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羟基保泰松

羟基保泰松用途

Oxyphenbutazone 是一种苯丁酮衍生物,具有抗炎作用。Oxyphenbutazone 是一种非选择性的 COX 抑制剂。Oxyphenbutazone 能选择性地杀死不复制的结核分枝杆菌。

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羟基保泰松名称

[ CAS 号 ]:
129-20-4

[ 中文名 ]:
羟保松

[ 英文名 ]:
G-29701

[中文别名 ]:

羟布宗

[英文别名 ]:

p-Oxyphenylbutazone
oxyphenbutazon
Oxazolidin
ossifenbutazone
EINECS 204-936-2
oxyphenylbutazone
MFCD00057278
Idrobutazina
Oxyphenbutazone
Tanderil

羟基保泰松生物活性

[ 描述 ]:

Oxyphenbutazone 是一种苯丁酮衍生物,具有抗炎作用。Oxyphenbutazone 是一种非选择性的 COX 抑制剂。Oxyphenbutazone 能选择性地杀死不复制的结核分枝杆菌。

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 感染

研究领域 >> 炎症/免疫

信号通路 >> 免疫及炎症 >> COX

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

COX[1]

[体外研究]

扑热息痛增强甲氨蝶呤(MTX)对Hep3B细胞的抗癌作用[1]。噻吩丁氮酮(2.5-7.5μM；48小时)与(MTX,0.25-1.0μM)共处理对Hep3B细胞具有潜在的细胞毒性[1]。扑热息痛对肝细胞具有修复作用[1]。细胞毒性试验[1]细胞株：Hep3B细胞浓度：2.5μM、5μM、7.5μM孵育时间：48h结果：增强了MTX的细胞毒性。

[体内研究]

当与甲氨喋呤(5.0或2.5 mg/kg/周；i.p.)联合治疗时,扑热息痛(70 mg/kg/周；p.o.；分两次给药；13周)具有潜在的抗癌活性[1]。动物模型：5-6周Wistar品系白化雄性大鼠(150-220g)[1]剂量：70mg/kg/周(与MTX 5.0或2.5mg/kg/周联合治疗)给药：口服；每周1次；分两次给药；13周结果：与MTX联合治疗时,大鼠表现出潜在的抗癌活性。

[参考文献]

[1]. Saleem S, et al. Oxyphenbutazone promotes cytotoxicity in rats and Hep3B cellsvia suppression of PGE2 and deactivation of Wnt/β-catenin signaling pathway. Mol Cell Biochem. 2018 Jul;444(1-2):187-196.

[2]. Gold B, et al. Nonsteroidal anti-inflammatory drug sensitizes Mycobacterium tuberculosis to endogenous and exogenous antimicrobials. Proc Natl Acad Sci U S A. 2012 Oct 2;109(40):16004-11.

羟基保泰松物理化学性质

[ 密度 ]:
1.241g/cm3

[ 沸点 ]:
485.6ºC at 760mmHg

[ 熔点 ]:
109-111°C

[ 分子式 ]:
C₁₉H₂₀N₂O₃

[ 分子量 ]:
324.37400

[ 闪点 ]:
247.5ºC

[ 精确质量 ]:
324.14700

[ PSA ]:
60.85000

[ LogP ]:
3.62340

[ 蒸汽压 ]:
4.7E-10mmHg at 25°C

[ 折射率 ]:
1.61

[ 储存条件 ]:
Hygroscopic, -20°C Freezer, Under Inert Atmosphere

羟基保泰松MSDS

羟基保泰松毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UQ8400000

CHEMICAL NAME :: 3,5-Pyrazolidinedione, 4-butyl-1-(p-hydroxyphenyl)-2-phenyl-

CAS REGISTRY NUMBER :: 129-20-4

BEILSTEIN REFERENCE NO. :: 0307474

LAST UPDATED :: 199612

DATA ITEMS CITED :: 24

MOLECULAR FORMULA :: C19-H20-N2-O3

MOLECULAR WEIGHT :: 324.41

WISWESSER LINE NOTATION :: T5VNNV EHJ BR DQ& CR& E4

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 420 mg/kg/4W-I

TOXIC EFFECTS :: Liver - hepatitis (hepatocellular necrosis), diffuse Blood - agranulocytosis Blood - thrombocytopenia

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 27 mg/kg/14D

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting Blood - hemorrhage

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 50 mg/kg/7D

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure) Nutritional and Gross Metabolic - body temperature increase

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 24 mg/kg/4D

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of salivary glands Endocrine - other changes

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 329 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 145 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 68 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 :: 330 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold

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 :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 52 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 178 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 104 mg/kg

TOXIC EFFECTS :: Brain and Coverings - recordings from specific areas of CNS Behavioral - excitement Lungs, Thorax, or Respiration - respiratory stimulation

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 1165 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 - hamster

DOSE/DURATION :: 1180 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

DOSE :: 560 mg/kg

SEX/DURATION :: male 28 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - male fertility index (e.g. # males impregnating females per # males exposed to fertile nonpregnant females)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 100 mg/kg

SEX/DURATION :: female 10 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - mating performance (e.g. # sperm positive females per # females mated; # copulations per # estrus cycles)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 700 mg/kg

SEX/DURATION :: female 1-7 day(s) after conception

TOXIC EFFECTS :: 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 :: 700 mg/kg

SEX/DURATION :: female 10-16 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 :: Mold - Aspergillus nidulans

DOSE/DURATION :: 1 gm/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 26,159,1974 *** REVIEWS *** IARC Cancer Review:Human No Adequate Data 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: 13,183,1977 IARC Cancer Review:Animal No Adequate Data 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: 13,183,1977 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: 7,56,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5469 No. of Facilities: 25 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 290 (estimated) No. of Female Employees: 121 (estimated)

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羟基保泰松安全信息

[ 符号 ]:

GHS07, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H400

[ 警示性声明 ]:
P273

[ 危害码 (欧洲) ]:
Xn,N

[ 风险声明 (欧洲) ]:
22-50

[ 安全声明 (欧洲) ]:
61

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

[ WGK德国 ]:
3

[ 海关编码 ]:
2933990090

羟基保泰松合成路线

羟基保泰松上下游产品

羟基保泰松上游产品

羟基保泰松下游产品

羟基保泰松海关

[ 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%

羟基保泰松文献

Bone marrow depression due to mianserin, phenylbutazone, oxyphenbutazone, and chloramphenicol--Part I.

Adverse Drug React. Acute Poisoning Rev. 5(2) , 97-136, (1986)

Bone marrow depression due to mianserin, phenylbutazone, oxyphenbutazone, and chloramphenicol--Part II.

Adverse Drug React. Acute Poisoning Rev. 5(3) , 181-96, (1986)

Disposition and tolerance of suxibuzone in horses.

Equine Vet. J. 31(5) , 411-6, (1999)

Suxibuzone (SBZ), a nonsteroidal anti-inflammatory drug, was administered to 6 horses at a dose rate of 7.5 mg/kg bwt by intravenous (i.v.) route. Plasma and synovial fluid concentrations of suxibuzon...

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