Reboxetine mesylate (Synonyms: FCE 20124, PNU 155950E)

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 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].

References:
[1]. Wong, E.H., et al., Reboxetine: a pharmacologically potent, selective, and specific norepinephrine reuptake inhibitor. Biol Psychiatry, 2000. 47(9): p. 818-29.
[2]. Versiani, M., et al., Reboxetine, a unique selective NRI, prevents relapse and recurrence in long-term treatment of major depressive disorder. J Clin Psychiatry, 1999. 60(6): p. 400-6.
[3]. Page, M.E. and I. Lucki, Effects of acute and chronic reboxetine treatment on stress-induced monoamine efflux in the rat frontal cortex. Neuropsychopharmacology, 2002. 27(2): p. 237-47.