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| 10mg |
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| Targets |
Nisoxetine hydrochloride targets the norepinephrine transporter (NET). It is a selective NET inhibitor with a Kd of 0.76 nM. It has little or no affinity for a range of other neurotransmitter receptors. By inhibiting NET, it increases the synaptic concentration of norepinephrine, enhancing noradrenergic neurotransmission.
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| ln Vitro |
Nisoxetine hydrochloride suppresses the binding of [3H]nisoxetine, which has a Ki of 1.4±0.1 nM, to the pyramidal frontal cortex membrane[2]. [3H]normethoxide concentration into pyramidal frontal synaptosomes is inhibited by nisoxetine hydrochloride, Ki. At membrane potentials of -70 and -100 mV, nisoxetine hydrochloride inhibits Na+ current with an IC50 of 1.6 and 28.6 μM, respectively [3].
In vitro, nisoxetine hydrochloride is a potent NET inhibitor with a Kd of 0.76 nM. It selectively inhibits norepinephrine uptake. This potent and selective inhibition makes it a valuable tool for studying the noradrenergic system. |
| ln Vivo |
Nisoxetine (2.2 µM; single intrathecal injection) hydrochloride demonstrated 100%, 100%, and 100% arrest of motor function and proprioception, with durations of action of 61, 96, and 236 minutes, respectively [3]. Nisoxetine (3)
Specific in vivo activity data for nisoxetine hydrochloride are not extensively detailed. It has been studied for its antidepressant and local anesthetic properties. In vivo, it would be expected to increase extracellular norepinephrine levels in the brain. |
| Enzyme Assay |
NET inhibition is measured using radioligand binding assays with membranes from cells expressing the transporter. Nisoxetine hydrochloride is incubated at varying concentrations, and Kd values are calculated.
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| Cell Assay |
Cellular activity of nisoxetine hydrochloride is evaluated in cells expressing the norepinephrine transporter. Norepinephrine uptake is measured using radiolabeled norepinephrine.
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| Animal Protocol |
Animal/Disease Models: SD (SD (Sprague-Dawley)) rat (290-340 g) [3]
Doses: 0.6, 1.2, ,10, 30 mg/kg, ip) Refeeding response to hydrochloride inhibitory factor (intervention standard food )[4]. 1.8, 2.2 µM Route of Administration: Single intrathecal injection Experimental Results: ED50 for blocking motor function, proprioception and nociception were 0.82, 0.75 and 0.70 µM respectively. In vivo efficacy of nisoxetine hydrochloride has been evaluated in animal models of depression and ADHD. Behavioral and neurochemical endpoints are assessed. |
| ADME/Pharmacokinetics |
Nisoxetine hydrochloride has a molecular formula of C17H22ClNO2 and a molecular weight of 307.82. Its chemical name is 3-(2-methoxyphenoxy)-N-methyl-3-phenylpropan-1-amine hydrochloride. It is a crystalline solid.
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| Toxicity/Toxicokinetics |
Toxicological data for nisoxetine hydrochloride are limited in the cited literature. The compound is intended for research use only. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
Nisoxetine hydrochloride is a selective norepinephrine reuptake inhibitor (SNRI). It is a research tool for studying the noradrenergic system and has potential therapeutic applications for ADHD and MDD. It is also a local anesthetic that can block voltage-gated sodium channels.
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| Molecular Formula |
C17H22CLNO2
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|---|---|
| Molecular Weight |
307.818
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| Exact Mass |
307.134
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| Elemental Analysis |
C, 66.33; H, 7.20; Cl, 11.52; N, 4.55; O, 10.40
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| CAS # |
57754-86-6
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| Related CAS # |
Nisoxetine;53179-07-0
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| PubChem CID |
134453
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| Appearance |
White to off-white solid powder
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| Density |
1.054g/cm3
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| Boiling Point |
404.8ºC at 760mmHg
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| Flash Point |
170.6ºC
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| LogP |
4.617
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
21
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| Complexity |
253
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=[N+](C1=CC=CC=C1SC2=CCO2)[O-].[H]Cl
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| InChi Key |
LCEURBZEQJZUPV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H21NO2.ClH/c1-18-13-12-15(14-8-4-3-5-9-14)20-17-11-7-6-10-16(17)19-2;/h3-11,15,18H,12-13H2,1-2H3;1H
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| Chemical Name |
3-(2-methoxyphenoxy)-N-methyl-3-phenylpropan-1-amine hydrochloride
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| Synonyms |
Lilly 94939; Nisoxetine hydrochloride; Nisoxetine HCl; NSC 298819
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~812.16 mM)
H2O : ~8.33 mg/mL (~27.06 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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