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二氟尼柳

二氟尼柳用途

Diflunisal (MK-647) 是一种水杨酸盐衍生物,具有非甾体抗炎和尿酸舒缓性能,可单独用作止痛剂和类风湿关节炎患者。Diflunisal是环氧合酶 (COX) 的抑制剂。

二氟尼柳名称

[ CAS 号 ]:
22494-42-4

[ 中文名 ]:
二氟尼柳

[ 英文名 ]:
Diflunisal

[中文别名 ]:

[英文别名 ]:

Dolobil
Difludol
Dolisal
2',4'-Difluoro-4-hydroxy-3-biphenylcarboxylic acid
Flustar
4',6'-difluoro-4-hydroxybiphenyl-3-carboxylic acid
Dolobis
Diflunisal
EINECS 245-034-9
Fluodonil

二氟尼柳生物活性

[ 描述 ]:

Diflunisal (MK-647) 是一种水杨酸盐衍生物,具有非甾体抗炎和尿酸舒缓性能,可单独用作止痛剂和类风湿关节炎患者。Diflunisal是环氧合酶 (COX) 的抑制剂。

[ 相关类别 ]:

研究领域 >> 炎症/免疫

[ 靶点 ]

COX

[体内研究]

向大鼠施用递增剂量的二氟尼柳表明剂量对二氟尼柳的药代动力学的影响非常复杂。二氟尼柳的血浆浓度随时间呈指数下降,尽管半衰期随着剂量的增加而增加。当剂量从3mg/kg增加至10mg/kg时,CLP显着降低,然后在10至60mg/kg的剂量范围内保持相对恒定。已显示二氟尼柳与大鼠血浆蛋白高度结合并且依赖于浓度。未结合的二氟尼柳的比例在5至300μg/ mL的浓度范围内增加约10倍[1]。 Diflunisal口服后表现出活性,其效力比阿司匹林高约25倍,约为glafenine的3倍,是zomepirac的2倍[2]。

[动物实验]

大鼠[1]对于剂量依赖性的研究，通过注射给予二氟尼柳，剂量为3,10,30和60mg / kg（1.5,5,15和30mg / mL给药溶液，在0.1M NaHCO 3中）。输注研究包括推注注射二氟尼柳，然后立即以恒定速率输注7小时。输注研究中包括七组大鼠。使用的负荷剂量为2,3,5,10,25,50和80 mg / kg，相应的输注速度分别为3,4.5,9,18,36,72和144μg/ min（0.576 mL / hr，7不同的给药溶液：在0.1M NaHCO 3中的0.31,0.47,0.94,1.88,3.75,7.5和15mg / mL。在适当的时间连续收集血液样品用于剂量依赖性研究，但是每小时收集用于输注研究。通过离心血样立即获得血浆，并用乙腈提取，然后冷冻（-20℃）直至测定[1]。

[参考文献]

[1]. Lin JH, et al. Dose-dependent pharmacokinetics of diflunisal in rats: dual effects of protein binding and metabolism. J Pharmacol Exp Ther. 1985 Nov;235(2):402-6.

[2]. Winter CA, et al. Analgesic activity of diflunisal [MK-647; 5-(2,4-difluorophenyl)salicylic acid] in rats with hyperalgesia induced by Freund's adjuvant. J Pharmacol Exp Ther. 1979 Dec;211(3):678-85.

[3]. Cappon GD, et al. Relationship between cyclooxygenase 1 and 2 selective inhibitors and fetal development when administered to rats and rabbits during the sensitive periods for heart development and midline closure. Birth Defects Res B Dev Reprod Toxicol. 2003 Feb;68(1):47-56.

