Nisoxetine

Modify Date: 2024-01-10 19:15:24

Nisoxetine Structure
Nisoxetine structure
Common Name Nisoxetine
CAS Number 53179-07-0 Molecular Weight 271.35400
Density 1.054g/cm3 Boiling Point 404.8ºC at 760mmHg
Molecular Formula C17H21NO2 Melting Point N/A
MSDS N/A Flash Point 170.6ºC

 Use of Nisoxetine


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].

 Names

Name 3-(2-Methoxyphenoxy)-N-methyl-3-phenyl-1-propanamine
Synonym More Synonyms

 Nisoxetine Biological Activity

Description 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].
Related Catalog
Target

Kd: 0.76 nM (NET)[1]

In Vitro 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: Sprague-Dawley rats(290-340 g)[3] Dosage: 0.6, 1.2, 1.8, 2.2 µM Administration: A single intrathecal injection Result: Showed ED50s of 0.82, 0.75 and 0.70 µM in blocking 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.  

[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.  

 Chemical & Physical Properties

Density 1.054g/cm3
Boiling Point 404.8ºC at 760mmHg
Molecular Formula C17H21NO2
Molecular Weight 271.35400
Flash Point 170.6ºC
Exact Mass 271.15700
PSA 30.49000
LogP 3.81570
Index of Refraction 1.547

 Safety Information

HS Code 2922299090

 Synthetic Route

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Nisoxetine Structure

Nisoxetine

CAS#:53179-07-0

Literature: Andersen, Jacob; Stuhr-Hansen, Nicolai; Zachariassen, Linda Gronborg; Koldso, Heidi; Schiott, Birgit; Stromgaard, Kristian; Kristensen, Anders S. Molecular Pharmacology, 2014 , vol. 85, # 5 p. 703 - 714

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Nisoxetine Structure

Nisoxetine

CAS#:53179-07-0

Literature: Andersen, Jacob; Stuhr-Hansen, Nicolai; Zachariassen, Linda Gronborg; Koldso, Heidi; Schiott, Birgit; Stromgaard, Kristian; Kristensen, Anders S. Molecular Pharmacology, 2014 , vol. 85, # 5 p. 703 - 714

 Customs

HS Code 2922299090
Summary 2922299090. other amino-naphthols and other amino-phenols, other than those containing more than one kind of oxygen function, their ethers and esters; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

 Synonyms

3,5-dicarbomethoxy-1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)pyridine
Adalat CC
4-(2'-nitro-phenyl)-2,6-dimethyl-3,5-dimethoxycarbonyl-1,4-dihydro-pyridine
Procardia XL
1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridine-dicarboxylic acid dimethyl ester
Procardia
Adalat
[125I]-Iodonisoxetine
(R,S)-nisoxetine
[3H]-Nifedipine
Fenihidin
N-methyl-3-(2-methoxyphenoxy)-3-phenylpropylamine
Cordipin
[3H]-Nisoxetine
Fenihidine
N-methyl-3-(2-methoxyphenoxy)-3-phenyl-1-propylamine
Corinfar
4-(2-nitrophenyl)-3,5-dimethoxycarbonyl-2,6-dimethyl-1,4-dihydropyridine
nifedipine
4-(2'-nitrophenyl)-2,6-dimethyl-3,5-dicarbmethoxy-1,4-dihydropyridine
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