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| 靶点 |
MAO (monoamine oxidase)
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| 体外研究 (In Vitro) |
过氧亚硝酸盐是血管内室中由超氧化物阴离子和一氧化氮产生的一种活性氮。过氧亚硝酸盐破坏血浆蛋白、红细胞和血小板的膜。这就解释了为什么过亚硝酸盐的过量生产会导致疾病和衰老。拮抗过氧亚硝酸盐的治疗方法可以延缓衰老和疾病进展。我们开发了一种体外测定法，可以研究过氧亚硝酸盐在血管内室中引起的氧化损伤。该测定将损伤与蛋白质羰基、3-硝基酪氨酸（3-NT）和硫代巴比妥酸反应物质的形成速率相关联。使用该测定法，我们评估了酚嗪（一种活性醛的清除剂）拮抗过氧亚硝酸盐作用的能力。在此，我们发现吩噻嗪显著降低了血浆和血小板中过氧亚硝酸盐引起的脂质过氧化损伤。此外，它还抑制了血浆和血小板蛋白中羰基和3-NT的形成。
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| 体内研究 (In Vivo) |
在小鼠中，与媒介物对照治疗的小鼠相比，在严重胸部压迫后立即腹膜内注射酚嗪，此后每天注射一次，持续6周，在脊髓损伤后4周和5周改善后肢功能，减少星形胶质细胞增生，促进轴突再生/发芽。Phenelzine的应用上调了脊髓中L1的表达，并刺激了脊髓组织中同源L1介导的细胞内信号级联。在炎症的急性期，经吩嗪治疗的小鼠损伤脊髓中的促炎细胞因子水平降低，如白细胞介素-1β、白细胞介素-6和肿瘤坏死因子-α[2]。
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| 酶活实验 |
这项研究开发了一种体外测定法，可以研究过氧亚硝酸盐在血管内室中引起的氧化损伤。该测定将损伤与蛋白质羰基、3-硝基酪氨酸（3-NT）和硫代巴比妥酸反应物质的形成速率相关联。使用该测定法，本研究评估了酚嗪（一种活性醛的清除剂）拮抗过氧亚硝酸盐作用的能力。在此，本研究表明，吩噻嗪可显著降低血浆和血小板中过氧亚硝酸盐引起的脂质过氧化损伤[1]。
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| 动物实验 |
In mice, intraperitoneal injection of phenelzine immediately after severe thoracic compression, and thereafter once daily for 6 weeks, improved hind limb function, reduced astrogliosis and promoted axonal regrowth/sprouting at 4 and 5 weeks after spinal cord injury compared to vehicle control-treated mice[2].
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| 参考文献 |
[1]. Phenelzine reduces the oxidative damage induced by peroxynitrite in plasma lipids and proteins. Arch Physiol Biochem. 2018 Dec;124(5):418-423.
[2]. Phenelzine, a small organic compound mimicking the functions of cell adhesion molecule L1, promotes functional recovery after mouse spinal cord injury. Restor Neurol Neurosci . 2018;36(4):469-483. |
| 其他信息 |
Phenelzine is a primary amine.
Phenelzine, with the formula β-phenylethylhydrazine, is a monoamine oxidase inhibiting antidepressant that is effective in the treatment of panic disorder and social anxiety disorder. It was developed by Parke Davis and originally FDA approved on June 9th, 1961. It is currently approved under prescription by the name of Nardil.
Phenelzine is a Monoamine Oxidase Inhibitor. The mechanism of action of phenelzine is as a Monoamine Oxidase Inhibitor. Phenelzine is a monoamine oxidase inhibitor (MAO inhibitor) used in therapy of moderate-to-severe depression. Phenelzine therapy is associated with rare instances of clinically apparent acute liver injury. Phenelzine is only found in individuals that have used or taken this drug. It is an irreversible non-selective inhibitor of monoamine oxidase. May be used to treat major depressive disorder.Although the exact mechanism of action has not been determined, it appears that the irreversible, nonselective inhibition of MAO by phenelzine relieves depressive symptoms by causing an increase in the levels of serotonin, norepinephrine, and dopamine in the neuron. One of the MONOAMINE OXIDASE INHIBITORS used to treat DEPRESSION; PHOBIC DISORDERS; and PANIC. View More
Drug Indication Pharmacodynamics The elimination of monoamine oxidase by phenelzine results in the elevation of brain amines such as 2-phenylethylamine which is a metabolite of phenelzine. These amines have then marked effects on the uptake and release of catecholamines and serotonin in nerve endings. Phenelzine is shown to elevate brain levels of the gamma-aminobutyric acid (GABA) and alanine (ALA) as well as to inhibit the activity of the transaminases that normally metabolize these amino acids. In preclinical studies, it has been shown to be neuroprotective in cerebral ischemia. Absorption Phenelzine is rapidly absorbed from the gastrointestinal tract. The decay of the drug action is not dependent on the pharmacokinetic parameters but on the rate of protein synthesis which restores the functional levels of monoamine oxidase. The mean Cmax is 19.8 ng/ml and it occurs after 43 minutes of dose administration. Route of Elimination The elimination of the administered dose is mainly composed of the phenelzine metabolites, phenylacetic acid and parahydroxyphenylacetic acid that constitute 79% of the dose found in the urine in the first 96 hours. Volume of Distribution The volume of distribution of phenelzine is hard to determine as drugs from this kind penetrate the CNS very well into the tissue where their activity is desired. Following ip injection of 2.5 mg/kg bw phenelzine-1-(14)C sulfate to rats, 62% of the dose was recovered in the urine within 24 hours. Metabolism / Metabolites For the metabolic studies, it is assumed that phenelzine is acetylated. Some of the metabolites of phenelzine are phenylacetic acid, 2-phenylethylamine and 4-hydroxyphenylacetic acid as major metabolites and N-acetyl-phenelzine as a minor metabolite. DrugBank Nardil is extensively metabolized, primarily by oxidation via monoamine oxidase. After oral administration of (13)C6-phenelzine, 73% of the administered dose was recovered in urine as phenylacetic acid and parahydroxyphenylacetic acid within 96 hours. Acetylation to N2-acetylphenelzine is a minor pathway. Biological Half-Life After administration phenelzine presents a very short half-life of 11.6 hours in humans. The mean