tcsc2771 Reboxetine (mesylate)

Reboxetine Mesylate is a norepinephrine reuptake inhibitor use in the treatment of unipolar depression.

Target: Others

Reboxetine 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 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 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].