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Moclobemide

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Chemical Structure| 71320-77-9 同义名 : Ro111163
CAS号 : 71320-77-9
货号 : A566201
分子式 : C13H17ClN2O2
纯度 : 99%+
分子量 : 268.739
MDL号 : MFCD00865388
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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].
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 <<
实验方案
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
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