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.

Product information

CAS Number: 57754-86-6

Molecular Weight: 307.82

Formula: C17H22ClNO2

Chemical Name: [3-(2-methoxyphenoxy)-3-phenylpropyl](methyl)amine hydrochloride

Smiles: Cl.COC1=CC=CC=C1OC(CCNC)C1C=CC=CC=1

InChiKey: LCEURBZEQJZUPV-UHFFFAOYSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Nisoxetine inhibits [3H]Nisoxetine binding to rat frontal cortical membranes with a Ki of 1.4±0.1 nM. Nisoxetine inhibits [3H]Noradrenaline uptake into rat frontal cortical synaptosomes with a Ki of 2.1±0.3 nM. 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 (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.

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