[CAS NO. 57754-86-6] Nisoxetine hydrochloride
PRODUCTS SPECIFICATIONS [57754-86-6]
DESCRIPTION [57754-86-6]
Overview
| MDL | MFCD00153850 |
|---|---|
| Molecular Weight | 307.82 |
| Molecular Formula | C17H22ClNO2 |
| SMILES | CNCCC(OC1=CC=CC=C1OC)C2=CC=CC=C2.[H]Cl |
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 (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]
.
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: | With ED 50 s of 0.82 , 0.75 and 0.70 µM in motor function, proprioception, and nociception respectively. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 812.16 mM ; Need ultrasonic)
H 2 O : 8.33 mg/mL ( 27.06 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.2487 mL | 16.2433 mL | 32.4865 mL |
| 5 mM | 0.6497 mL | 3.2487 mL | 6.4973 mL |
| 10 mM | 0.3249 mL | 1.6243 mL | 3.2487 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.
Synonyms