中文名:Reboxetine mesylate
英文名:Reboxetine mesylate
英文别名:PNU 155950E, FCE20124 mesylate;Morpholine, 2-[(R)-(2-ethoxyphenoxy)phenylmethyl]-, (2R)-, methanesulfonate (1:1)
纯度:10mM in DMSO
货号:R409242
包装:1ml
Cas号:98769-84-7
存储温度:-80℃储存
产品介绍:
Information
Reboxetine (PNU 155950E) is anorepinephrinereuptake inhibitor withKiof 8.2 nM.
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.
Cell Data
cell lines:HDMECs
Concentrations:
Incubation Time:
Powder Purity:≥99%
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关键字: PNU 155950E, FCE20124 mesylate;Morpholine, 2-[(R)-(2-ethoxyphenoxy)phenylmethyl]-, (2R)-, methanesulfonate (1:1)
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