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.
IC50&Target
Kd: 0.76 nM (NET)
体外研究
Nisoxetine inhibits [H]Nisoxetine binding to rat frontal cortical membranes with a Ki of 1.4±0.1 nM.
Nisoxetine inhibits [H]Noradrenaline uptake into rat frontal cortical synaptosomes with a Ki of 2.1±0.3 nM.
Nisoxetine inhibits Na currents with IC50s 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 ED50s of 0.82 , 0.75 and 0.70 µM in motor function, proprioception, and nociception respectively.
分子式
C9H7NO3S.HCl
分子量
307.82
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:
H2O : 8.33 mg/mL (27.06 mM; ultrasonic and warming and heat to 60°C)