53179-07-0
53179-07-0 structure
- Name: Nisoxetine
- Chemical Name: 3-(2-Methoxyphenoxy)-N-methyl-3-phenyl-1-propanamine
- CAS Number: 53179-07-0
- Molecular Formula: C17H21NO2
- Molecular Weight: 271.35400
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel Monoamine Transporter
- Create Date: 2018-05-13 08:00:00
- Modify Date: 2024-01-10 19:15:24
-
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].
| Name | 3-(2-Methoxyphenoxy)-N-methyl-3-phenyl-1-propanamine |
|---|---|
| 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 |
| 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 |
| 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 |
| HS Code | 2922299090 |
|---|
|
~%
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 |
|
~%
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 |
| 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% |