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哈尔碱；哈尔明碱；肉叶云香碱；去氢骆驼蓬碱

用途

Harmine是一种具有抗癌和抗炎活性的天然双特异性酪氨酸磷酸化调节激酶 ((DYRK)) 抑制剂。

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名称

[ CAS 号 ]:
442-51-3

[ 中文名 ]:
肉叶云香碱

[ 英文名 ]:
Harmine

[中文别名 ]:

[英文别名 ]:

9H-Pyrido(3,4-b)indole, 7-methoxy-1-methyl-
Yajeine
Banisterine
Harmine
7-Methoxy-1-methyl-9H-β-carboline
Telepathin
Yagein
Garmin
Telepathien
Harmin

生物活性

[ 描述 ]:

Harmine是一种具有抗癌和抗炎活性的天然双特异性酪氨酸磷酸化调节激酶 ((DYRK)) 抑制剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

信号通路 >> 蛋白酪氨酸激酶 >> DYRK

信号通路 >> 细胞周期/DNA损伤 >> RAD51

研究领域 >> 癌症

天然产物 >> 生物碱

研究领域 >> 神经疾病

[ 靶点 ]

5-HT2A Receptor:397 nM (Ki)

DYRK1A

RAD51

[体外研究]

Harmine是5-HT2A的抑制剂,Ki为397 nM [1]。 Harmine通过选择的DANDY抑制DYRK1A的tau磷酸化,IC50为190 nM [2] .Harmine通过干扰Rad51募集负调节HR,导致肝癌细胞的严重细胞毒性。此外,NHEJ抑制剂Nu7441显着增强Hep3B细胞对Harmine的抗增殖作用[3]。

[体内研究]

结果表明,TBI组脑水含量显着增加。与TBI组相比,Harmine治疗在第1,3和5天显着降低组织水含量。与TBI组相比,Harmine治疗显着降低了3天和5天的逃避潜伏期。与没有Harmine治疗的TBI组相比,TBI后TBI给予显着改善TBI后1,3和5天大鼠的运动功能恢复。与TBI组相比,Harmine治疗组的神经元存活率显着增加。与TBI组相比,给予Harmine导致GLT-1表达显着升高。与TBI组相比,Harmine的给药显着降低了caspase 3的表达[4]。

[动物实验]

大鼠[4]共150只雄性Sprague-Dawley大鼠（年龄10-12周;体重280-320g;用于本研究。大鼠随机分为三组：假手术组（假手术组） ; n = 15）; TBI组（TBI; n = 35）和TBI + Harmine治疗组（Harmine; n = 35）。在TBI（ip，30 mg / kg / d）后立即给予Harmine用于向上假性和TBI组接受等体积的0.9％生理盐水（ip）。大鼠按如下分组进行行为恢复检查：Sham，n = 3; TBI，n = 7;和Harmine，n = 7.在TBI后，在第1,3和5天评估NSS。每只大鼠由对动物治疗不知情的观察者进行评估[4]。

[参考文献]

[1]. Glennon RA, et al. Binding of beta-carbolines and related agents at serotonin (5-HT(2) and 5-HT(1A)), dopamine (D(2)) and benzodiazepine receptors. Drug Alcohol Depend. 2000 Aug 1;60(2):121-32.

[2]. Neumann F, et al. DYRK1A inhibition and cognitive rescue in a Down syndrome mouse model are induced by new fluoro-DANDY derivatives. Sci Rep. 2018 Feb 12;8(1):2859.

[3]. Zhang L, et al. Harmine suppresses homologous recombination repair and inhibits proliferation of hepatoma cells. Cancer Biol Ther. 2015;16(11):1585-92.

[4]. Zhong Z, et al. Treatment with harmine ameliorates functional impairment and neuronal death following traumatic brain injury. Mol Med Rep. 2015 Dec;12(6):7985-91.

[相关活性小分子]

T0070907 | 2-胺基-5-(4-硝基苯磺酰)-噻唑 | 血清胺盐酸盐 | RS-1 | 阿魏酸钠 | 3-氯-1-(3,4-二氯苯基)-4-(4-吗啉基)-1H-吡咯-2,5-二酮 | 盐酸硫利达嗪 | 依匹哌唑 | 利培酮 | TG6-10-1 | AZ191 | 卡利拉嗪 | 喹硫平 | 舍吲哚 | MIRK-IN-1

物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
421.4±40.0 °C at 760 mmHg

[ 熔点 ]:
262-264 °C(lit.)

