盐酸尼索西汀

盐酸尼索西汀用途

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 0.61 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。

盐酸尼索西汀名称

[ CAS 号 ]:
57754-86-6

[ 中文名 ]:
盐酸尼索西汀

[ 英文名 ]:
Nisoxetine hydrochloride

[英文别名 ]:

MFCD00153850

盐酸尼索西汀生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钠通道

研究领域 >> 神经疾病

信号通路 >> 跨膜转运 >> 单胺转运蛋白

[ 靶点 ]

Kd: 0.61 nM (NET)[1]

[体外研究]

尼索西汀抑制[3H]尼索西汀与大鼠额叶皮质膜结合,Ki为1.4±0.1nm[2]。尼索西汀抑制[3H]去甲肾上腺素进入大鼠额叶皮质突触体的摄取,Ki为2.1±0.3nm[2]。尼索西汀在膜电位分别为-70和-100 mV时,用1.6和28.6µM的IC50s抑制Na+电流[3]。

[体内研究]

尼索西汀(0.6-2.2µM；鞘内单次注射)对大鼠脊髓麻醉具有剂量依赖性作用[3]。尼索西汀(2.2µM；单次鞘内注射)在运动功能、本体感觉方面显示100%、100%和100%的阻滞,作用持续时间分别约61、96和236 min[3]。动物模型：Sprague-Dawley大鼠(290-340g)[3]剂量：0.6,1.2,1.8,2.2µM给药：单次鞘内注射结果：运动功能、本体感觉、痛觉ED50s分别为0.82、0.75和0.70µM。

[参考文献]

[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.

盐酸尼索西汀物理化学性质

[ 密度 ]:
1.054g/cm3

[ 沸点 ]:
404.8ºC at 760mmHg

[ 分子式 ]:
C₁₇H₂₂ClNO₂

[ 分子量 ]:
307.81500

[ 闪点 ]:
170.6ºC

[ 精确质量 ]:
307.13400

[ PSA ]:
30.49000

[ LogP ]:
4.61770

[ 外观性状 ]:
白色固体

[ 储存条件 ]:
室温

盐酸尼索西汀MSDS

详细MSDS(安全技术说明书)

盐酸尼索西汀安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
S22-S26-S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2930909090

盐酸尼索西汀海关

[ 海关编码 ]: 2930909090

[ 中文概述 ]:
2930909090. 其他有机硫化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

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

盐酸尼索西汀文献

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)

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