| Description: |
Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.61 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gated sodium channels[1][2][3]. |
| Target: |
Kd: 0.61 nM (NET)[1] |
| 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. |
| In Vitro: |
Nisoxetine inhibits [3H]Nisoxetine binding to rat frontal cortical membranes with a Ki of 1.4±0.1 nM[2]. Nisoxetine inhibits [3H]Noradrenaline uptake into rat frontal cortical synaptosomes with a Ki of 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]. |
| References: |
[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. |
