N-甲基金雀花碱

N-甲基金雀花碱用途

N-Methylcytisine (Caulophylline) 是一种三环喹啉类生物碱,具有降血糖、镇痛、抗炎活性。N-Methylcytisine 是中枢神经系统中乙酰胆碱烟碱受体的选择性配体,对鱿鱼视神经节中的烟碱乙酰胆碱受体具有很高的亲和力 (Kd: 50 nM)。

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N-甲基金雀花碱名称

[ CAS 号 ]:
486-86-2

[ 中文名 ]:
N-甲基野靛碱

[ 英文名 ]:
N-methylcytisine

[中文别名 ]:

[英文别名 ]:

N-methylcytisine
N－Methylcytisine
Caulophylline

N-甲基金雀花碱生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 胆碱受体

信号通路 >> 神经信号通路 >> 胆碱受体

研究领域 >> 炎症/免疫

[ 靶点 ]

kd: 50 nM (nicotinic acetylcholine receptors)[2]

[参考文献]

[1]. Jiao YF, et al. N-Methylcytisine Ameliorates Dextran-Sulfate-Sodium-Induced Colitis in Mice by Inhibiting the Inflammatory Response. Molecules. 2018 Feb 25;23(3). pii: E510.

[2]. Pliashkevich IuG, et al. [N-methylcytisine--a selective ligand of nicotinic receptors of acetylcholine in the CNS]. Biull Eksp Biol Med. 1987 Dec;104(12):690-2.

N-甲基金雀花碱物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
400.8±34.0 °C at 760 mmHg

[ 熔点 ]:
137-139ºC

[ 分子式 ]:
C₁₂H₁₆N₂O

[ 分子量 ]:
204.27

[ 闪点 ]:
191.9±18.0 °C

[ 精确质量 ]:
204.126266

[ PSA ]:
25.24000

[ LogP ]:
0.46

[ 外观性状 ]:
褐色粉末

[ 蒸汽压 ]:
0.0±0.9 mmHg at 25°C

[ 折射率 ]:
1.616

[ 储存条件 ]:
室温，密封，干燥

N-甲基金雀花碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HA4400000

CHEMICAL NAME :: Cytisine, 12-methyl-

CAS REGISTRY NUMBER :: 486-86-2

BEILSTEIN REFERENCE NO. :: 0012448

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C12-H16-N2-O

MOLECULAR WEIGHT :: 204.30

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 511 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Behavioral - muscle contraction or spasticity

REFERENCE :: BJPCBM British Journal of Pharmacology. (Macmillan Press Ltd., Houndmills, Basingstoke, Hants. RG21 2XS, UK) V.34- 1968- Volume(issue)/page/year: 35,161,1969

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 51 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Behavioral - muscle contraction or spasticity

REFERENCE :: BJPCBM British Journal of Pharmacology. (Macmillan Press Ltd., Houndmills, Basingstoke, Hants. RG21 2XS, UK) V.34- 1968- Volume(issue)/page/year: 35,161,1969

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 22 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 79,334,1943

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 160 mg/kg

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

REFERENCE :: JOETD7 Journal of Ethnopharmacology. (Elsevier Scientific Pub. Ireland Ltd., POB 85, Limerick, Ireland) V.1- 1979- Volume(issue)/page/year: 7,24,1983

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N-甲基金雀花碱安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
HA4400000

N-甲基金雀花碱

N-甲基金雀花碱用途

N-甲基金雀花碱名称

N-甲基金雀花碱生物活性

N-甲基金雀花碱物理化学性质

N-甲基金雀花碱毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

N-甲基金雀花碱安全信息

N-甲基金雀花碱合成路线

详细合成路线

N-甲基金雀花碱上下游产品

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