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Synonyms | PNU 155950E, FCE20124 mesylate | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C19H23NO3.CH4O3S |
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分子量 | 409.5 | CAS No. | 98769-84-7 | |
Solubility (25°C)* | 体外 | DMSO | 82 mg/mL (200.24 mM) | |
Water | 82 mg/mL (200.24 mM) | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Reboxetine mesylate (PNU 155950E, FCE20124) is a norepinephrine reuptake inhibitor with Ki of 8.2 nM. |
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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] |
キナーゼアッセイ | Binding assay | |
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Rat brain tissue is homogenized in 9 volumes of 0.32 M sucrose using a rotating pestle on setting 50 (10 up and down strokes). The homogenate is centrifuged at 1×103 g for 10 min at 4 ℃, the supernatant is collected and centrifuged at 2×105 g for 20 min at 4 ℃. The resulting pellet is resuspended to a protein concentration of approximately 2 mg/mL. The pellet is resuspended with Kreb’s-Hepes buffer (20 mM Hepes, 4.16 mM NaHCO3, 0.44 mM KH2PO4, 0.63 mM NaH2PO4, 127 mM NaCl, 5.36 mM KCl, 1.26 mM CaCl2, and 0.98 mM MgCl2) pH 7.0, so that 30 μg–150 μg protein are added per test tube. All assays are carried out in 0.5 mL final volume. Appropriate radioligands and assay conditions are employed in determining affinity of Reboxetine at the 39 different receptors and 6 enzyme targets. |
The Meningioma Enhancer Landscape Delineates Novel Subgroups and Drives Druggable Dependencies [ Cancer Discov, 2020, CD-20-0160] | PubMed: 32703768 |
Highly Sensitive Label-Free Detection of Small Molecules with an Optofluidic Microbubble Resonator [ Micromachines (Basel), 2018, 9(6)E274] | PubMed: 30424207 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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