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去甲替林

去甲替林用途

去甲替林(去甲基阿米替林)是阿米替林的主要活性代谢产物,是一种用于缓解抑郁症症状的三环类抗抑郁药。去甲替林是一种有效的自噬抑制剂[1][2]。

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去甲替林名称

[ CAS 号 ]:
72-69-5

[ 中文名 ]:
去甲替林

[ 英文名 ]:
Nortriptyline

[英文别名 ]:

Sesaval
Lumbeck
NORTRIPTYLINE
Ateben
noramitriptyline
Noritren
allegron
[14C]-Nortriptyline
desmethylamitriptyline
lambeck

去甲替林生物活性

[ 描述 ]:

去甲替林(去甲基阿米替林)是阿米替林的主要活性代谢产物,是一种用于缓解抑郁症症状的三环类抗抑郁药。去甲替林是一种有效的自噬抑制剂[1][2]。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 自噬 >> 自噬

研究领域 >> 神经疾病

[参考文献]

[1]. Dean L. Amitriptyline Therapy and CYP2D6 and CYP2C19 Genotype. In: Pratt VM, Scott SA, Pirmohamed M, et al., eds. Medical Genetics Summaries. Bethesda (MD): National Center for Biotechnology Information (US); March 23, 2017.

[2]. Petrosyan E, et al. Repurposing Autophagy Regulators in Brain Tumors [published online ahead of print, 2022 Feb 18]. Int J Cancer. 2022;10.1002/ijc.33965.

去甲替林物理化学性质

[ 密度 ]:
1.084 g/cm3

[ 沸点 ]:
403.4ºC at 760 mmHg

[ 分子式 ]:
C₁₉H₂₁N

[ 分子量 ]:
263.37700

[ 闪点 ]:
194.9ºC

[ 精确质量 ]:
263.16700

[ PSA ]:
12.03000

[ LogP ]:
4.21730

[ 外观性状 ]:
白色固体

[ 折射率 ]:
1.633

[ 储存条件 ]:
2-8°C

去甲替林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HO9800000

CHEMICAL NAME :: 5H-Dibenzo(a,d)cycloheptene-delta(sup 5),gamma-propylamine, 10,11-dihydro-N-methyl-

CAS REGISTRY NUMBER :: 72-69-5

LAST UPDATED :: 199707

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C19-H21-N

MOLECULAR WEIGHT :: 263.41

WISWESSER LINE NOTATION :: L C676 BY&T&J BU3M1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 502 mg/kg

TOXIC EFFECTS :: Behavioral - muscle weakness Behavioral - ataxia Behavioral - muscle contraction or spasticity

REFERENCE :: HEPHD2 Handbook of Experimental Pharmacology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.50- 1978- Volume(issue)/page/year: 55,527,1980

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 22 mg/kg

TOXIC EFFECTS :: Behavioral - muscle weakness Behavioral - ataxia Behavioral - muscle contraction or spasticity

REFERENCE :: HEPHD2 Handbook of Experimental Pharmacology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.50- 1978- Volume(issue)/page/year: 55,527,1980

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 370 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,1561,1970

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 70 mg/kg

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

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 6,338,1963

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 17 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay)

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 17,65,1974 *** REVIEWS *** TOXICOLOGY REVIEW DICPBB Drug Intelligence and Clinical Pharmacy. (POB 42435, Cincinnati, OH 45242) V.3- 1969- Volume(issue)/page/year: 8,690,1974 TOXICOLOGY REVIEW CLCHAU Clinical Chemistry (Winston-Salem, NC). (American Assoc. for Clinical Chemistry, 1725 K St., NW, Washington, DC 20006) V.1- 1955- Volume(issue)/page/year: 19,361,1973 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4842 No. of Facilities: 25 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 2440 (estimated) No. of Female Employees: 1459 (estimated)

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去甲替林安全信息

[ 海关编码 ]:
2921499090

去甲替林合成路线

详细合成路线

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去甲替林海关

[ 海关编码 ]: 2921499090

[ 中文概述 ]:
2921499090 其他芳香单胺及衍生物及它们的盐. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2921499090 other aromatic monoamines and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%