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Reboxetine mesylate Norepinephrine inhibitor

Cat.No.S3199

Reboxetine (PNU 155950E) is a norepinephrine reuptake inhibitor with Ki of 8.2 nM.
Reboxetine mesylate Norepinephrine inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 409.5

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Quality Control

Batch: Purity: 99.97%
99.97

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (200.24 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 82 mg/mL

Ethanol : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 409.5 Formula

C19H23NO3.CH4O3S

 Storage (From the date of receipt)
CAS No. 98769-84-7 Download SDF Storage of Stock Solutions

Synonyms PNU 155950E, FCE20124 mesylate Smiles CCOC1=CC=CC=C1OC(C2CNCCO2)C3=CC=CC=C3.CS(=O)(=O)O

Mechanism of Action

Targets/IC50/Ki
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.
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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/12093597/
  • [5] https://pubmed.ncbi.nlm.nih.gov/12388649/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00886886 Completed
Mood Disorder|Substance-related Disorders|Amphetamine-related Disorders
University Hospital Basel Switzerland
 April 2009 Phase 1
NCT00141128 Completed
Urinary Incontinence Stress
Pfizer
 December 2005 Phase 2

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