CAS 57754-86-6|Nisoxetine hydrochloride
| Common Name | Nisoxetine hydrochloride | ||
|---|---|---|---|
| CAS Number | 57754-86-6 | Molecular Weight | 307.81500 |
| Density | 1.054g/cm3 | Boiling Point | 404.8ºC at 760mmHg |
| Molecular Formula | C17H22ClNO2 | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | 170.6ºC |
Names
| Name | Nisoxetine hydrochloride |
|---|---|
| Synonym | More Synonyms |
Nisoxetine hydrochloride BiologicalActivity
| 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]. |
|---|---|
| Related Catalog | Signaling Pathways >>Membrane Transporter/Ion Channel >>Sodium ChannelResearch Areas >>Neurological DiseaseSignaling Pathways >>Membrane Transporter/Ion Channel >>Monoamine Transporter |
| Target | Kd: 0.61 nM (NET)[1] |
| 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]. |
| 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. |
| 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. |
Chemical & Physical Properties
| Density | 1.054g/cm3 |
|---|---|
| Boiling Point | 404.8ºC at 760mmHg |
| Molecular Formula | C17H22ClNO2 |
| Molecular Weight | 307.81500 |
| Flash Point | 170.6ºC |
| Exact Mass | 307.13400 |
| PSA | 30.49000 |
| LogP | 4.61770 |
| InChIKey | LCEURBZEQJZUPV-UHFFFAOYSA-N |
| SMILES | CNCCC(Oc1ccccc1OC)c1ccccc1.Cl |
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| Safety Phrases | S22-S26-S36 |
| RIDADR | NONH for all modes of transport |
| HS Code | 2930909090 |
Customs
| HS Code | 2930909090 |
|---|---|
| Summary | 2930909090. other organo-sulphur compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0% |
Articles33
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Synonyms
| MFCD00153850 |
