| Bioactivity | 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[1][2][3]. | ||||||||||||
| Target | Kd: 0.76 nM (NET) | ||||||||||||
| Invitro | Nisoxetine 抑制 [3H]Nisoxetine 与大鼠额叶皮层膜的结合，Ki 为 1.4±0.1 nM[2]。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[2]。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[3]。 | ||||||||||||
| In Vivo | 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]. Nisoxetine (3,10, 30 mg/kg, i.p.) inhibits refeeding response (intake of standard chow) in rats[4]. Animal Model: | ||||||||||||
| Name | Nisoxetine | ||||||||||||
| CAS | 53179-07-0 | ||||||||||||
| Formula | C17H21NO2 | ||||||||||||
| Molar Mass | 271.35 | ||||||||||||
| Appearance | Viscous liquid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Béïque JC, et, al. Affinities of venlafaxine and various reuptake inhibitors for the serotonin and norepinephrine transporters. Eur J Pharmacol. 1998 May 15; 349(1): 129-32. [2]. Cheetham SC, et, al. [3H]nisoxetine-a radioligand for noradrenaline reuptake sites: correlation with inhibition of [3H]noradrenaline uptake and effect of DSP-4 lesioning and antidepressant treatments. Neuropharmacology. 1996 Jan; 35(1): 63-70. [3]. Leung YM, et, al. Nisoxetine blocks sodium currents and elicits spinal anesthesia in rats. Pharmacol Rep. 2013; 65(2): 350-7. [4]. Bello NT, et al. High-fat diet-induced alterations in the feeding suppression of low-dose nisoxetine, a selective norepinephrine reuptake inhibitor. J Obes. 2013;2013:457047. |