[相关活性小分子]

二氟尼柳物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
386.9±42.0 °C at 760 mmHg

[ 熔点 ]:
32-36 °C

[ 分子式 ]:
C₁₃H₈F₂O₃

[ 分子量 ]:
250.198

[ 闪点 ]:
187.8±27.9 °C

[ 精确质量 ]:
250.044144

[ PSA ]:
57.53000

[ LogP ]:
4.44

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.0±0.9 mmHg at 25°C

[ 折射率 ]:
1.601

[ 储存条件 ]:
Refrigerator

二氟尼柳MSDS

详细MSDS(安全技术说明书)

二氟尼柳毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DV2030000

CHEMICAL NAME :: 3-Biphenylcarboxylic acid, 2',4'-difluoro-4-hydroxy-

CAS REGISTRY NUMBER :: 22494-42-4

LAST UPDATED :: 199806

DATA ITEMS CITED :: 18

MOLECULAR FORMULA :: C13-H8-F2-O3

MOLECULAR WEIGHT :: 250.21

WISWESSER LINE NOTATION :: QVR BQ ER BF DF

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 71 mg/kg/5D-I

TOXIC EFFECTS :: Behavioral - tolerance Liver - jaundice, cholestatic

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 429 mg/kg/17W-I

TOXIC EFFECTS :: Blood - agranulocytosis Nutritional and Gross Metabolic - body temperature increase

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 392 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 :: 159 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 - rat

DOSE/DURATION :: 185 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 :: 439 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 124 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 :: 212 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 :: 603 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 800 mg/kg/4D-I

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9400 mg/kg/14W-I

TOXIC EFFECTS :: Gastrointestinal - other changes Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 520 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 780 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Sister chromatid exchange

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 350 mg/kg

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 370,1,1996 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X6814 No. of Facilities: 16 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 94 (estimated) No. of Female Employees: 62 (estimated)

二氟尼柳安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335-H361

[ 警示性声明 ]:
P280-P301 + P312 + P330-P305 + P351 + P338

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22;R36/37/38;R63

[ 安全声明 (欧洲) ]:
S22-S26-S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
DV2030000

[ 海关编码 ]:
2918290000

二氟尼柳合成路线

详细合成路线

二氟尼柳上下游产品

二氟尼柳上游产品

二氟尼柳下游产品

二氟尼柳海关

[ 海关编码 ]: 2922299090

[ 中文概述 ]:
2922299090. 其他氨基(萘酚、酚)及醚、酯〔包括它们的盐, 但含有一种以上含氧基的除外〕. 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:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ Summary ]:
2922299090. other amino-naphthols and other amino-phenols, other than those containing more than one kind of oxygen function, their ethers and esters; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

二氟尼柳文献

Synthesis and biological evaluation of amide derivatives of diflunisal as potential anti-tumor agents.

Bioorg. Med. Chem. Lett. 19(15) , 4399-402, (2009)

To discover the new medicinal activity, the structure of diflunisal has been modified. Forty amide derivatives of diflunisal were synthesized starting from diflunisal in three steps. Their inhibition ...

Evaluation of the drug-polymer interaction in calcium alginate beads containing diflunisal.

Pharmazie 65(2) , 106-9, (2010)

Calcium alginate gel beads have been developed in recent years as a unique vehicle for oral drug delivery due to their excellent biocompatibility, biodegradability, simple method of preparation, abund...

Simultaneous determination of ezetimibe and simvastatin in pharmaceutical preparations by MEKC.

J. Chromatogr. Sci. 48(2) , 95-9, (2010)

A micellar electrokinetic capillary chromatography method was developed and validated for the simultaneous determination of ezetimibe and simvastatin in pharmaceutical preparations. The influence of b...

更多文献

二氟尼柳相关知识

[二氟尼柳]-说明书-作用-二氟尼柳片副作用

2019-01-14 16:38:51

导读：二氟尼柳，本品为白色结晶，难溶于水。本品为白色结晶，难溶于水。它是水杨酸衍生物，具有解热、镇痛、抗炎作用，比阿司匹林镇痛消炎作用强且维持时间长，胃肠道刺激小。主要用于轻、中度疼痛的镇痛，如关节炎、腕、踝关节的扭伤、小手术、肿瘤等疼痛。【药品名称】通用名称：二氟尼柳片商品名称：二氟尼柳...