鱼藤酮_MSDS_作用_用途_鱼藤酮CAS号【83-79-4】

Rotenone是线粒体电子传递链复合物I抑制剂。

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1）体外活性
丝裂原活化蛋白激酶（MAPK），Toll样受体，Wnt和Ras信号通路密切参与鱼藤酮对ENS的作用。通过MCE处理降低了鱼藤酮诱导的细胞死亡，如通过促凋亡蛋白水平的下降所测量的。此外，MCE治疗显着增加抗细胞凋亡Bcl2的水平并阻断细胞色素c的释放，从而减轻鱼藤酮诱导的多巴胺能神经元损失，如纹状体中酪氨酸羟化酶（TH）免疫染色所证明。
2）体内活性
鱼藤酮引起兴奋性氨基酸神经递质的显着增加; 在PD大鼠模型的小脑中观察到谷氨酸和天冬氨酸以及抑制性氨基酸，GABA，甘氨酸和牛磺酸的显着降低。鱼藤酮（1.5,2或2.5 mg / kg）引起黑质中α-突触核蛋白的剂量依赖性增加。此外，在2和2.5 mg / kg时，鱼藤酮导致黑质中酪氨酸羟化酶免疫反应神经元和大鼠纹状体中多巴胺的数量显着减少。

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[ 描述 ]:

Rotenone是线粒体电子传递链复合物I抑制剂。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 线粒体代谢

研究领域 >> 神经疾病

[体外研究]

丝裂原活化蛋白激酶(MAPK),Toll样受体,Wnt和Ras信号通路密切参与鱼藤酮对ENS的作用[2]。通过处理降低了鱼藤酮诱导的细胞死亡,如通过促凋亡蛋白水平的下降所测量的。此外,处理显着增加抗细胞凋亡Bcl2的水平并阻断细胞色素c的释放,从而减轻鱼藤酮诱导的多巴胺能神经元损失,如纹状体中酪氨酸羟化酶(TH)免疫染色所证明[3]。

[体内研究]

鱼藤酮引起兴奋性氨基酸神经递质的显着增加;在大鼠PD模型的小脑中观察到谷氨酸和天冬氨酸以及抑制性氨基酸,GABA,甘氨酸和牛磺酸的显着减少[1]。鱼藤酮(1.5,2或2.5 mg/kg)引起黑质中α-突触核蛋白的剂量依赖性增加。此外,在2和2.5 mg/kg时,鱼藤酮导致黑质中酪氨酸羟化酶免疫反应神经元和大鼠纹状体中多巴胺的数量显着减少[4]。

[参考文献]

[1]. Khadrawy YA, et al. Cerebellar neurochemical and histopathological changes in rat model of Parkinson's disease induced by intrastriatal injection of rotenone. Gen Physiol Biophys. 2016 Nov 30

[2]. Guan Q, et al. RNA-Seq Expression Analysis of Enteric Neuron Cells with Rotenone Treatment and Prediction of Regulated Pathways. Neurochem Res. 2016 Nov 30

[3]. Kishore Kumar SN, et al. Morinda citrifolia mitigates rotenone-induced striatal neuronal loss in male Sprague-Dawley rats by preventing mitochondrial pathway of intrinsic apoptosis. Redox Rep. 2016 Nov 24:1-12

[4]. Zhang ZN, et al. Subcutaneous rotenone rat model of Parkinson's disease: dose exploration study. Brain Res. 2016 Nov 19. pii: S0006-8993(16)30776-4

[相关活性小分子]

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
559.8±50.0 °C at 760 mmHg

[ 熔点 ]:
159-164 °C(lit.)

[ 分子式 ]:
C₂₃H₂₂O₆

[ 分子量 ]:
394.417

[ 闪点 ]:
244.6±30.2 °C

[ 精确质量 ]:
394.141632

[ PSA ]:
63.22000

[ LogP ]:
4.65

[ 外观性状 ]:
无色斜方片状结晶。

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.591

[ 储存条件 ]:
室温，避光

[ 稳定性 ]:
Stable, but light and air sensitive. Combustible. Incompatible with oxidizing agents, especially in the presence of alkalies.

