Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Reboxetine mesylate (FCE20124 mesylate) is a norepinephrine reuptake inhibitor (Ki: 8.2 nM).
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5 mg | 在庫あり | ¥ 11,500 | |||
10 mg | 在庫あり | ¥ 17,000 | |||
25 mg | 在庫あり | ¥ 38,000 | |||
50 mg | 在庫あり | ¥ 70,500 | |||
100 mg | 在庫あり | ¥ 112,000 | |||
500 mg | 在庫あり | ¥ 243,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 11,500 |
説明 | Reboxetine mesylate (FCE20124 mesylate) is a norepinephrine reuptake inhibitor (Ki: 8.2 nM). |
ターゲット&IC50 | 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. [1] |
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. [1] 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. [2] 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. [3] 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. [4] 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. [5] |
別名 | FCE20124 mesylate, Edronax, PNU155950E mesylate, PNU 155950E |
分子量 | 409.5 |
分子式 | C19H23NO3·CH4O3S |
CAS No. | 98769-84-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 20.5 mg/mL (50 mM)
DMSO: 20.5 mg/mL (50 mM)
You can also refer to dose conversion for different animals. 詳細
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Reboxetine mesylate 98769-84-7 GPCR/G Protein Neuroscience Norepinephrine Adrenergic Receptor disorder FCE20124 activity FCE-20124 Mesylate depression antidepressant FCE20124 mesylate panic Beta Receptor FCE-20124 FCE 20124 Mesylate FCE 20124 inhibit Edronax PNU155950E Reboxetine PNU155950E mesylate PNU155950E Mesylate FCE20124 Mesylate Reboxetine Mesylate PNU 155950E Inhibitor inhibitor