Reboxetine mesylate

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生物活性

Description

Reboxetine Mesylate is a norepinephrine reuptake inhibitor use in the treatment of unipolar depression.Target: OthersReboxetine is a drug of the norepinephrine reuptake inhibitor class. Reboxetine dose-dependently and potently inhibits locus coeruleus neuronal firing in rats with ED50 of 191 ??g/kg. Reboxetine inhibition of the locus coeruleus neurons is reversible by the ??2 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 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 [2]. 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 [3].

Clinical Trial

NCT00372190

Radboud University

Pelvic Organ Prolapse

August 2006

NCT00572702

Charles University, Czech Republic-Ministry of Health, Czech Republic

Pelvic Organ Prolapse

January 2007

NCT00833001

Ethicon, Inc.

Cystocele-Rectocele-Enterocele

April 2008

Phase 2-Phase 3

NCT03070873

Nanjing Medical University

Pelvic Organ Prolapse

January 1, 2010

NCT02231099

Radboud University

Pelvic Organ Prolapse-Cystocele-Rectocele-Uterine Prolapse

January 2011

NCT00566917

Karolinska Institutet-The regional agreement on medical training and clinical research (ALF) between Stockholm county council and Karolinska Institutet.-The Swedish Society of Medicine-Investigators meetings supported by Gynecare Scandinavia.

Vaginal Prolapse

December 2007

Phase 4

NCT00679276

William Beaumont Hospitals

Vaginal Prolapse

May 2008

NCT00402844

Karolinska Institutet-Karolinska University Hospital

Pelvic Organ Prolapse

August 2006

Phase 2-Phase 3