Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Reboxetine (also known as PNU 155950E; Trade name: Edronax)is a selective norepinephrine reuptake inhibitor with Ki of 8.2 nM and antidepressant activity. Reboxetine completely and dose-dependently blocks [3H]-dopamine uptake to the human norepinephrine transporters (hNET) in Madin-Darby canine kidney (MDCK) cells, with a Ki value of 11 nM. With an ED50 of 191 μg/kg, reboxetine potently and dose-dependently inhibits the firing of locus coeruleus neurons in rats. The α2 antagonist piperoxan (1.5 mg/kg, IV) can reverse the effects of reboxetine-induced inhibition of locus coeruleus neurons. The mice's blepharospasm and hypothermia caused by reserpine are reversed by reboxetine in a dose-dependent manner.
Targets |
norepinephrine reuptake ( Ki = 8.2 nM )
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ln Vitro |
In vitro activity: Reboxetine completely and dose-dependently blocks [3H]-dopamine uptake to the human norepinephrine transporters (hNET) in Madin-Darby canine kidney (MDCK) cells, with a Ki value of 11 nM. [1]
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ln Vivo |
Reboxetine potently and dose-dependently inhibits the firing of locus coeruleus neurons in rats with ED50 of 191 μg/kg. Piperoxan (1.5 mg/kg, IV), an α2 antagonist, can reverse the effects of reboxetine-induced inhibition of locus coeruleus neurons. The mice's blepharospasm and hypothermia caused by reserpine are reversed by reboxetine in a dose-dependent manner. Additionally, it is discovered that reboxetine counteracts the dose-dependent hypothermia in mice induced by clonidine. In rats, reboxetine (ED50 = 10 mg/kg and 3 mg/kg (p.o.)) reverses blepharospasm and hypothermia caused by reserpine.[1] In patients with DSM-III-R panic disorder, reboxetine significantly lowers the mean number of panic attacks and phobic symptoms. Additionally, reboxetine improves scores on the Sheehan Disability Scale, Hopkins Symptom Checklist-90, and Hamilton Rating Scale for Depression.[2] In patients with recurrent DSM-III-R major depression, reboxetine is linked to a significantly lower relapse rate than placebo (22% vs. 56%) and a higher cumulative probability of a maintained response during long-term treatment. After an episode ends, reboxetine effectively prevents depression symptoms from returning.[3] Reboxetine (0.3 mg/kg–20 mg/kg) administered systemically to rats dose-dependently raises extracellular norepinephrine in the frontal cortex, but has no effect on extracellular serotonin. The rat frontal cortex's extracellular dopamine is also increased by reboxetine (20 mg/kg). When Reboxetine is administered chronically for 14 days, the rat frontal cortex exhibits increased basal concentrations of extracellular norepinephrine and dopamine as well as a greater net increase in these substances—but not serotonin.[4] Reboxetine dose-dependently reduces the self-administration of nicotine by approximately 60%. Reboxetine (5.6 mg/kg) is administered repeatedly over the course of 14 sessions, which reduces nicotine self-administration and sucrose-maintained responding.[5]
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Cell Assay |
Cell Line: SH-SY5Y cells
Concentration: 0.1 μM, 1 μM, 5 μM Incubation Time: 24 hours Result: Prevented the Dexamethasone-induced decreases in cell viability and proliferation rate. |
Animal Protocol |
Harlan-bred, male CF-1 mice (18-20 g), depression models
3 mg/kg, 30 mg/kg Intraperitoneal injection |
References |
Molecular Formula |
C20H27NO6S
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Molecular Weight |
409.5
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Exact Mass |
409.16
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Elemental Analysis |
C, 58.66; H, 6.65; N, 3.42; O, 23.44; S, 7.83
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CAS # |
98769-84-7
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Related CAS # |
Reboxetine; 71620-89-8; (R,R)-Reboxetine mesylate; 105017-39-8
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Appearance |
Solid powder
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SMILES |
CCOC1=CC=CC=C1O[C@@H]([C@H]2CNCCO2)C3=CC=CC=C3.CS(=O)(=O)O
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InChi Key |
CGTZMJIMMUNLQD-STYNFMPRSA-N
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InChi Code |
InChI=1S/C19H23NO3.CH4O3S/c1-2-21-16-10-6-7-11-17(16)23-19(15-8-4-3-5-9-15)18-14-20-12-13-22-18;1-5(2,3)4/h3-11,18-20H,2,12-14H2,1H3;1H3,(H,2,3,4)/t18-,19-;/m1./s1
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Chemical Name |
(2R)-2-[(R)-(2-ethoxyphenoxy)-phenylmethyl]morpholine;methanesulfonic acid
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Synonyms |
PNU 155950E; PNU155950E; PNU-155950E; FCE-20124 mesylate; PNU-155950E mesylate; FCE 20124 mesylate; PNU 155950E mesylate; FCE20124 mesylate; PNU155950E mesylate; Reboxetine mesilate; Reboxetine; Edronax; Reboxetine mesylate; Vestra (TN); AC1L2RIX; AC1Q6WCV; DSSTox_CID_25690; DSSTox_RID_81062; DSSTox_GSID_45690.
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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: 82~125 mg/mL (200.2~305.3 mM)
Water: < 1 mg/mL Ethanol: ~82 mg/mL (~200.2 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 110 mg/mL (268.62 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4420 mL | 12.2100 mL | 24.4200 mL | |
5 mM | 0.4884 mL | 2.4420 mL | 4.8840 mL | |
10 mM | 0.2442 mL | 1.2210 mL | 2.4420 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.
The effects of the norepinephrine selective reuptake inhibitor, reboxetine on extracellular NE and 5-HT in the rat frontal cortex were measured using in vivo microdialysis with HPLC-EC. Neuropsychopharmacology . 2002 Aug;27(2):237-47. td> |
Panel A shows the effect of acute administration (first arrow) of reboxetine (10 mg/kg, ♦, n = 7; or 20 mg/kg, ▪, n = 10) on extracellular NE. Neuropsychopharmacology . 2002 Aug;27(2):237-47. td> |
Chronic administration of reboxetine via subcutaneous osmotic minipumps (10 mg/kg/day, 14 days, ♦, n = 10) elevated basal extracellular NE levels approximately by fourfold over chronic saline treated controls (□, n = 8). Neuropsychopharmacology . 2002 Aug;27(2):237-47. td> |