Reboxetine mesylate

製品コードS3199 バッチS319901

印刷

化学情報

Chemical Structure Synonyms PNU 155950E, FCE20124 mesylate Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H23NO3.CH4O3S
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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Reboxetine mesylate (PNU 155950E, FCE20124) is a norepinephrine reuptake inhibitor with Ki of 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. [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]

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
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.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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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