Phenelzine
(Synonyms: 苯乙肼,NSC 170957) 目录号 : GC31033
Phenelzine是一种单胺氧化酶（MAO）抑制剂。
Cas No.:51-71-8
Sample solution is provided at 25 µL, 10mM.
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Phenelzine is a monoamine oxidase (MAO) inhibitor [1]. Phenelzine irreversibly inhibits monoamine oxidase A and B in the brain, reducing the breakdown of neurotransmitters such as norepinephrine, dopamine, and serotonin, thereby increasing their levels and improving mood [2-3]. Phenelzine is primarily used to treat refractory depression [4].
In PC12 cells, Phenelzine (1-50μM; 24h) reduced the condensation and fragmentation of nuclei caused by 1-methyl-4-phenylpyridinium (MPP+) [5]. In 3T3-F442A and 3T3-L1 cells, reductions in cellular triglycerides and sterol regulatory element binding protein-1c (SREBP-1c) were detected at lower Phenelzine (1-10μM; 8d) concentrations [6]. In Molt-4 cells, Phenelzine (5-25μM; 24h) can upregulate the levels of histone H3K4 monomethylation, H3K4 dimethylation and histone H3 acetylation, upregulate the expression of p21 and p15 proteins, and downregulate the expression of DNMT1, ultimately inhibiting the proliferation of Molt-4 cells and inducing cell apoptosis [7].
In experimental autoimmune encephalomyelitis (EAE) mice model, Phenelzine (15mg/kg; ip; 28d) can delay the onset of disease, alleviate the chronic stage of EAE mice, and significantly improve non-motor symptoms such as exploratory behavior and emotional disorders [8]. In experimental autoimmune encephalomyelitis mice model, Phenelzine (15mg/kg; ip; 14d) elevates the levels of GABA, dopamine and biogenic amines in the central nervous system [9].
References:
[1]. Robinson D S, Nies A, Ravaris C L, et al. The monoamine oxidase inhibitor, phenelzine, in the treatment of depressive-anxiety states: a controlled clinical trial[J]. Archives of General Psychiatry, 1973, 29(3): 407-413.
[2]. Matveychuk D, MacKenzie E M, Kumpula D, et al. Overview of the neuroprotective effects of the MAO-inhibiting antidepressant phenelzine[J]. Cellular and Molecular Neurobiology, 2022, 42(1): 225-242.
[3]. MacKenzie E M, Grant S L, Baker G B, et al. Phenelzine causes an increase in brain ornithine that is prevented by prior monoamine oxidase inhibition[J]. Neurochemical Research, 2008, 33(3): 430-436.
[4]. Van den Eynde V, Abdelmoemin W R, Abraham M M, et al. The prescriber’s guide to classic MAO inhibitors (phenelzine, tranylcypromine, isocarboxazid) for treatment-resistant depression[J]. CNS spectrums, 2023, 28(4): 427-440.
[5]. Lee C S, Han E S, Lee W B. Antioxidant effect of phenelzine on MPP+-induced cell viability loss in differentiated PC12 cells[J]. Neurochemical research, 2003, 28(12): 1833-1841.
[6]. Chiche F, Le Guillou M, Chetrite G, et al. Antidepressant phenelzine alters differentiation of cultured human and mouse preadipocytes[J]. Molecular Pharmacology, 2009, 75(5): 1052-1061.
[7]. Qiu Y, Huang Y, Ma X. Effect of phenelzine on the proliferation, apoptosis and histone methylation and acetylation of Molt-4 cells[J]. Zhonghua xue ye xue za zhi= Zhonghua Xueyexue Zazhi, 2016, 37(2): 144-148.
[8]. Musgrave T, Benson C, Wong G, et al. The MAO inhibitor phenelzine improves functional outcomes in mice with experimental autoimmune encephalomyelitis (EAE)[J]. Brain, Behavior, and Immunity, 2011, 25(8): 1677-1688.
[9]. Benson C A, Wong G, Tenorio G, et al. The MAO inhibitor phenelzine can improve functional outcomes in mice with established clinical signs in experimental autoimmune encephalomyelitis (EAE)[J]. Behavioural brain research, 2013, 252: 302-311.
