Nisoxetine hydrochloride

Names

[ Name ]:
Nisoxetine hydrochloride

[Synonym ]:
MFCD00153850

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]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> Monoamine Transporter

[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

MSDS

Click to get detail MSDS

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%

Articles

Serotonergic signalling suppresses ataxin 3 aggregation and neurotoxicity in animal models of Machado-Joseph disease.

Brain 138 , 3221-37, (2015)

Polyglutamine diseases are a class of dominantly inherited neurodegenerative disorders for which there is no effective treatment. Here we provide evidence that activation of serotonergic signalling is...

The pro-inflammatory cytokine TNF-α regulates the activity and expression of the serotonin transporter (SERT) in astrocytes.

Neurochem. Res. 38(4) , 694-704, (2013)

Pro-inflammatory cytokines have been implicated in the precipitation of depression and related disorders, and the antidepressant sensitive serotonin transporter (SERT) may be a major target for immune...

Plasma membrane monoamine transporters: structure, regulation and function.

Nat. Rev. Neurosci. 4 , 13-25, (2003)

Related Compounds

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