产品
编 号:F381352
分子式:C17H21NO2
分子量:271.35
产品类型
结构图
CAS No: 53179-07-0
联系客服
产品详情
生物活性:
Nisoxetine is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.
体内研究:
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. Nisoxetine (3,10, 30 mg/kg, i.p.) inhibits refeeding response (intake of standard chow) in rats. Animal Model:Sprague-Dawley rats(290-340 g)
Dosage:0.6, 1.2, 1.8, 2.2 μM
Administration:A single intrathecal injection
Result:Showed ED50s of 0.82, 0.75 and 0.70 μM in blocking motor function, proprioception, and nociception respectively.
体外研究:
Nisoxetine 抑制 [3H]Nisoxetine 与大鼠额叶皮层膜的结合,Ki 为 1.4±0.1 nM。Nisoxetine 抑制[3H]去甲肾上腺素摄取到大鼠额叶皮质突触体中,Ki 为 2.1±0.3 nM。Nisoxetine 抑制 Na+ 电流,膜电位为 -70 和 -100 mV 时的 IC50 分别为 1.6 和 28.6 μM。