Tranylcypromine hemisulfate

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Chemical Structure| 13492-01-8 同义名 : 反式-2-苯基环丙胺 半硫酸盐 ;SKF 385 hemisulfate; Parnate; Tranylcypromine Sulfate; Tranylcypromine(hemisulfate)
CAS号 : 13492-01-8
货号 : A354034
分子式 : C18H24N2O4S
纯度 : 99%
分子量 : 364.46
MDL号 : MFCD00079222
存储条件：

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Tranylcypromine hemisulfate is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. TCP (Tranylcypromine) significantly prevented Aβ-induced neuronal death in a concentration-dependent fashion and was maximally protective only at 10 µM. TCP-But was maximally protective in mixed neuronal cultures at 1 µM, a lower concentration compared to TCP, whereas the new derivative, TCP-Ac(TCP acetamide), was more efficacious than TCP and TCP-But (TCP butyramide) and significantly protected cortical neurons against Aβ toxicity at nanomolar concentrations (100 nM)[3]. TC (tranylcypromine) treatment significantly and substantially reduced the lesion size and improved generalized hyperalgesia in a dose-dependent fashion in mice with induced endometriosis. In addition, TC treatment resulted in reduced immunoreactivity to biomarkers of proliferation, angiogenesis, and H3K4 methylation, leading to arrested EMT (epithelial-mesenchymal transition) and lesion growth[4]. Tranylcypromine (100 μM) significantly protects RGCs (retinal ganglion cell) from glutamate neurotoxicity-induced apoptosis as well as apoptosis induced by oxidative stress. Tranylcypromine promotes mitogen-activated protein kinase 12 (p38 MAPKγ) expression under conditions of glutamate (Glu)-induced stress. Besides, tranylcypromine contributes to RGC survival via alterations of p38 MAPKγ activity. Tranylcypromine (500 mM) injection exerts neuroprotective effects within intracellular apoptotic signaling pathways and suppresses morphologic changes in the retina of the rat, suppresses caspase 3 activity and recovers p38 MAPKγ expression in the retina after NMDA-induced injury, and enhances RGC survival after retinal injury via the attenuation of NMDA neurotoxicity[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.72mL

2.74mL

1.37mL

27.44mL

5.49mL

2.74mL
参考文献

[1]Sun Q, Ding D, 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.

[2]Caraci F, Pappalardo G, 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;764:256-63.

[3]Caraci F, Pappalardo G, Basile L, Giuffrida A, Copani A, Tosto R, Sinopoli A, Giuffrida ML, Pirrone E, Drago F, Pignatello R, Guccione S. 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

[4]Sun Q, Ding D, Liu X, Guo SW. 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

[5]Tsutsumi T, Iwao K, Hayashi H, Kirihara T, Kawaji T, Inoue T, Hino S, Nakao M, Tanihara H. 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