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首页 / 抑制剂/激动剂 / 神经信号通路 / MAO / Moclobemide

吗氯贝胺 /Moclobemide {[allProObj[0].p_purity_real_show]}

货号：A566201 同义名： Ro111163

Moclobemide is a reversible MAO-A inhibitor.

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Moclobemide 化学结构 CAS号：71320-77-9
Moclobemide 化学结构
CAS号：71320-77-9
Moclobemide 3D分子结构
CAS号：71320-77-9
Moclobemide 化学结构 CAS号：71320-77-9
Moclobemide 3D分子结构 CAS号：71320-77-9
规格 价格 会员价 库存 数量
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Moclobemide 纯度/质量文件 产品仅供科研

货号：A566201 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]
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• BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]
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• PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]
更多 >
产品名称 MAO ↓ MAO-A ↓ MAO-B ↓ 其他靶点 纯度
Sennoside A ++

MAO, IC50: 17 μM

 		98%+
Glycyrrhizic acid ++++

MAO, IC50: 0.16 μM

 		80% HPLC
Rasagiline ++++

MAO-A, IC50: 412 nM

 		++++

MAO-B, IC50: 4.43 nM

 		99+%
Isatin ++

MAO, IC50: 15 μM

 		+

MAO-A, IC50: 58 μM

 		++

MAO-B, IC50: 14 μM

 		98%
Paeonol +

MAO-A, IC50: 54.6 μM

 		+

MAO-B, IC50: 42.5 μM

 		98%
Tranylcypromine hydrochloride +++

MAO-A, IC50: 11.5 μM

 		+++

MAO-B, IC50: 7 μM

 		97%
Moclobemide +++

MAO-A (5-HT), IC50: 6.1 μM

 		99%+
Pargyline HCl ++

MAO-A, Ki: 13 μM

 		+++

MAO-B, Ki: 0.5 μM

 		99%+
Safinamide ++++

MAO-B, IC50: 98 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Moclobemide 生物活性

靶点

  • MAO-A

    MAO-A (5-HT), IC50:6.1 μM
描述 Moclobemide is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A[3]. Moclobemide is a reversible inhibitor of monoamine-oxidase-A (RIMA) and has been extensively evaluated in the treatment of a wide spectrum of depressive disorders. The effective therapeutic dose range for moclobemide in most acute phase trials was 300 to 600 mg, divided in 2 to 3 doses. Cases of refractory depression might improve with a combination of moclobemide with other antidepressants, such as clomipramine or a SSRI (selective serotonin reuptake inhibitors)[4]. In humans, moclobemide is rapidly absorbed after a single oral administration and maximum concentration in plasma is reached within an hour. In the case of moclobemide, increase in the level of serotonin is the most pronounced. Moclobemide administration also leads to increased monoamine receptor stimulation, reversal of reserpine induced behavioral effects, selective depression of REM sleep, down regulation of beta-adrenoceptors and increases in plasma prolactin and growth hormone levels. It reduces scopolamine-induced performance decrement and alcohol induced performance deficit which suggest a neuroprotective role[5]. Long-term treatment with moclobemide causes gynecomastia in rats, which is reversible[6]. Morever, moclobemide overdose in combination with a serotonergic agent (even in normal therapeutic doses) can cause severe serotonin toxicity[7].

Moclobemide 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02269540 Major Depressive Disorder Early Phase 1 Recruiting July 2018 Canada, Ontario ... 展开 >> Research Imaging Centre, Centre for Addiction and Mental Health Recruiting Toronto, Ontario, Canada, M5T 1R8 Principal Investigator: Jeffrey H Meyer, MD, PhD 收起 <<
NCT01544309 Hypercholesterolemia With Conc... 展开 >>omitant Type 2 Diabetes 收起 << Not Applicable Completed - -
NCT00068224 - Completed - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<

Moclobemide 参考文献

[1]Verleye M, Steinschneider R, et al. Moclobemide attenuates anoxia and glutamate-induced neuronal damage in vitro independently of interaction with glutamate receptor subtypes. Brain Res. 2007 Mar 23;1138:30-8.

[2]Da Prada M, Kettler R, et al. Neurochemical profile of moclobemide, a short-acting and reversible inhibitor of monoamine oxidase type A. J Pharmacol Exp Ther. 1989 Jan;248(1):400-14.

[3]Can NÖ, Osmaniye D, Levent S, Sağlık BN, İnci B, Ilgın S, Özkay Y, Kaplancıklı ZA. Synthesis of New Hydrazone Derivatives for MAO Enzymes Inhibitory Activity. Molecules. 2017 Aug 20;22(8):1381

[4]Bonnet U. Moclobemide: therapeutic use and clinical studies. CNS Drug Rev. 2003 Spring;9(1):97-140

[5]Nair NP, Ahmed SK, Kin NM. Biochemistry and pharmacology of reversible inhibitors of MAO-A agents: focus on moclobemide. J Psychiatry Neurosci. 1993 Nov;18(5):214-25

[6]Ma XC, Wang Y, Liu JH, Tu ZH. Moclobemide-induced gynecomastia in rats. Acta Pharmacol Sin. 2000 Oct;21(10):893-6

[7]Isbister GK, Hackett LP, Dawson AH, Whyte IM, Smith AJ. Moclobemide poisoning: toxicokinetics and occurrence of serotonin toxicity. Br J Clin Pharmacol. 2003 Oct;56(4):441-50

Moclobemide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.72mL

0.74mL

0.37mL

18.61mL

3.72mL

1.86mL

37.21mL

7.44mL

3.72mL

Moclobemide 技术信息

CAS号71320-77-9
分子式C13H17ClN2O2
分子量 268.739
别名 Ro111163
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature
溶解度

DMSO: 105 mg/mL(390.71 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Moclobemide | 71320-77-9 | Ro111163 | Ro 111163 | Ro-111163 | Neuronal Signaling | Monoamine Oxidase | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Moclobemide 纯度/质量文件 | Moclobemide 亚型比较 | Moclobemide 生物活性 | Moclobemide 临床数据 | Moclobemide 参考文献 | Moclobemide 实验方案 | Moclobemide 技术信息

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