哈尔满碱

哈尔满碱用途

Harmane,一种 β-咔啉生物碱 (BCA),是有效的神经毒素,可引起严重的动作震颤和精神病学表现。Harmane 对 I1 咪唑啉受体 (I1-Imidazoline receptor, IC50=30 nM) 的选择性是对 α2-肾上腺素受体 (IC50=18 μM) 的 1000 倍。Harmane 还是有效和选择性的单胺氧化酶抑制剂 (对 MAO A/B 的 IC50 值分别为 0.5 μM 和 5 μM)。Harmane 具有致突变作用。

哈尔满碱名称

[ CAS 号 ]:
486-84-0

[ 中文名 ]:
哈尔满碱

[ 英文名 ]:
Harmane

[中文别名 ]:

[英文别名 ]:

1-Methyl-9H-β-carboline
2-Methyl-b-carboline
Harmane
Aribine
MFCD00004957
Harman
1-Methyl-β-carboline
1-methylbetacarboline
Aribin
1-Methyl-9H-pyrid[3,4-b]indole

哈尔满碱生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> 咪唑啉受体

研究领域 >> 癌症

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 咪唑啉受体

信号通路 >> 神经信号通路 >> 单胺氧化酶

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

研究领域 >> 神经疾病

[ 靶点 ]

hMAO-A:0.5 μM (IC50)

MAO-B:5 μM (IC50)

α2-adrenergic receptor:18 μM (IC50)

I1-Imidazoline receptor:30 nM (IC50)

[参考文献]

[1]. Louis ED, et, al. Blood harmane concentrations and dietary protein consumption in essential tremor. Neurology. 2005 Aug 9;65(3):391-6.

[2]. Musgrave IF, et, al. Harmane produces hypotension following microinjection into the RVLM: possible role of I(1)-imidazoline receptors. Br J Pharmacol. 2000 Mar;129(6):1057-9.

[3]. Glover V, et, al. β-Carbolines as selective monoamine oxidase inhibitors:In vivo implications

[4]. Umezawa K, et, al. Comutagenic effect of norharman and harman with 2-acetylaminofluorene derivatives. Proc Natl Acad Sci U S A. 1978 Feb;75(2):928-30.

哈尔满碱物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
386.9±22.0 °C at 760 mmHg

[ 熔点 ]:
235-238 °C(lit.)

[ 分子式 ]:
C₁₂H₁₀N₂

[ 分子量 ]:
182.221

[ 闪点 ]:
176.2±13.6 °C

[ 精确质量 ]:
182.084396

[ PSA ]:
28.68000

[ LogP ]:
3.26

[ 外观性状 ]:
粉末

[ 蒸汽压 ]:
0.0±0.8 mmHg at 25°C

[ 折射率 ]:
1.750

[ 储存条件 ]:
库房通风低温干燥,与食品原料分开存放

哈尔满碱MSDS

详细MSDS(安全技术说明书)

哈尔满碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UV0280000

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

CAS REGISTRY NUMBER :: 486-84-0

BEILSTEIN REFERENCE NO. :: 0143898

LAST UPDATED :: 199612

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C12-H10-N2

MOLECULAR WEIGHT :: 182.24

WISWESSER LINE NOTATION :: T B656 EN HMJ F

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 50 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex)

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 200 mg/kg

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

TYPE OF TEST :: DNA adduct

MUTATION DATA

TYPE OF TEST :: Mutation in mammalian somatic cells

TEST SYSTEM :: Rodent - hamster Lung

DOSE/DURATION :: 100 mg/L

REFERENCE :: CALEDQ Cancer Letters (Shannon, Ireland). (Elsevier Scientific Pub. Ireland Ltd., POB 85, Limerick, Ireland) V.1- 1975- Volume(issue)/page/year: 17,249,1983

哈尔满碱安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
20/21

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
1544

[ WGK德国 ]:
3

[ RTECS号 ]:
UV0280000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933990090

哈尔满碱合成路线

详细合成路线

哈尔满碱上下游产品

哈尔满碱上游产品

哈尔满碱下游产品

哈尔满碱海关

[ 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%

哈尔满碱文献

Chemical genetics reveals a complex functional ground state of neural stem cells.

Nat. Chem. Biol. 3(5) , 268-273, (2007)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain canc...

Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.

Nat. Chem. Biol. 5 , 765-71, (2009)

Studies of gene function and molecular mechanisms in Plasmodium falciparum are hampered by difficulties in characterizing and measuring phenotypic differences between individual parasites. We screened...

The use of natural product scaffolds as leads in the search for trypanothione reductase inhibitors

Bioorg. Med. Chem. 16 , 6689, (2008)

Twenty-three heterocyclic compounds were evaluated for their potential as trypanothione reductase inhibitors. As a result, the harmaline, 10-thiaisoalloxazine, and aspidospermine frameworks were ident...

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