Moclobemide (Ro 111163)

製品コードS3212 バッチS321201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C13H17ClN2O2
分子量 268.74 CAS No. 71320-77-9
Solubility (25°C)* 体外 DMSO 53 mg/mL (197.21 mM)
Ethanol 10 mg/mL (37.21 mM)
Water 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 Moclobemide is a MAO-A (5-HT) inhibitor with IC50 of 6.1 μM.
in vitro Moclobemide orally administered 2 hours before decapitation preferentially inhibits MAO-A and PEA in rat brain with ED50 of 7.6 μmol/kg and 78 μmol/kg, respectively. Moclobemide orally administered 2 hours before decapitation preferentially inhibits MAO-A and PEA in rat liver with ED50 of 8.4 μmol/kg and 6.6 μmol/kg, respectively. Moclobemide (0.1 mM), which inhibits brain MAO-A activity by over 80%, does not affect benzylamine oxidase (rat heart) and diamine oxidase (rat small intestine) activity in vitro. [1] Moclobemide (10 mM-100 mM) includes in the culture medium during anoxia or with glutamate significantly increases in a concentration-dependent manner the amount of surviving neurons compared to controls in neuronal-astroglial cultures from rat cerebral cortex. [2]
in vivo Moclobemide (10 mg/kg p.o.) induces a significant decrease of all monoamine metabolites measured in rat brain. [1] Moclobemide, given via the drinking water (4.5 mg/kg/day), produces significant decreases in adrenal weight of rats after 5 (-23%) and 7 weeks (-16%) of treatment. Moclobemide upregulates hippocampal mineralocorticoid receptor (MR) levels in rats by 65%, 76% and 19% at 2 weeks, 5 weeks and 7 weeks of treatment, and upregulates Glucocorticoid receptor (GR) levels in this limbic brain structure by 10% at 5 weeks. Moclobemide treatment (5 weeks, 4.5 mg/kg/day) significantly attenuates stress (30 min novel environment)-induced plasma ACTH (-35%) and corticosterone (-29%) levels. [3] Moclobemide (2.5 mg/kg/day) decreases immobility and increases climbing behavior following treatment for 3 days, but increases in both swimming and climbing behaviors are measured following treatment for 14 days. Moclobemide (15 mg/kg/day) decreased immobility and increased swimming for 3 days, whereas treatment for 14 days significantly increases both active behavior (swimming and climbing). [4] Moclobemide (100 mg/kg/day) combined with triethyltin blocks the development of brain edema and the increase in the cerebral chloride content induced by triethyltin in rats. Moclobemide (100 mg/kg/day) reduces the increase in the cerebral sodium content and attenuates the neurological deficit in rats. [5]

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
20 μL aliquots of the homogenates are preincubated with the inhibitor in a total volume of 220 μL at 37 ℃ for 30 min. At the end of the preincubation period, the enzyme reaction is started by addition of 80 μL of the MAO-A substrate [14C]-5-HT (0.3 mCi/mmol, final concentration 2 × 10-4 M) or of the MAO-B substrate [14C]PEA (8 mCi/mmol; final concentration, 2 × 10-5 M) and the incubation continued for 10 mm at 37 ℃. Then, the reaction is stopped by addition of 200 μL of 2 N HCl, and the deaminated metabolites are extracted by vigorous shaking for 10 min with 5 mL of diethylether (5-HT-extraction) or n-heptane (PEA-extraction). After centrifugation (103 × g 30 sec) the water-phase is frozen in dry ice and the organic layer poured into plastic vials containing 5 mL of scintillation cocktail. Finally, the radioactivity is determined in a scintillation spectrometry.

カスタマーフィードバック

Data from [Data independently produced by , , Sci Rep, 2016, 6: 36382.]

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：

Screening Health-Promoting Compounds for Their Capacity to Induce the Activity of FOXO3 [ J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493] PubMed: 34508571
Attenuated monoamine oxidase a impairs endometrial receptivity in women with adenomyosis via downregulation of FOXO1 [ Biol Reprod, 2021, ioab182] PubMed: 34568943
Partial reversal of the effort-related motivational effects of tetrabenazine with the MAO-B inhibitor deprenyl (selegiline): Implications for treating motivational dysfunctions. [ Pharmacol Biochem Behav, 2018, 166:13-20] PubMed: 29309800
Harmine Induces Adipocyte Thermogenesis through RAC1-MEK-ERK-CHD4 Axis. [Nie T, et al. Sci Rep, 2016, 6:36382] PubMed: 27805061

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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