反苯环丙胺半硫酸盐
货号：
IT2240
品牌：
Jinpan
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产品简介
| 有效期 | 2年 |
| 描述 | 是一种不可逆，非选择性 MAO 抑制剂。 |
| EC | EINECS 236-807-1 |
| MDL | MFCD00079222 |
| 别名 | 反-2-苯基环丙基胺半硫酸盐 |
| 英文名称 | Tranylcypromine Hemisulfate |
| CAS | 13492-01-8 |
| 分子式 | C18H24N2O4S |
| 分子量 | 364.46 |
| 储存条件 | 2-8℃ |
| 纯度 | ≥98% |
| 外观（性状） | Solid |
| 单位 | 瓶 |
| 生物活性 | Tranylcypromine hemisulfate是一种用于治疗抑郁症的不可逆，非选择性 MAO 抑制剂。[1-4] |
| In Vitro | Tranylcypromine（10 nM至10μM）独立于神经胶质细胞的存在，对人Aβ（1-42）寡聚体诱导的毒性发挥神经保护作用[1]。 Tranylcypromine（100μM）显著保护RGC免受谷氨酸神经毒性诱导的细胞凋亡以及氧化应激诱导的细胞凋亡。在谷氨酸（Glu）诱导的应激条件下，Tranylcypromine促进丝裂原活化蛋白激酶12（p38MAPKγ）的表达。此外，反苯环丙胺通过改变p38MAPKγ活性有助于RGC的存活[3]。 |
| In Vivo | 在诱导子宫内膜异位症的小鼠中，Tranylcypromine治疗显著且显著减少病变大小并以剂量依赖性方式改善全身性痛觉过敏。此外，反苯环丙胺处理导致对增殖，血管生成和H3K4甲基化的生物标志物的免疫反应性降低，导致EMT和病变生长停滞[2]。 Tranylcypromine（500 mM）注射在细胞内凋亡信号通路中发挥神经保护作用，抑制大鼠视网膜的形态变化，抑制caspase 3活性，恢复NMDA诱导的损伤后视网膜中p38MAPKγ的表达，增强视网膜损伤后的RGC存活率通过NMDA神经毒性的减弱[3]。如通过BrdU免疫组织化学检测的，Tranylcypromine（10μg/ g）导致所检查的组合脑区域中标记细胞的近似且显著加倍。 Tranylcypromine引起小脑细胞增殖的最大增加[4]。 |
| SMILES | N[C@H]1[C@H](C2=CC=CC=C2)C1.[0.5H2SO4] |
| 靶点 | Monoamine Oxidase（MAO） |
| 动物实验 | Briefly, the rats are anesthetized with an intraperitoneal injection of a 1:1 mixture of xylazine hydrochloride (4 mg/kg) and ketamine hydrochloride (10 mg/kg). Then, the pupil is dilated with phenylephrine hydrochloride and tropicamide eye drops, and 20 nmol NMDA with or without tranylcypromine is injected into the vitreous cavity. To assess the inhibitory effect of mitogen-activated protein kinase (MAPK), 100 nmol BIRB796 is intravitreally injected at the same time of NMDA injection. The injections are performed under a microscope using a 33-gauge needle connected to a microsyringe; the needle is inserted approximately 1.0 mm behind the corneal limbus. Next, either PBS (vehicle control) or 500 mM tranylcypromine (1000 nmol) mixed with 10 mM NMDA (20 nmol) in a total volume of 2.0 μL is injected into the vitreous cavity.[3] |
| 数据来源文献 | [1]. Caraci F, et al. Neuroprotective effects of the monoamine oxidase inhibitor tranylcypromine and its amide derivatives against Aβ(1-42)-induced toxicity. Eur J Pharmacol. 2015 Oct 5;764:256-263. [2]. Sun Q, et al. Tranylcypromine, a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Reprod Biol Endocrinol. 2016 Apr 9;14:17. [3]. Tsutsumi T, et al. Potential Neuroprotective Effects of an LSD1 Inhibitor in Retinal Ganglion Cells via p38 MAPK Activity. Invest Ophthalmol Vis Sci. 2016 Nov 1;57(14):6461-6473. [4]. Romanczyk TB, et al. The antidepressant tranylcypromine alters cellular proliferation and migration in the adult goldfish brain. Anat Rec (Hoboken). 2014 Oct;297(10):1919-26 |
| 规格 | 100mg |