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Reboxetine mesylate

Catalog No. T6963   CAS 98769-84-7
Synonyms: FCE20124 mesylate, Edronax, PNU155950E mesylate, PNU 155950E

Reboxetine mesylate (FCE20124 mesylate) is a norepinephrine reuptake inhibitor (Ki: 8.2 nM).

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Reboxetine mesylate Chemical Structure
Reboxetine mesylate, CAS 98769-84-7
Pack Size Availability Price/USD Quantity
5 mg In stock $ 50.00
10 mg In stock $ 73.00
25 mg In stock $ 165.00
50 mg In stock $ 306.00
100 mg In stock $ 488.00
500 mg In stock $ 1,060.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.72%
Purity: 99.64%
Purity: 99.24%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Reboxetine mesylate (FCE20124 mesylate) is a norepinephrine reuptake inhibitor (Ki: 8.2 nM).
Targets&IC50 norepinephrine reuptake:8.2 nM(Ki)
In vitro Reboxetine dose-dependently and completely inhibits [3H]-dopamine uptake to the human norepinephrine transporters (hNET) with Ki value of 11 nM in Madin–Darby canine kidney (MDCK) cells. [1]
In vivo Reboxetine dose-dependently and potently inhibits locus coeruleus neuronal firing in rats with ED50 of 191 μg/kg. Reboxetine inhibition of the locus coeruleus neurons is reversible by the α2 antagonist piperoxan (1.5 mg/kg, IV). Reboxetine dose-dependently reverses reserpine-induced blepharospasm and hypothermia in the mouse. Reboxetine is also found to antagonize clonidine-induced hypothermia dose-dependently in mice. Reboxetine reverses reserpine-induced blepharospasm and hypothermia in rats with ED50 of 10 mg/kg and 3 mg/kg (p.o.), respectively. [1] Reboxetine results in a significant reduction in the mean number of panic attacks and phobic symptoms in patients with DSM-III-R panic disorder. Reboxetine also results in improvement in Hamilton Rating Scale for Depression, Hopkins Symptom Checklist-90, and Sheehan Disability Scale scores. [2] Reboxetine is associated with a markedly lower relapse rate than placebo (22% vs. 56%) and a greater cumulative probability of a maintained response during long-term treatment in patients with recurrent DSM-III-R major depression. Reboxetine effectively prevents recurrence of depressive symptoms following episode resolution. [3] Acute systemic administration of Reboxetine (0.3 mg/kg-20 mg/kg) dose-dependently increases extracellular norepinephrine in the rat frontal cortex while having no effect on extracellular serotonin. Reboxetine (20 mg/kg) also increases extracellular dopamine in the rat frontal cortex. Chronic administration of Reboxetine for 14 days results in elevated basal concentrations of extracellular norepinephrine and dopamine and a greater net increase of extracellular norepinephrine and dopamine, but not serotonin in the rat frontal cortex. [4] Reboxetine dose dependently decreases nicotine self-administration by ~60%. Repeated administration of Reboxetine (5.6 mg/kg) decreases nicotine self-administration and sucrose-maintained responding across the 14 sessions. [5]
Synonyms FCE20124 mesylate, Edronax, PNU155950E mesylate, PNU 155950E
Molecular Weight 409.5
Formula C19H23NO3·CH4O3S
CAS No. 98769-84-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 20.5 mg/mL (50 mM)

DMSO: 20.5 mg/mL (50 mM)

TargetMolReferences and Literature

1. Wong EH, et al. Biol Psychiatry, 2000, 47(9), 818-829. 2. Versiani M, et al. J Clin Psychiatry, 2002, 63(1), 31-37. 3. Versiani M, et al. J Clin Psychiatry, 1999, 60(6), 400-406. 4. Page ME, et al. Neuropsychopharmacology, 2002, 27(2), 237-247. 5. Rauhut AS, et al. J Pharmacol Exp Ther, 2002, 303(2), 664-672.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Neurodegenerative Disease Compound Library Adrenergic Receptor-Targeted Compound Library Approved Drug Library GPCR Compound Library Neurotransmitter Receptor Compound Library Neuronal Signaling Compound Library Drug Repurposing Compound Library

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Keywords

Reboxetine mesylate 98769-84-7 GPCR/G Protein Neuroscience Adrenergic Receptor Norepinephrine disorder FCE20124 activity FCE-20124 Mesylate depression antidepressant FCE20124 mesylate panic Beta Receptor FCE-20124 FCE 20124 Mesylate FCE 20124 inhibit Edronax PNU155950E Reboxetine PNU155950E mesylate PNU155950E Mesylate FCE20124 Mesylate Reboxetine Mesylate PNU 155950E Inhibitor inhibitor

 

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