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肼酞嗪

肼酞嗪用途

肼屈嗪是一种口服活性降压药,通过松弛动脉血管平滑肌细胞层直接降低外周阻力。肼屈嗪具有抗氧化活性,并且抑制活性氧(ROS)释放和O2生成,IC50值分别为9.53 mM和1.19 mM[1][2]。

肼酞嗪名称

[ CAS 号 ]:
86-54-4

[ 中文名 ]:
肼酞嗪

[ 英文名 ]:
Hydralazine

[中文别名 ]:

[英文别名 ]:

肼酞嗪生物活性

[ 描述 ]:

肼屈嗪是一种口服活性降压药,通过松弛动脉血管平滑肌细胞层直接降低外周阻力。肼屈嗪具有抗氧化活性,并且抑制活性氧(ROS)释放和O2生成,IC50值分别为9.53 mM和1.19 mM[1][2]。

[ 相关类别 ]:

研究领域 >> 心血管疾病
研究领域 >> 炎症/免疫

[ 靶点 ]

IC50: 9.53 mM (ROS), 1.19 mM (O2·-)[1]


[参考文献]

[1]. Arce C, Segura-Pacheco B, Perez-Cardenas E, Taja-Chayeb L, Candelaria M, Dueñnas-Gonzalez A. Hydralazine target: from blood vessels to the epigenome. J Transl Med. 2006 Feb 28;4:10.

[2]. Leiro JM, et al. Antioxidant activity and inhibitory effects of hydralazine on inducible NOS/COX-2 gene and protein expression in rat peritoneal macrophages. Int Immunopharmacol. 2004 Feb;4(2):163-77.

肼酞嗪物理化学性质

[ 密度 ]:
1.2583 (rough estimate)

[ 沸点 ]:
276.07°C (rough estimate)

[ 熔点 ]:
172ºC

[ 分子式 ]:
C8H8N4

[ 分子量 ]:
160.17600

[ 精确质量 ]:
160.07500

[ PSA ]:
63.83000

[ LogP ]:
1.68870

[ 外观性状 ]:
黄色针状

[ 折射率 ]:
1.5872 (estimate)

肼酞嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TH8925000
CHEMICAL NAME :
Phthalazine, 1-hydrazino-
CAS REGISTRY NUMBER :
86-54-4
BEILSTEIN REFERENCE NO. :
0132615
LAST UPDATED :
199612
DATA ITEMS CITED :
29
MOLECULAR FORMULA :
C8-H8-N4
MOLECULAR WEIGHT :
160.20
WISWESSER LINE NOTATION :
T66 CNNJ BMZ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
2086 mg/kg/2Y-I
TOXIC EFFECTS :
Skin and Appendages - dermatitis, allergic (after systemic exposure)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
730 mg/kg/2Y-I
TOXIC EFFECTS :
Skin and Appendages - dermatitis, allergic (after systemic exposure)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
89 ug/kg
TOXIC EFFECTS :
Cardiac - cardiomyopathy including infarction Cardiac - changes in coronary arteries
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
90 mg/kg
TOXIC EFFECTS :
Cardiac - pulse rate increase, without fall in BP Vascular - BP lowering not characterized in autonomic section
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
25 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 :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
34 mg/kg
TOXIC EFFECTS :
Cardiac - change in rate Behavioral - somnolence (general depressed activity) Gastrointestinal - nausea or vomiting
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
122 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 - mouse
DOSE/DURATION :
100 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 :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
150 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 :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
52 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 :
Mammal - dog
DOSE/DURATION :
100 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 :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
50 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 - rabbit
DOSE/DURATION :
300 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 - guinea pig
DOSE/DURATION :
250 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3600 mg/kg/5W-I
TOXIC EFFECTS :
Blood - normocytic anemia Blood - changes in other cell count (unspecified) Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
9360 mg/kg/26W-I
TOXIC EFFECTS :
Blood - normocytic anemia 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 - mouse
DOSE/DURATION :
45427 mg/kg/2Y-C
TOXIC EFFECTS :
Tumorigenic - Carcinogenic by RTECS criteria Lungs, Thorax, or Respiration - tumors
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
7 mg/kg
SEX/DURATION :
female 34-35 week(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Unreported
DOSE :
54 mg/kg
SEX/DURATION :
female 26-39 week(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - blood and lymphatic systems (including spleen and marrow)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Unreported
DOSE :
330 mg/kg
SEX/DURATION :
female 1-22 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)
TYPE OF TEST :
Specific locus test

MUTATION DATA

TYPE OF TEST :
Unscheduled DNA synthesis
TEST SYSTEM :
Rodent - rabbit Liver
DOSE/DURATION :
5 mmol/L
REFERENCE :
PNASA6 Proceedings of the National Academy of Sciences of the United States of America. (National Academy of Sciences, Printing & Pub. Office, 2101 Constitution Ave., Washington, DC 20418) V.1- 1915- Volume(issue)/page/year: 79,1269,1982 *** REVIEWS *** IARC Cancer Review:Human Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 24,85,1980 IARC Cancer Review:Group 3 IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,222,1987 TOXICOLOGY REVIEW INTEAG Internist. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.1- 1960- Volume(issue)/page/year: 15,7,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4187 No. of Facilities: 85 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 8409 (estimated) No. of Female Employees: 7509 (estimated)

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推荐生产厂家/供应商:

公司名:上海化源世纪贸易有限公司

区域:上海市普陀区

价格:

联系人:徐经理

产品详情:Hydralazine Discontinued See: H716531


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