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噻洛芬酸

噻洛芬酸用途

Tiaprofenic acid 是一种具有抗炎镇痛作用的口服非甾体抗炎药 (NSAID)。Tiaprofenic acid 通过抑制环氧化酶 (COX) 抑制前列腺素合成。Tiaprofenic acid 可用于治疗风湿性疾病。

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噻洛芬酸名称

[ CAS 号 ]:
33005-95-7

[ 中文名 ]:
噻洛芬酸

[ 英文名 ]:
Tiaprofenic Acid

[中文别名 ]:

[英文别名 ]:

2-(5-Benzoylthiophen-2-yl)propanoic acid
Tiaprofenic acid
2-(5-Benzoylthiophen-2-yl)propionic Acid

噻洛芬酸生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> 免疫及炎症 >> COX

[体内研究]

雌性Lewis大鼠静脉注射(静脉注射)硫丙酸15mg/kg,持续输注0.02mg/min,持续6h。硫丙酸可显著降低血清硫酸盐浓度,提高硫酸盐清除率。肾脏再吸收硫酸盐的比例也显著降低[2]。

[参考文献]

[1]. G L Plosker, et al. Tiaprofenic Acid. A Reappraisal of Its Pharmacological Properties and Use in the Management of Rheumatic Diseases. Drugs. 1995 Dec;50(6):1050-75.

[2]. L J Benincosa, et al. Tiaprofenic Acid Inhibits the Renal Reabsorption of Sulfate in Rats. Prostaglandins Leukot Essent Fatty Acids. 1993 Jul;49(1):503-8.

噻洛芬酸物理化学性质

[ 密度 ]:
1.29 g/cm3

[ 沸点 ]:
450.3ºC at 760 mmHg

[ 熔点 ]:
96° (isopropyl ether)

[ 分子式 ]:
C₁₄H₁₂O₃S

[ 分子量 ]:
260.30800

[ 闪点 ]:
226.1ºC

[ 精确质量 ]:
260.05100

[ PSA ]:
82.61000

[ LogP ]:
3.16720

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 折射率 ]:
1.612

[ 储存条件 ]:
室温

[ 水溶解性 ]:
Practically insoluble in water, freely soluble in acetone, in ethanol (96 per cent) and in methylene chloride.

噻洛芬酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XM7580000

CHEMICAL NAME :: 2-Thiopheneacetic acid, 5-benzoyl-alpha-methyl-

CAS REGISTRY NUMBER :: 33005-95-7

BEILSTEIN REFERENCE NO. :: 1380662

LAST UPDATED :: 199612

DATA ITEMS CITED :: 16

MOLECULAR FORMULA :: C14-H12-O3-S

MOLECULAR WEIGHT :: 260.32

WISWESSER LINE NOTATION :: T5SJ BY1&VQ EVR

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 168 mg/kg/14D-I

TOXIC EFFECTS :: Vascular - shock Lungs, Thorax, or Respiration - other changes Gastrointestinal - ulceration or bleeding from small intestine

REFERENCE :: MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 158,647,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 672 mg/kg/7W-I

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - anorexia (human) Liver - other changes

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 1,803,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 16 mg/kg/2D-I

TOXIC EFFECTS :: Behavioral - wakefulness Behavioral - hallucinations, distorted perceptions Behavioral - excitement

REFERENCE :: CMAJAX Canadian Medical Association Journal. (Canadian Medical Assoc., POB 8650, Ottawa, ON K1G 0G8, Canada) V.1- 1911- Volume(issue)/page/year: 137,1022,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 257 mg/kg/30D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes in urine composition Kidney, Ureter, Bladder - inflammation, necrosis, or scarring of bladder

REFERENCE :: MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 160,123,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 720 mg/kg/60D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes in urine composition Kidney, Ureter, Bladder - inflammation, necrosis, or scarring of bladder

REFERENCE :: MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 160,123,1994

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 181 mg/kg

TOXIC EFFECTS :: Behavioral - antipsychotic

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 9,715,1975

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 225 mg/kg

TOXIC EFFECTS :: Behavioral - antipsychotic

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 9,715,1975

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 215 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 15,688,1984

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 690 mg/kg

TOXIC EFFECTS :: Behavioral - antipsychotic

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 9,715,1975

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 355 mg/kg

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

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4159986

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 675 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 15,688,1984 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2190 mg/kg/1Y-I

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - other changes Related to Chronic Data - death Related to Chronic Data - changes in ovarian weight

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 8,1743,1980 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1800 mg/kg

SEX/DURATION :: male 10 week(s) pre-mating female 2 week(s) pre-mating - 6 day(s) after conception

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

REFERENCE :: JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 6,195,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 7200 mg/kg

SEX/DURATION :: male 10 week(s) pre-mating female 2 week(s) pre-mating - 6 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 6,195,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 200 mg/kg

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

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

REFERENCE :: JZKEDZ Jitchuken Zenrinsho Kenkyuho. Central Institute for Experimental Animals, Research Reports. (Jikken Dobutsu Chuo Kenkyusho, 1433 Nogawa, Takatsu-ku, Kawasaki 211, Japan) V.1- 1975- Volume(issue)/page/year: 6,205,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 975 mg/kg

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

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 8,1773,1980

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噻洛芬酸安全信息

[ 危险品运输编码 ]:
UN 2811 6.1/PG III

[ RTECS号 ]:
XM7580000

[ 包装等级 ]:
III

噻洛芬酸合成路线

详细合成路线

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噻洛芬酸上游产品

噻洛芬酸下游产品

噻洛芬酸文献

The effect of terpenes on percutaneous absorption of tiaprofenic acid gel.

Arch. Pharm. Res. 33(11) , 1781-8, (2010)

Tiaprofenic acid is a potent analgesic and nonsteroidal anti-inflammatory drug (NSAID) and like any other nonsteroidal anti-inflammatory drug, oral administration of the conventional dosage forms of t...

Time-resolved spectroscopic study of the photochemistry of tiaprofenic acid in a neutral phosphate buffered aqueous solution from femtoseconds to final products.

J. Phys. Chem. B 117(3) , 811-24, (2013)

The photo-decarboxylation and overall reaction mechanism of tiaprofenic acid (TPA) was investigated by femtosecond transient absorption (fs-TA), nanosecond transient absorption (ns-TA), and nanosecond...

[New technologies in laparoscopic surgery].

Chirurg. 72(3) , 252-60, (2001)

The technology associated with endoscopic surgery continues to evolve as a result of industrial R & D and research within academic surgical departments with interest in surgical endoscopic and remote ...

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