[CAS NO. 53179-07-0] Nisoxetine
PRODUCTS SPECIFICATIONS [53179-07-0]
DESCRIPTION [53179-07-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 271.35 |
| Molecular Formula | C17H21NO2 |
| SMILES | CNCCC(OC1=CC=CC=C1OC)C2=CC=CC=C2 |
1 Publications Citing Use of MCE
Summary
IC50 & Target
Kd: 0.76 nM (NET) [1]
In Vitro
Nisoxetine inhibits [
3
H]Nisoxetine binding to rat frontal cortical membranes with a K
i
of 1.4±0.1 nM
[2]
.
Nisoxetine inhibits [
3
H]Noradrenaline uptake into rat frontal cortical synaptosomes with a K
i
of 2.1±0.3 nM
[2]
.
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
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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: | Showed ED 50 s of 0.82, 0.75 and 0.70 µM in blocking motor function, proprioception, and nociception respectively. |
Appearance
Viscous liquid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Pure form | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 921.32 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.6853 mL | 18.4264 mL | 36.8528 mL |
| 5 mM | 0.7371 mL | 3.6853 mL | 7.3706 mL |
| 10 mM | 0.3685 mL | 1.8426 mL | 3.6853 mL |
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.
- [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.