathecal injection) hydrochloride 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].
Nisoxetine (3,10, 30 mg/kg, i.p.) hydrochloride inhibits refeeding response (intake of standard chow) in rats[4].

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