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反苯环丙胺半硫酸盐

反苯环丙胺半硫酸盐用途

Tranylcypromine hemisulfate是一种用于治疗抑郁症的不可逆,非选择性 MAO 抑制剂。

反苯环丙胺半硫酸盐名称

[ CAS 号 ]:
13492-01-8

[ 中文名 ]:
反苯环丙胺半硫酸盐

[ 英文名 ]:
trans-2-Phenylcyclopropylamine hemisulfate salt

[中文别名 ]:

[英文别名 ]:

TRANS-2-PHENYLCYCLOPROPYLAMINE HEMISULFATE SALT
Tranylcypromine sulfate
Tranylcypromine
Tranylcypromine (hemisulfate)

反苯环丙胺半硫酸盐生物活性

[ 描述 ]:

Tranylcypromine hemisulfate是一种用于治疗抑郁症的不可逆,非选择性 MAO 抑制剂。

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> 组蛋白去甲基化酶

信号通路 >> 神经信号通路 >> 单胺氧化酶

研究领域 >> 神经疾病

[体外研究]

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)显着保护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]。

[体内研究]

在诱导子宫内膜异位症的小鼠中,Tranylcypromine治疗显着且显着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着加倍。 Tranylcypromine引起小脑细胞增殖的最大增加[4]。

[动物实验]

简言之，通过腹膜内注射盐酸甲苯噻嗪（4mg / kg）和盐酸氯胺酮（10mg / kg）的1：1混合物麻醉大鼠。然后，用盐酸苯肾上腺素和托吡卡胺滴眼剂扩张瞳孔，并将含有或不含反苯环丙胺的20nmol NMDA注射到玻璃体腔中。为了评估丝裂原活化蛋白激酶（MAPK）的抑制作用，在NMDA注射的同时玻璃体内注射100nmol BIRB796。使用连接到微量注射器的33号针在显微镜下进行注射;将针插入角膜缘后约1.0mm处。接下来，将总体积为2.0μL的PBS（载体对照）或与10mM NMDA（20nmol）混合的500mM反苯环丙胺（1000nmol）注射到玻璃体腔中。

[参考文献]

[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.

[相关活性小分子]

反苯环丙胺半硫酸盐物理化学性质

[ 密度 ]:
1.065g/cm3

[ 沸点 ]:
218.3ºC at 760mmHg

[ 分子式 ]:
C₉H₁₂NO₂S_0.5

[ 分子量 ]:
182.23

[ 闪点 ]:
90.8ºC

[ PSA ]:
135.02000

[ LogP ]:
4.83100

[ 蒸汽压 ]:
0.127mmHg at 25°C

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
Soluble in water; very slightly soluble in ethanol (96%) and in ether .

反苯环丙胺半硫酸盐MSDS

详细MSDS(安全技术说明书)

反苯环丙胺半硫酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GZ2625000

CAS REGISTRY NUMBER :: 13492-01-8

LAST UPDATED :: 199610

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C9-H11-N.1/2H2-O4-S

MOLECULAR WEIGHT :: 360.46

WISWESSER LINE NOTATION :: L3TJ AZ BR 2 &..H2.S-O4

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 34 mg/kg/60D-I

TOXIC EFFECTS :: Peripheral Nerve and Sensation - paresthesis Musculoskeletal - joints

REFERENCE :: AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 140,1229,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 1200 ug/kg/3D-I

TOXIC EFFECTS :: Vascular - BP lowering not characterized in autonomic section

REFERENCE :: AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 144,119,1987

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 45 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ABMGAJ Acta Biologica et Medica Germanica. (Berlin, Ger. Dem. Rep.) V.1-41, 1958-82. For publisher information, see BBIADT. Volume(issue)/page/year: 18,617,1967

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 38 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,359,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 41 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: EJPHAZ European Journal of Pharmacology. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1967- Volume(issue)/page/year: 6,115,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 37 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,359,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BJPCAL British Journal of Pharmacology and Chemotherapy. (London, UK) V.1-33, 1946-68. For publisher information, see BJPCBM. Volume(issue)/page/year: 25,158,1965 *** REVIEWS *** TOXICOLOGY REVIEW IDPYAK Industrial Pharmacology. (Mount Kisco, NY) V.1-3, 1974-79. Discontinued. Volume(issue)/page/year: 2,209,1975 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5685 No. of Facilities: 8 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 239 (estimated) No. of Female Employees: 157 (estimated)

反苯环丙胺半硫酸盐安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300-H311-H331

[ 警示性声明 ]:
P261-P264-P280-P301 + P310-P311

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R23/24/25

[ 安全声明 (欧洲) ]:
36/37/39-45

[ 危险品运输编码 ]:
UN 2811 6

[ WGK德国 ]:
3

[ RTECS号 ]:
GZ2625000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)