1. Membrane Transporter/Ion Channel
  2. Monoamine Transporter
    Sodium Channel
  3. Nisoxetine hydrochloride

Nisoxetine hydrochloride 

目录号: HY-B1704A 纯度: >98.0%
产品使用指南

Nisoxetine hydrochloride 是一种有效的和选择性的去甲肾上腺素转运蛋白 (NET) 的抑制剂,Kd 值为 0.76 nM。Nisoxetine hydrochloride 是一种抗抑郁药和局部麻药,它可以阻断电压门控性钠通道。

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Nisoxetine hydrochloride Chemical Structure

Nisoxetine hydrochloride Chemical Structure

CAS No. : 57754-86-6

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Description

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 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.
Molecular Weight

307.82

Formula

C₁₇H₂₂ClNO₂

CAS No.

57754-86-6

中文名称

盐酸尼索西汀

SMILES

CNCCC(OC1=CC=CC=C1OC)C2=CC=CC=C2.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >98.0%

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Keywords:

NisoxetineMonoamine TransporterSodium ChannelNa channelsNa+ channelsnoradrenalinetransporterNETantidepressantlocalanestheticsodiumchannelsuptakedepressionInhibitorinhibitorinhibit

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Nisoxetine hydrochloride
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