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马普替林

马普替林用途

马普替林是一种高选择性去甲肾上腺素能再摄取阻断剂,具有很强的抗抑郁疗效。马普替林通过靶向ERK信号通路和CRABP1诱导癌细胞凋亡。马普替尼抑制细胞增殖和转移,具有抗癌作用[1][2]。

马普替林名称

[ CAS 号 ]:
10262-69-8

[ 中文名 ]:
马普替林

[ 英文名 ]:
maprotiline

[中文别名 ]:

[英文别名 ]:

Deprilept
Dibencycladine
N-methyl-9,10-ethanoanthracene-9(10H)-propanamine
Maprotilina
Maprotylina [Polish]
Maprotilinum
MFCD00661057
Maprotilin
Maprotilinum [INN-Latin]
EINECS 233-599-4

马普替林生物活性

[ 描述 ]:

[ 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

[体外研究]

马普替林(10μM)增强肝癌细胞对索拉非尼(2μM)的敏感性并诱导凋亡[2]。马普替林(0、10或20μM,72小时)作用于ERK途径,并抑制HepG2和Huh7细胞中SREBP2的磷酸化[2]。马普替林可能靶向CRABP1并调节HCC细胞中胆固醇的生物合成[2]。细胞侵袭实验[2]细胞系：人肝癌细胞系Huh7和HepG2浓度：0、10、20μM孵育时间：24小时结果：抑制肝癌细胞迁移,抑制上皮-间充质转化。细胞活性测定[2]细胞系：人肝癌细胞系Huh7和HepG2浓度：0、10、20μM孵育时间：0、24、48、72、96、120小时结果：触发细胞凋亡,并以剂量和时间依赖性方式抑制Huh7细胞和HepG1细胞的活性。Western Blot分析[2]细胞系：人肝癌细胞系Huh7和HepG2浓度：0、10、20μM孵育时间：72小时结果：抑制肝癌细胞胆固醇生物合成。

[体内研究]

马普替林(腹腔注射；3、10或30 mg/kg)与合成大麻素WIN 55212-2结合,有效减少神经病理性疼痛[1]。马普替林(腹腔注射；0、20或40 mg/kg；每周两次；3周)对器官、免疫系统和造血功能显示低毒副作用[2]。马普替林(腹腔注射；0、20或40 mg/kg；每周两次；3周)通过与CRABP1相互作用抑制胆固醇生物合成,抑制肝癌细胞的生长和转移[2]。动物模型：雄性Balb-c小鼠(25-30g)[1]剂量：3、10、30mg/kg给药：腹腔注射；治疗30分钟后评估结果：神经病变小鼠疼痛相关行为减弱。动物模型：裸鼠(BALB/C nu/nu,4-6周龄,雌性)[2]剂量：40 mg/kg给药：腹腔注射；一周两次3周结果：降低血清和肿瘤中的胆固醇水平,抑制Huh7衍生肿瘤异种移植物的生长,无明显毒性作用。

[参考文献]

[1]. Gunduz O, et al. Analysis of the anti-allodynic effects of combination of a synthetic cannabinoid and a selective noradrenaline re-uptake inhibitor in nerve injury-induced neuropathic mice. Eur J Pain. 2016 Mar. 20(3):465-71.

[2]. Zheng C, et al. Maprotiline Suppresses Cholesterol Biosynthesis and Hepatocellular Carcinoma Progression Through Direct Targeting of CRABP1. Front Pharmacol. 2021 May 20. 12:689767.

马普替林物理化学性质

[ 密度 ]:
1.08 g/cm3

[ 沸点 ]:
399.6ºC at 760 mmHg

[ 分子式 ]:
C₂₀H₂₃N

[ 分子量 ]:
277.40300

[ 闪点 ]:
187.7ºC

[ 精确质量 ]:
277.18300

[ PSA ]:
12.03000

[ LogP ]:
4.60230

[ 蒸汽压 ]:
1.35E-06mmHg at 25°C

[ 折射率 ]:
1.599

[ 储存条件 ]:
室温，密闭，干燥

马普替林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KJ4552000

CHEMICAL NAME :: 9,10-Ethanoanthracene-9(10H)-propylamine, N-methyl-

CAS REGISTRY NUMBER :: 10262-69-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C20-H23-N

MOLECULAR WEIGHT :: 277.44

WISWESSER LINE NOTATION :: L6 H666/GP 2AF P&&TTJ O3M1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 26 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - coma Vascular - BP elevation not characterized in autonomic section

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 2,260,1977

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 760 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 105 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - muscle weakness Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: APPHAX Acta Poloniae Pharmaceutica. For English translation, see APPFAR. (Ars Polona, POB 1001, 00-680 Warsaw 1, Poland) V.1- 1937- Volume(issue)/page/year: 40,235,1983

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 38 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 :: 660 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 140 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: APPHAX Acta Poloniae Pharmaceutica. For English translation, see APPFAR. (Ars Polona, POB 1001, 00-680 Warsaw 1, Poland) V.1- 1937- Volume(issue)/page/year: 40,235,1983

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 31 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 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5760 mg/kg/22W-I

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects Related to Chronic Data - death

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1709,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 650 mg/kg/7W-I

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects

REFERENCE :: ARTODN Archives of Toxicology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.32- 1974- Volume(issue)/page/year: 51,43,1982

马普替林安全信息

[ 危险品运输编码 ]:
3249

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2921499090

马普替林合成路线

详细合成路线

马普替林上下游产品

马普替林上游产品

马普替林下游产品

马普替林制备

由β-（9-蒽基）丙酸经还原得9-（3-羟基丙基）蒽，经氯代后与甲胺缩合得β[（9-蒽基）丙基]甲胺，然后与乙烯缩合制得麦普替林。

马普替林海关

[ 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%