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Submit ReviewReboxetine mesylate
Description: Potent and selective noradrenalin uptake inhibitor; orally active
Chemical Name: (2R*)-2-[(R*)-(2-Ethoxyphenoxy)phenylmethyl]morpholine mesylate
Purity: ≥99% (HPLC)
Biological Activity for Reboxetine mesylate
Reboxetine mesylate is a potent and selective inhibitor of noradrenalin uptake (Ki values are 1.1, 129 and > 10000 nM for rat NET, SERT and DAT respectively). Displays > 1000-fold selectivity over α-adrenoceptors, 5-HT, dopamine and muscarinic ACh receptors. Orally active antidepressant.
Compound Libraries for Reboxetine mesylate
Reboxetine mesylate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Reboxetine mesylate
| M. Wt | 409.5 |
| Formula | C19H23NO3.CH3SO3H |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 98769-84-7 |
| PubChem ID | 76970698 |
| InChI Key | OEQQXKDUXVTKMH-BGLVZNNJSA-N |
| Smiles | [H][C@]2(OCCNC2)[C@@H]([C@]3=CC=CC=C3)OC1=C(OCC)C=CC=C1.[H][C@@]5(OCCNC5)[C@H]([C@]6=CC=CC=C6)OC4=C(OCC)C=CC=C4.CS(=O)(O)=O.CS(=O)(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Reboxetine mesylate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 20.48 | 50 | |
| DMSO | 20.48 | 50 |
Preparing Stock Solutions for Reboxetine mesylate
The following data is based on the product molecular weight 409.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.88 mL | 24.42 mL | 48.84 mL |
| 2.5 mM | 0.98 mL | 4.88 mL | 9.77 mL |
| 5 mM | 0.49 mL | 2.44 mL | 4.88 mL |
| 25 mM | 0.1 mL | 0.49 mL | 0.98 mL |
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Product Datasheets for Reboxetine mesylate
References for Reboxetine mesylate
References are publications that support the biological activity of the product.
Sacchetti et al (1999) Studies on the acute and chronic effects of reboxetine on extracellular noradrenaline and other monoamines in the rat brain. Br.J.Pharmacol. 128 1332 PMID: 10578149
Wong et al (2000) Reboxetine: a pharmacologically potent, selective, and specific NE reuptake inhibitor. Biol.Psychiatry. 47 818 PMID: 10812041
Millan et al (2001) S33005, a novel ligand at both serotonin and NE transporters: I Receptor binding, electrophysiological, and neurochemical profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine. J.Pharmacol.Exp.Ther. 298 565 PMID: 11454918
Owen and Whitton (2003) Reboxetine modulates NE efflux in the frontal cortex of the freely moving rat: the involvement of α2 and 5-HT1A receptors. Neurosci.Lett. 348 171 PMID: 12932821
If you know of a relevant reference for Reboxetine mesylate, please let us know.
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Keywords: Reboxetine mesylate, Reboxetine mesylate supplier, Potent, selective, noradrenalin, noradrenaline, reuptake, inhibitors, inhibits, orally, active, Transporters, NET, Adrenergic, adrenaline, adrenalin, Monoamine, Neurotransmitter, 1982, Tocris Bioscience
9 Citations for Reboxetine mesylate
Citations are publications that use Tocris products. Selected citations for Reboxetine mesylate include:
Zhu et al (2018) Cortical bone is an extraneuronal site of norepinephrine uptake in adult mice. Bone Rep 9 188 PMID: 30581894
Hughes et al (2013) Endogenous analgesic action of the pontospinal noradrenergic system spatially restricts and temporally delays the progression of neuropathic pain following tibial nerve injury. Int J Neuropsychopharmacol 154 1680 PMID: 23707289
Kreiner et al (2019) Stimulation of noradrenergic transmission by reboxetine is beneficial for a mouse model of progressive parkinsonism. Sci Rep 9 5262 PMID: 30918302
Stuart et al (2013) A translational rodent assay of affective biases in depression and antidepressant therapy. Neuropsychopharmacology 38 1625 PMID: 23503126
Kobayashi et al (2010) Inhibition of G-protein-activated inwardly rectifying K+ channels by the selective NE reuptake inhibitors atomox. and reboxetine. Neuropsychopharmacology 35 1560 PMID: 20393461
Munari et al (2015) Brain Histamine Is Crucial for Selective Serotonin Reuptake Inhibitors' Behavioral and Neurochemical Effects. Neurochem Int 18 pyv045 PMID: 25899065
Suto et al (2014) Peripheral nerve injury and gabapentin, but not their combination, impair attentional behavior via direct effects on noradrenergic signaling in the brain. Pain 155 1935 PMID: 24837843
Hutchinson et al (2012) Differential regulation of MeCP2 phosphorylation in the CNS by DA and serotonin. Pain 37 321 PMID: 21956448
Ferreira et al (2012) Presynaptic CB(1) cannabinoid receptors control frontocortical serotonin and glutamate release--species differences. Theriogenology 61 219 PMID: 22609378
Do you know of a great paper that uses Reboxetine mesylate from Tocris? Please let us know.
Reviews for Reboxetine mesylate
Average Rating: 5 (Based on 1 Review.)
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Reboxetine mesysate effect in mice. Brain MCP-1..
By
Anonymous on 01/10/2018
Assay Type: In Vivo
Species: Mouse
Reboxetine mesylate was dissolved in saline serum and 20 mg/kg (100 μL) were administered intraperitoneally to mice. After 24h, brain samples were taken and MCP-1 synthesis was analyzed by immunohistochemistry. This way, we confirmed that reboxetine treatment induces MCP-1 synthesis in cortical astrocytes.
In the figure, MCP-1 is labeled in red and GFAP in green.