详细MSDS(安全技术说明书)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DJ2800000

CHEMICAL NAME :: (1)Benzopyrano(3,4-b)furo(2,3-h)(1)benzopyran-6(6ah)- one, 1,2,12,12a-tetrahydro-2-alpha- isopropenyl-8,9-dimethoxy-

CAS REGISTRY NUMBER :: 83-79-4

LAST UPDATED :: 199803

DATA ITEMS CITED :: 71

MOLECULAR FORMULA :: C23-H22-O6

MOLECULAR WEIGHT :: 394.45

WISWESSER LINE NOTATION :: T G5 D6 B666 CV HO MO POT&TT&J IY1&U1 SO1 TO1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: Standard Draize test

ROUTE OF EXPOSURE :: Administration into the eye

SPECIES OBSERVED :: Rodent - rabbit

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 143 mg/kg

TOXIC EFFECTS :: Gastrointestinal - other changes

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 294 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 mg/kg

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

TYPE OF TEST :: LCLo - Lowest published lethal concentration

ROUTE OF EXPOSURE :: Inhalation

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 500 mg/m3/30M

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

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

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >940 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1600 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - coma Cardiac - pulse rate increase, without fall in BP

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 200 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - coma Cardiac - pulse rate increase, without fall in BP

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 132 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2800 ug/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2650 ug/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 300 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - nausea or vomiting

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 650 ug/kg

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation Gastrointestinal - nausea or vomiting

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 650 ug/kg

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation Gastrointestinal - nausea or vomiting

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1600 mg/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - hypermotility, diarrhea

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

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >1 gm/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 20 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 350 ug/kg

TOXIC EFFECTS :: Behavioral - ataxia Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - respiratory stimulation

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 5 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - pig

DOSE/DURATION :: 3700 ug/kg

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - nausea or vomiting

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - chronic pulmonary edema Gastrointestinal - ulceration or bleeding from stomach

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 10 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Bird - pigeon

DOSE/DURATION :: 1 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation Gastrointestinal - nausea or vomiting

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Bird - duck

DOSE/DURATION :: >2 gm/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Amphibian - frog

DOSE/DURATION :: 4 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1505 mg/kg/14D-C

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5460 mg/kg/13W-C

TOXIC EFFECTS :: Liver - changes in liver weight Blood - changes in bone marrow (not otherwise specified) Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 54600 mg/kg/13W-C

TOXIC EFFECTS :: Liver - changes in liver weight Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - hamster

DOSE/DURATION :: 180 mg/kg/9D-C

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - chronic pulmonary edema Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3245 mg/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Endocrine - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 71 mg/kg/42D-I

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Skin and Appendages - tumors

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 68 mg/kg/40D-I

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Skin and Appendages - tumors

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3285 mg/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Endocrine - thyroid tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 100 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 50 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2960 ug/kg

SEX/DURATION :: female 6-9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 98 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - live birth index (measured after birth)

MUTATION DATA

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TEST SYSTEM :: Rodent - hamster Lung

