Nisoxetine hydrochloride

• CAT Number: I010357
• CAS Number: 57754-86-6
• Molecular Formula: C17H22ClNO2
• Molecular Weight: 307.82
• Purity: ≥95%
• Synonyms: 3-(2-methoxyphenoxy)-N-methyl-3-phenylpropan-1-amine;hydrochloride
• InChI: InChI=1S/C17H21NO2.ClH/c1-18-13-12-15(14-8-4-3-5-9-14)20-17-11-7-6-10-16(17)19-2;/h3-11,15,18H,12-13H2,1-2H3;1H
• InChIKey: LCEURBZEQJZUPV-UHFFFAOYSA-N
• SMILES: CNCCC(C1=CC=CC=C1)OC2=CC=CC=C2OC.Cl

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].
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].
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].

Reference

[1]. Béïque JC, et, al. Affinities of venlafaxine and various reuptake inhibitors for the serotonin and norepinephrine transporters. Eur J Pharmacol. 1998 May 15; 349(1): 129-32.
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[2]. Cheetham SC, et, al. [3H]nisoxetine-a radioligand for noradrenaline reuptake sites: correlation with inhibition of [3H]noradrenaline uptake and effect of DSP-4 lesioning and antidepressant treatments. Neuropharmacology. 1996 Jan; 35(1): 63-70.
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[3]. Leung YM, et, al. Nisoxetine blocks sodium currents and elicits spinal anesthesia in rats. Pharmacol Rep. 2013; 65(2): 350-7.
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[4]. Bello NT, et al. High-fat diet-induced alterations in the feeding suppression of low-dose nisoxetine, a selective norepinephrine reuptake inhibitor. J Obes. 2013;2013:457047.
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