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安替比林

安替比林用途

Antipyrine是止痛退热剂。

安替比林名称

[ CAS 号 ]:
60-80-0

[ 中文名 ]:
安替比林

[ 英文名 ]:
Antipyrine

[中文别名 ]:

[英文别名 ]:

Anodynin
2,3-dimethyl-1-phenyl-3-pyrazolin-5-one
Azophen
Sedatin
Azophene
Fenazon
EINECS 200-486-6
Fenazone
Methozin
Parodyne

安替比林生物活性

[ 描述 ]:

Antipyrine是止痛退热剂。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 炎症/免疫

[参考文献]

[1]. Stevenson, I.H., Factors influencing antipyrine elimination. Br J Clin Pharmacol, 1977. 4(3): p. 261-5.

[相关活性小分子]

安替比林物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
319.0±0.0 °C at 760 mmHg

[ 熔点 ]:
109-111 °C(lit.)

[ 分子式 ]:
C₁₁H₁₂N₂O

[ 分子量 ]:
188.226

[ 闪点 ]:
114.8±15.0 °C

[ 精确质量 ]:
188.094955

[ PSA ]:
26.93000

[ LogP ]:
0.27

[ 外观性状 ]:
无色晶体

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.585

[ 储存条件 ]:
库房通风低温干燥

[ 稳定性 ]:
Stable. Incompatible with ammonia, strong acids, alkalies, strong oxidizing agents, metallic salts, phenol.

[ 水溶解性 ]:
1000 g/L (20 ºC)

安替比林MSDS

详细MSDS(安全技术说明书)

安替比林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CD2450000

CHEMICAL NAME :: Antipyrine

CAS REGISTRY NUMBER :: 60-80-0

LAST UPDATED :: 199701

DATA ITEMS CITED :: 23

MOLECULAR FORMULA :: C11-H12-N2-O

MOLECULAR WEIGHT :: 188.25

WISWESSER LINE NOTATION :: T5NNVJ A1 BR& E1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 74 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 :: 1705 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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1570 mg/kg

TOXIC EFFECTS :: Autonomic Nervous System - other (direct) parasympathomimetic Cardiac - other changes Nutritional and Gross Metabolic - body temperature decrease

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1310 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 :: 750 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 :: 1 gm/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 :: 500 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 - dog

DOSE/DURATION :: 500 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 - cat

DOSE/DURATION :: 1250 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - nausea or vomiting

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 700 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 :: Mammal - cat

DOSE/DURATION :: 525 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - nausea or vomiting

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Rectal

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 800 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 :: Subcutaneous

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 :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 600 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 :: Rodent - guinea pig

DOSE/DURATION :: 1400 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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 1600 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Amphibian - frog

DOSE/DURATION :: 2 gm/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 :: 361 gm/kg/92W-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Kidney, Ureter, Bladder - tumors Kidney, Ureter, Bladder - Kidney tumors

MUTATION DATA

TYPE OF TEST :: DNA inhibition

TEST SYSTEM :: Human HeLa cell

DOSE/DURATION :: 80 mmol/L

REFERENCE :: CRNGDP Carcinogenesis (London). (Oxford Univ. Press, Pinkhill House, Southfield Road, Eynsham, Oxford OX8 1JJ, UK) V.1- 1980- Volume(issue)/page/year: 13,2389,1992 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 07420 No. of Facilities: 41 (estimated) No. of Industries: 3 No. of Occupations: 3 No. of Employees: 739 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 07420 No. of Facilities: 163 (estimated) No. of Industries: 4 No. of Occupations: 7 No. of Employees: 1907 (estimated) No. of Female Employees: 1486 (estimated)

安替比林安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36-S37/39

[ 危险品运输编码 ]:
3249

[ WGK德国 ]:
1

[ RTECS号 ]:
CD2450000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933110000

安替比林合成路线

详细合成路线

安替比林上下游产品

安替比林上游产品

安替比林下游产品

安替比林制备

由1-苯基-3-甲基吡唑酮-5经甲基化、水解而得。在干燥的甲基化罐中，加入吡唑酮，再加入硫酸二甲酯，升温至160℃，反应6h，加热水煮沸2h。将此甲基化反应物放入盛有氢氧化钠溶液的水解罐中，在100-110℃搅拌水解3h。静置分层，取安替比林油层放在结晶罐内，加蒸馏水稀释，搅拌，降温至10℃以下，析出晶体，甩滤，水洗，甩干得安替比林粗品。粗品用蒸馏水重结晶，活性炭脱色，即得成品。甲基化操作还可以采用氯甲烷或溴甲烷作原料，将这类甲基化试剂作成甲醇溶液，稍微过量地与1-萘基-3-甲基吡啶酮搅拌反应。然后蒸去甲醇，将反应物溶于水中，用氢氧化钠使呈微碱性，用苯萃取安替比林，再从苯中重结晶，最后用活性炭精制和水重晶。另一种方法是，用等摩尔的N，N-苯基甲基肼和乙酰乙酸乙酯在130-160℃油浴上加热回流制得。用沸水从浓稠的油状液体中萃取安替比林，然后蒸发除去水而得到晶体。

安替比林海关

[ 海关编码 ]: 2933110000

[ 中文概述 ]:
2933110000 二甲基苯基吡唑酮及其衍生物〔二甲基苯基吡唑酮即安替比林〕。监管条件:无。增值税率:17.0%。退税率:9.0%。最低关税: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 ]:
2933110000 1,5-dimethyl-2-phenyl-1h-pyrazol-3(2h)-one。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0% General tariff:20.0%

安替比林文献

Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).

J. Med. Chem. 48 , 3269-79, (2005)

Growing interest in the use of both the logarithm of the partition coefficient of the neutral species in the alkane/water system (log P(N)(alk)) and the difference between log P(N)(oct) (the logarithm...

The free radical scavenger, edaravone, ameliorates delayed neuropsychological sequelae after acute carbon monoxide poisoning in rabbits.

Undersea Hyperb. Med. 40(3) , 223-9, (2013)

The mechanism underlying delayed neuropsychological sequelae (DNS) after acute carbon monoxide (CO) poisoning is unclear. There are no effective treatments for DNS. As part of a new generation of anti...

Protective effect of edaravone against Alzheimer's disease-relevant insults in neuroblastoma N2a cells.

Neurosci. Lett. 531(2) , 160-5, (2012)

Oxidative stress has been demonstrated to be involved in the pathogenesis of Alzheimer's disease (AD). Thus, antioxidant therapy may represent a promising avenue for the treatment of AD. Edaravone (3-...

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