Nisoxetine hydrochloride

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

57754-86-6

盐酸尼索西汀

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，K_d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。

生物活性

Nisoxetine hydrochloride is a potent and selective inhibitor ofnoradrenaline transporter (NET), with aK_dof 0.76 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gatedsodium channels^[1]^[2]^[3].

IC₅₀& Target

Kd: 0.76 nM (NET)^[1]

体外研究
(In Vitro)

Nisoxetine inhibits [³H]Nisoxetine binding to rat frontal cortical membranes with a K_iof 1.4±0.1 nM^[2].
Nisoxetine inhibits [³H]Noradrenaline uptake into rat frontal cortical synaptosomes with a K_iof 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].

体内研究
(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.

分子量

307.82

性状

Solid

Formula

C₁₇H₂₂ClNO₂

CAS 号

57754-86-6

中文名称

盐酸尼索西汀

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

DMSO : 250 mg/mL(812.16 mM;Need ultrasonic)

H₂O : 8.33 mg/mL(27.06 mM;ultrasonic and warming and heat to 60℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.2487 mL	16.2433 mL	32.4865 mL
5 mM	0.6497 mL	3.2487 mL	6.4973 mL
10 mM	0.3249 mL	1.6243 mL	3.2487 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。