Nisoxetine hydrochloride

Modify Date: 2024-01-03 20:49:54

Nisoxetine hydrochloride Structure
Nisoxetine hydrochloride structure
Common Name Nisoxetine hydrochloride
CAS Number 57754-86-6 Molecular Weight 307.81500
Density 1.054g/cm3 Boiling Point 404.8ºC at 760mmHg
Molecular Formula C17H22ClNO2 Melting Point N/A
MSDS Chinese USA Flash Point 170.6ºC

 Use of Nisoxetine hydrochloride


Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.61 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gated sodium channels[1][2][3].

 Names

Name Nisoxetine hydrochloride
Synonym More Synonyms

 Nisoxetine hydrochloride Biological Activity

Description Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.61 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gated sodium channels[1][2][3].
Related Catalog
Target

Kd: 0.61 nM (NET)[1]

In Vitro Nisoxetine inhibits [3H]Nisoxetine binding to rat frontal cortical membranes with a Ki of 1.4±0.1 nM[2]. Nisoxetine inhibits [3H]Noradrenaline uptake into rat frontal cortical synaptosomes with a Ki of 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].
In Vivo 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]. Animal Model: Sprague-Dawley rats(290-340 g)[3] Dosage: 0.6, 1.2, 1.8, 2.2 µM Administration: A single intrathecal injection Result: With ED50s of 0.82 , 0.75 and 0.70 µM in motor function, proprioception, and nociception respectively.
References

[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.

[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.

[3]. Leung YM, et, al. Nisoxetine blocks sodium currents and elicits spinal anesthesia in rats. Pharmacol Rep. 2013; 65(2): 350-7.

 Chemical & Physical Properties

Density 1.054g/cm3
Boiling Point 404.8ºC at 760mmHg
Molecular Formula C17H22ClNO2
Molecular Weight 307.81500
Flash Point 170.6ºC
Exact Mass 307.13400
PSA 30.49000
LogP 4.61770

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Safety Phrases S22-S26-S36
RIDADR NONH for all modes of transport
HS Code 2930909090

 Customs

HS Code 2930909090
Summary 2930909090. other organo-sulphur compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

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 Synonyms

MFCD00153850
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