apparent half-life, estimated from urinary excretion data in patients who received oral doses of 30 mg thrice daily, was 0.87 hours following the initial dose and 3.11 hours after 13 days of treatment. Mechanism of Action The basic mechanism of action of phenelzine acts as an inhibitor and substrate of monoamine oxidase which subsequently causes an elevation in brain levels of catecholamines and serotonin. It also presents a similar structure to amphetamine which explains the effect on the uptake and release of dopamine, noradrenaline, and serotonin. Phenelzine has been reported to inhibit tyrosine aminotransferase, aromatic amino acid decarboxylase, and dopamine B-hydroxylase. The antidepressant phenelzine is a monoamine oxidase inhibitor known to inhibit various other enzymes, among them semicarbazide-sensitive amine oxidase (currently named primary amine oxidase: SSAO/PrAO), absent from neurones but abundant in adipocytes. It has been reported that phenelzine inhibits adipocyte differentiation of cultured preadipocytes. To further explore the involved mechanisms, our aim was to study in vitro the acute effects of phenelzine on de novo lipogenesis in mature fat cells. Therefore, glucose uptake and incorporation into lipid were measured in mouse adipocytes in response to phenelzine, other hydrazine-based SSAO/PrAO-inhibitors, and reference agents. None of the inhibitors was able to impair the sevenfold activation of 2-deoxyglucose uptake induced by insulin. Phenelzine did not hamper the effect of lower doses of insulin. However, insulin-stimulated glucose incorporation into lipids was dose-dependently inhibited by phenelzine and pentamidine, but not by semicarbazide or BTT2052. In contrast, all these SSAO/PrAO inhibitors abolished the transport and lipogenesis stimulation induced by benzylamine. These data indicate that phenelzine does not inhibit glucose transport, the first step of lipogenesis, but inhibits at 100 uM the intracellular triacylglycerol assembly, consistently with its long-term anti-adipogenic effect and such rapid action was not found with all the hydrazine derivatives tested. Therefore, the alterations of body weight control consecutive to the use of this antidepressant drug might be not only related to central effects on food intake/energy expenditure, but could also depend on its direct action in adipocytes. Nonetheless, phenelzine antilipogenic action is not merely dependent on SSAO/PrAO inhibition. |
| 分子式 |
C8H12N2
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|---|---|
| 分子量 |
136.20
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| 精确质量 |
136.1
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| 元素分析 |
C, 70.55; H, 8.88; N, 20.57
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| CAS号 |
51-71-8
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| 相关CAS号 |
51-71-8; 156-51-4 (sulfate);
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| PubChem CID |
3675
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| 外观&性状 |
Typically exists as solid at room temperature
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| 密度 |
1.0±0.1 g/cm3
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| 沸点 |
281.4±19.0 °C at 760 mmHg
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| 闪点 |
143.7±25.1 °C
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| 蒸汽压 |
0.0±0.6 mmHg at 25°C
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| 折射率 |
1.550
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| LogP |
1.14
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| tPSA |
38.05
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| SMILES |
NNCCC1=CC=CC=C1
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| InChi Key |
RMUCZJUITONUFY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H12N2/c9-10-7-6-8-4-2-1-3-5-8/h1-5,10H,6-7,9H2
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| 化学名 |
Hydrazine, (2-phenylethyl)-
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| 别名 |
Phenelzine; 51-71-8; Phenethylhydrazine; 2-Phenylethylhydrazine; Nardil; Fenelzyne; Hydrazine, (2-phenylethyl)-; Fenelzyna;
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外实验) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| 溶解度 (体外实验) |
注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。
注射用配方
注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)(IP/IV/IM/SC等) *生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。 注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline) 注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil) 示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。 View More
注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)] 口服配方
口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠) 口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素) 示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。 View More
口服配方 3: 溶解于 PEG400 (聚乙二醇400) 请根据您的实验动物和给药方式选择适当的溶解配方/方案： 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 7.3421 mL | 36.7107 mL | 73.4214 mL | |
| 5 mM | 1.4684 mL | 7.3421 mL | 14.6843 mL | |
| 10 mM | 0.7342 mL | 3.6711 mL | 7.3421 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
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