Reboxetine mesylate

SKU: orb1300308

Description

Reboxetine mesylate

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 98769-84-7
• MW: 409.5
• Purity: 99.87%
• Formula: C₁₉H₂₃NO₃·CH₄O₃S
• SMILES: CS(O)(=O)=O.[H][C@@]1(CNCCO1)[C@H](Oc1ccccc1OCC)c1ccccc1
• Target: Adrenergic Receptor,Norepinephrine
• Solubility: H2O:20.5 mg/mL (50.06 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (12.21 mM);DMSO:250 mg/mL (610.5 mM)

Bioactivity

• Target IC50:
  Norepinephrine reuptake:8.2 nM(Ki)
• 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. 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. 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. 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. 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Adrenergic Receptor, AdrenergicReceptor, activity, antidepressant, Beta Receptor, disorder, depression, panic, inhibit, norepinephrine reuptake, Inhibitor, Edronax, FCE20124, FCE-20124, FCE20124 mesylate, FCE20124 Mesylate, FCE-20124 Mesylate, FCE 20124, FCE 20124 Mesylate, Reboxetine Mesylate, Reboxetine, Reboxetine mesylate, PNU155950E, PNU155950E mesylate, PNU155950E Mesylate, PNU 155950E

Compound Identifiers

PubChem CID

127150