Phenelzine是一种单胺氧化酶（MAO） 抑制剂[1]。Phenelzine不可逆地抑制脑内单胺氧化酶A和B，减少去甲肾上腺素、多巴胺和血清素等神经递质的分解，从而提高这些物质的水平并改善情绪 [2-3]。Phenelzine主要用于治疗难治性抑郁症 [4]。
在PC12细胞中，Phenelzine（1-50μM；24h）可降低1-甲基-4-苯基吡啶（MPP+）引起的细胞核凝聚和碎裂 [5]。在3T3-F442A和3T3-L1细胞中，在较低浓度的Phenelzine（1-10μM；8d）下，可检测到细胞甘油三酯和固醇调节元件结合蛋白-1c（SREBP-1c）的降低 [6]。在Molt-4细胞中，Phenelzine（5-25μM；24h）可以上调组蛋白H3K4单甲基化、H3K4二甲基化和组蛋白H3乙酰化水平，上调p21和p15蛋白表达，下调DNMT1表达，最终抑制Molt-4细胞增殖，诱导细胞凋亡 [7]。
在实验性自身免疫性脑脊髓炎（EAE）小鼠模型中，Phenelzine（15mg/kg；ip；28d）可以延缓发病，缓解EAE小鼠慢性期，并显著改善探索行为、情绪障碍等非运动症状 [8]。在实验性自身免疫性脑脊髓炎小鼠模型中，Phenelzine（15mg/kg；ip；14d）可提高中枢神经系统中GABA、多巴胺和生物胺的水平 [9]。
| Cell experiment [1]: | |
Cell lines | PC12 cells |
Preparation Method | PC12 cells (4 × 104) were treated with 1-methyl-4-phenylpyridinium (MPP+) in the presence of Phenelzine for 24h at 37℃. The medium (200μL) was incubated with 10μL of 10mg/mL MTT solution for 2h at 37℃. Culture medium was removed, and 100μL of dimethyl sulfoxide was added to each well to dissolve the formazan. Absorbance was measured at 570nm using a microplate reader. Cell viability was expressed as a percent of the control culture value. |
Reaction Conditions | 1-50μM; 24h |
Applications | Phenelzine reduced the condensation and fragmentation of nuclei caused by MPP+ in PC12 cells. |
| Animal experiment [2]: | |
Animal models | Experimental autoimmune encephalomyelitis (EAE) mice model |
Preparation Method | In acute phenelzine treatment experiments, researchers typically administer a single intraperitoneal injection of 30mg/kg of Phenelzine (as the free base, dissolved in antibacterial water) to experimental autoimmune encephalomyelitis (EAE) mice at the peak of disease (score ≥ 3) or to control mice. Three hours after administration, mice are sacrificed, and central nervous system tissue is removed and cryopreserved for subsequent neurotransmitter analysis. Chronic treatment experiments involve daily intraperitoneal injections of 15mg/kg of Phenelzine or an equal volume of solvent for 28 consecutive days, starting on day 7 after modeling. Central nervous system (CNS) tissue is harvested the morning after treatment for immunohistochemistry or HPLC analysis. |
Dosage form | 15mg/kg; ip; 28d |
Applications | Phenelzine can delay the onset of disease, alleviate the chronic stage of EAE mice, and significantly improve non-motor symptoms such as exploratory behavior and emotional disorders. |
References: | |
| Cas No. | 51-71-8 | SDF | |
| 别名 | 苯乙肼,NSC 170957 | ||
| 化学名 | (2-phenylethyl)-hydrazine, monosulfate | ||
| Canonical SMILES | NNCCC1=CC=CC=C1 | ||
| 分子式 | C8H12N2 | 分子量 | 136.19 |
| 溶解度 | Slightly soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 7.3427 mL | 36.7134 mL | 73.4268 mL |
| 5 mM | 1.4685 mL | 7.3427 mL | 14.6854 mL |
| 10 mM | 0.7343 mL | 3.6713 mL | 7.3427 mL |
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动物平均体重 | g | |
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动物数量 | 只 |
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