Moclobemide (Ro 111163)

製品コードS3212 バッチS321201

印刷

化学情報

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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は、MAO-A (5-HT)阻害剤で、IC50は6.1 μMです。
in vitro	Moclobemide (Ro 111163), when 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. This compound also inhibits MAO-A and PEA in rat liver with ED50 of 8.4 μmol/kg and 6.6 μmol/kg, respectively, under the same conditions. In vitro, it (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. When included in the culture medium during anoxia or with glutamate at concentrations of 10 mM-100 mM, it significantly increases in a concentration-dependent manner the amount of surviving neurons compared to controls in neuronal-astroglial cultures from rat cerebral cortex.
in vivo	Moclobemide (Ro 111163) (10 mg/kg p.o.) induces a significant decrease of all monoamine metabolites measured in rat brain. When given via the drinking water (4.5 mg/kg/day), this compound produces significant decreases in adrenal weight of rats after 5 (-23%) and 7 weeks (-16%) of treatment. It 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. Treatment with this agent (5 weeks, 4.5 mg/kg/day) significantly attenuates stress (30 min novel environment)-induced plasma ACTH (-35%) and corticosterone (-29%) levels. At a dosage of 2.5 mg/kg/day, it 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. When administered at 15 mg/kg/day, it decreased immobility and increased swimming for 3 days, whereas treatment for 14 days significantly increases both active behavior (swimming and climbing). At 100 mg/kg/day, this compound combined with triethyltin blocks the development of brain edema and the increase in the cerebral chloride content induced by triethyltin in rats. It also reduces the increase in the cerebral sodium content and attenuates the neurological deficit in rats.

プロトコル(参考用のみ)

キナーゼアッセイ	Binding assay
キナーゼアッセイ	20 μL aliquots of the homogenates are preincubated with Moclobemide (Ro 111163) 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.

参考

https://pubmed.ncbi.nlm.nih.gov/2783611/
https://pubmed.ncbi.nlm.nih.gov/17274964/
https://pubmed.ncbi.nlm.nih.gov/7845541/

https://pubmed.ncbi.nlm.nih.gov/16001105/
https://pubmed.ncbi.nlm.nih.gov/17632591/

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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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