[ 分子式 ]:
C₁₃H₁₂N₂O

[ 分子量 ]:
212.247

[ 闪点 ]:
139.8±17.0 °C

[ 精确质量 ]:
212.094955

[ PSA ]:
37.91000

[ LogP ]:
3.17

[ 外观性状 ]:
灰白色固体

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.706

[ 储存条件 ]:
库房低温,通风,干燥,与食品原料分开存放

MSDS

详细MSDS(安全技术说明书)

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UV0175000

CHEMICAL NAME :: 9H-Pyrido(3,4-b)indole, 7-methoxy-1-methyl-

CAS REGISTRY NUMBER :: 442-51-3

BEILSTEIN REFERENCE NO. :: 0178813

LAST UPDATED :: 199612

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C13-H12-N2-O

MOLECULAR WEIGHT :: 212.27

WISWESSER LINE NOTATION :: T B656 EN HMJ F1 KO1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 3 mg/kg

TOXIC EFFECTS :: Behavioral - sleep Behavioral - tremor Gastrointestinal - nausea or vomiting

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 129,133,1928

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 200 mg/kg

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

REFERENCE :: PSCBAY Psychopharmacology Service Center, Bulletin. (Bethesda, MD) V.1-3, 1961-65. For publisher information, see PSYBB9. Volume(issue)/page/year: 2,17,1963

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 243 mg/kg

TOXIC EFFECTS :: Behavioral - excitement Skin and Appendages - hair

REFERENCE :: PCJOAU Pharmaceutical Chemistry Journal (English Translation). Translation of KHFZAN. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) No.1- 1967- Volume(issue)/page/year: 10,1171,1976

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 50 mg/kg

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

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 129,133,1928

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 10 mg/kg

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

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 129,133,1928

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 129,133,1928

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 60 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - excitement Behavioral - ataxia

REFERENCE :: NEPHBW Neuropharmacology. (Pergamon Press Ltd., Headington Hill Hall, Oxford OX3 OBW, UK) V.9- 1970- Volume(issue)/page/year: 10,15,1971

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 100 mg/kg

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

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 129,133,1928

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Amphibian - frog

DOSE/DURATION :: 300 mg/kg

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

REFERENCE :: QJPPAL Quarterly Journal of Pharmacy & Pharmacology. (London, UK) V.2-21, 1929-48. For publisher information, see JPPMAB. Volume(issue)/page/year: 9,37,1936 *** REVIEWS *** TOXICOLOGY REVIEW PISDDJ Pacific Information Service on Street Drugs. (J.K. Brown, School of Pharmacy, Univ. of the Pacific, Stockton, CA 95211) V.1- 1972(?)- Volume(issue)/page/year: 5(3-6),-,1977 TOXICOLOGY REVIEW CTOXAO Clinical Toxicology. (New York, NY) V.1-18, 1968-81. For publisher information, see JTCTDW. Volume(issue)/page/year: 12,1,1978

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安全信息

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R20/21/22;R36

[ 安全声明 (欧洲) ]:
S22-S24/25-S36/37-S26

[ 危险品运输编码 ]:
1544

[ WGK德国 ]:
3

[ RTECS号 ]:
UV0175000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1

[ 海关编码 ]:
2933990090

合成路线

详细合成路线

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海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

哈尔碱；哈尔明碱；肉叶云香碱；去氢骆驼蓬碱

用途

名称

生物活性

物理化学性质

MSDS

详细MSDS(安全技术说明书)

毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

安全信息

合成路线

详细合成路线

上下游产品

上游产品

下游产品

海关

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哈尔碱； 哈尔明碱； 肉叶云香碱； 去氢骆驼蓬碱

用途

名称

生物活性

物理化学性质

MSDS

详细MSDS(安全技术说明书)

毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

安全信息

合成路线

详细合成路线

上下游产品

上游产品

下游产品

海关

相关化工产品/化学物质：

相关药品：

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相关化合物

哈尔碱；哈尔明碱；肉叶云香碱；去氢骆驼蓬碱