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 263,173,1991 *** REVIEWS *** ACGIH TLV-Not classifiable as a human carcinogen DTLVS* The Threshold Limit Values (TLVs) and Biological Exposure Indices (BEIs) booklet issues by American Conference of Governmental Industrial Hygienists (ACGIH), Cincinnati, OH, 1996 Volume(issue)/page/year: TLV/BEI,1997 ACGIH TLV-TWA 5 mg/m3 DTLVS* The Threshold Limit Values (TLVs) and Biological Exposure Indices (BEIs) booklet issues by American Conference of Governmental Industrial Hygienists (ACGIH), Cincinnati, OH, 1996 Volume(issue)/page/year: TLV/BEI,1997 TOXICOLOGY REVIEW CTRRDO Cancer Treatment Reports. (Washington, DC) V.60-71, 1976-87. For publisher information, see JNCIEQ. Volume(issue)/page/year: 60,1171,1976 *** U.S. STANDARDS AND REGULATIONS *** EPA FIFRA 1988 PESTICIDE SUBJECT TO REGISTRATION OR RE-REGISTRATION FEREAC Federal Register. (U.S. Government Printing Office, Supt. of Documents, Washington, DC 20402) V.1- 1936- Volume(issue)/page/year: 54,7740,1989 MSHA STANDARD-air:TWA 5 mg/m3 DTLVS* The Threshold Limit Values (TLVs) and Biological Exposure Indices (BEIs) booklet issues by American Conference of Governmental Industrial Hygienists (ACGIH), Cincinnati, OH, 1996 Volume(issue)/page/year: 3,224,1971 OSHA PEL (Gen Indu):8H TWA 5 mg/m3 CFRGBR Code of Federal Regulations. (U.S. Government Printing Office, Supt. of Documents, Washington, DC 20402) Volume(issue)/page/year: 29,1910.1000,1994 OSHA PEL (Construc):8H TWA 5 mg/m3 CFRGBR Code of Federal Regulations. (U.S. Government Printing Office, Supt. of Documents, Washington, DC 20402) Volume(issue)/page/year: 29,1926.55,1994 OSHA PEL (Shipyard):8H TWA 5 mg/m3 CFRGBR Code of Federal Regulations. (U.S. Government Printing Office, Supt. of Documents, Washington, DC 20402) Volume(issue)/page/year: 29,1915.1000,1993 OSHA PEL (Fed Cont):8H TWA 5 mg/m3 CFRGBR Code of Federal Regulations. (U.S. Government Printing Office, Supt. of Documents, Washington, DC 20402) Volume(issue)/page/year: 41,50-204.50,1994 *** OCCUPATIONAL EXPOSURE LIMITS *** OEL-AUSTRALIA:TWA 5 mg/m3 JAN 1993 OEL-BELGIUM:TWA 5 mg/m3 JAN 1993 OEL-DENMARK:TWA 5 mg/m3 JAN 1993 OEL-FINLAND:TWA 5 mg/m3;STEL 10 mg/m3 JAN 1993 OEL-GERMANY:TWA 5 mg/m3 JAN 1993 OEL-THE NETHERLANDS:TWA 5 mg/m3 JAN 1993 OEL-THE PHILIPPINES:TWA 5 mg/m3 JAN 1993 OEL-SWITZERLAND:TWA 5 mg/m3 JAN 1993 OEL-TURKEY:TWA 5 mg/m3 JAN 1993 OEL-UNITED KINGDOM:TWA 5 mg/m3;STEL 10 mg/m3 JAN 1993 OEL IN BULGARIA, COLOMBIA, JORDAN, KOREA check ACGIH TLV OEL IN NEW ZEALAND, SINGAPORE, VIETNAM check ACGIH TLV *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH RECOMMENDED EXPOSURE LEVEL (REL) : NIOSH REL TO ROTENONE-air:10H TWA 5 mg/m3 REFERENCE : NIOSH* National Institute for Occupational Safety and Health, U.S. Dept. of Health, Education, and Welfare, Reports and Memoranda. Volume(issue)/page/year: DHHS #92-100,1992 NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 67530 No. of Facilities: 70 (estimated) No. of Industries: 3 No. of Occupations: 4 No. of Employees: 2937 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 67530 No. of Facilities: 913 (estimated) No. of Industries: 3 No. of Occupations: 3 No. of Employees: 8100 (estimated) No. of Female Employees: 2470 (estimated)

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[ 符号 ]:

GHS06, GHS09

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H315-H319-H335-H410

[ 警示性声明 ]:
P273-P280-P301 + P310 + P330-P337 + P313-P391-P501

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T:Toxic;N:Dangerousfortheenvironment;

[ 风险声明 (欧洲) ]:
R25;R36/37/38;R50/53

[ 安全声明 (欧洲) ]:
22-24/25-36-45-60-61

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
DJ2800000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

详细合成路线

鱼藤酮上游产品

鱼藤酮下游产品

1.用有机溶剂萃取含有鱼藤酮的植物，如鱼藤属、醉鱼豆料或灰叶属植物的根部，然后浓缩萃取液，过滤，可得结晶产品。

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DNA-dependent protein kinase catalytic subunit (DNA-PKcs) and ataxia telangiectasia mutated (ATM) are the two major kinases involved in DNA double-strand break (DSB) repair, and are required for cellu...

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公司名：上海吉至生化科技有限公司

区域：上海市奉贤区

价格：
￥198.0/1g

联系人：刘佳

产品详情：鱼藤酮

公司名：上海脉铂医药科技有限公司

区域：上海市嘉定区

价格：
￥539.0/1g ￥1089.0/5g ￥589.0/1g ￥需询单/1g

联系人：李先生

产品详情：Rotenone

公司名：上海创赛科技有限公司