盐酸尼索西汀

中文名称:

盐酸尼索西汀

中文同义词:

盐酸尼索西汀;3-(2-甲氧基苯氧基)-N-甲基-3-苯基丙-1-胺盐酸盐

英文名称:

NISOXETINE HYDROCHLORIDE

英文同义词:

LY-94,939;(+/-)-GAMMA-(2-METHOXYPHENOXY)-N-METHYL-BENZENEPROPANAMINE HYDROCHLORIDE;NISOXETINE HYDROCHLORIDE;NISOXETINE HYDROCHLORIDE (LY-94,939) NOR PINEPHRINE UPTAKE;(+/-)-g-(2-Methoxyphenoxy)-N-methylbenzenepropanaminehydrochloride;NisoxetineHCl;Nsc298819;(±)-γ-(2-methoxyphenoxy)-n-methyl-benzenepropanamine hydrochloride

CAS号:

57754-86-6

分子式:

C17H22ClNO2

分子量:

307.82

EINECS号:

相关类别:

其它;Adrenoceptor

Mol文件:

57754-86-6.mol

储存条件 

Sealed in dry,Room Temperature

溶解度 

H2O: 20 mg/mL

形态

solid

颜色

white

生物活性

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。

靶点

Kd: 0.76 nM (NET)

体外研究

Nisoxetine inhibits [ 3 H]Nisoxetine binding to rat frontal cortical membranes with a K i of 1.4±0.1 nM. Nisoxetine inhibits [ 3 H]Noradrenaline uptake into rat frontal cortical synaptosomes with a K i of 2.1±0.3 nM. Nisoxetine inhibits Na + currents with IC 50 s of 1.6 and 28.6 µM at the membrane potential of -70 and -100 mV, respectively.

体内研究

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. Animal Model: Sprague-Dawley rats(290-340 g) Dosage: 0.6, 1.2, 1.8, 2.2 µM Administration: A single intrathecal injection Result: With ED 50 s of 0.82 , 0.75 and 0.70 µM in motor function, proprioception, and nociception respectively.

Animal Model:

Sprague-Dawley rats(290-340 g)

Dosage:

0.6, 1.2, 1.8, 2.2 µM

Administration:

A single intrathecal injection

Result:

With ED 50 s of 0.82 , 0.75 and 0.70 µM in motor function, proprioception, and nociception respectively.

安全说明 

22-26-36

WGK Germany 

3

RTECS号

NI2922170