盐酸尼索西汀

生物活性靶点体外研究体内研究盐酸尼索西汀试剂级价格

盐酸尼索西汀

CAS号:57754-86-6
英文名:NISOXETINE HYDROCHLORIDE
中文名:盐酸尼索西汀
CBNumber:CB9267088
分子式:C17H22ClNO2
分子量:307.82
MOL File:57754-86-6.mol

盐酸尼索西汀化学性质

储存条件 :Sealed in dry,Room Temperature
溶解度 :H₂O: 20 mg/mL
形态 :solid
颜色 :white
水溶解性 :Soluble to 100 mM in water

安全信息

安全说明 :22-26-36
WGK Germany :3
RTECS号 :NI2922170

盐酸尼索西汀性质、用途与生产工艺

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.